02287nas a2200217   4500008004100000022001400041245011800055210006900173260011000242300001400352490000600366520139800372100002401770700003001794700001901824700001901843700002601862700003101888700002601919856012401945       2015                        eng d  a2040-250300a1,2,3-Triazole derivatives as antitubercular agents: synthesis, biological evaluation and molecular docking study0 a123Triazole derivatives as antitubercular agents synthesis biolo  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcMAY  a1104-11160 v63 a<p>Searching for new active molecules against Mycobacterium tuberculosis (MTB) H37Ra, a small focused library of 1,2,3-triazoles has been efficiently prepared via a click chemistry approach. The newly synthesized compounds were tested against drug-sensitive MTB. Several derivatives were found to be promising inhibitors of MTB characterized by lower MIC values (5.8-29.9 mu g mL(-1)). Among all the synthesized 31 compounds, 15e was the most active compound against MTB. Based on the results from the antitubercular activity, SAR for the synthesized series has been developed. The active compounds from the anti-tubercular study were further tested for anti-proliferative activity against THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity against these three cell lines except THP-1 at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antioxidant activities with an IC50 range of 10.1-37.3 mu g mL(-1). The molecular docking study of the synthesized compounds was performed against the DprE1 enzyme of MTB to understand the binding interactions. Moreover, the synthesized compounds were also analysed for ADME properties and all the experimental results promote us to consider this series as a starting point for the development of novel and more potent anti-tubercular agents in the future.</p>1 aShaikh, Mubarak, H.1 aSubhedar, Dnyaneshwar, D.1 aNawale, Laxman1 aSarkar, Dhiman1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/123-triazole-derivatives-antitubercular-agents-synthesis-biological-evaluation-and-000566nas a2200109   4500008004100000245009600041210006900137260009100206100001900297700001900316856012100335       2015                        eng d00aDiscovery of new chemical entities against diseases of national importance :an HTS approach0 aDiscovery of new chemical entities against diseases of national   aCombi Chem-Bio Resource Center, OCD, National Chemical Laboratory, Pune - 411 008cFEB1 aNawale, Laxman1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/discovery-new-chemical-entities-against-diseases-national-importance-hts-approach00931nas a2200121   4500008004100000245008000041210006900121260005100190520042200241100001900663700001900682856010800701       2015                        eng d00aEfficacy study of potential anti-tubercular molecules: in-vitro and ex-vivo0 aEfficacy study of potential antitubercular molecules invitro and  aNational Chemical Laboratory, Pune 411008cFEB3 a<p>Tuberculosis: Infectious disease caused by the bacillus Mycobacterium tuberculosis Second leading infectious killer after HIV/AIDS In 2013, 8.6 million TB cases were reported out of which 1.3 million died Emergence of Multi-drug resistant TB (MDR-TB) and extremely drug resistant TB (XDR) for which no drugs are available. Latency being a cause of recurring TB infection is a major problem in eradication of TB</p>1 aNawale, Laxman1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/efficacy-study-potential-anti-tubercular-molecules-vitro-and-ex-vivo01370nas a2200145   4500008004100000245011400041210006900155260009000224520069800314100001801012700001901030700002601049700001901075856013001094       2015                        eng d00aHigh throughput screening of inhibitors for tuberculosis at NCL : a novel drug discovery initiative from CSIR0 aHigh throughput screening of inhibitors for tuberculosis at NCL   aCSIR-National Chemical Laboratory, PunebCSIR-National Chemical Laboratory, PunecSEP3 a<p>Discover and develop novel drugs that are effective at curing latent, drug sensitive and drug resistant TB Study the biology of tuberculosis bacilli in great detail to identify new metabolic pathways that may be vulnerable to drugs Test thousands of potential drugs in our screening facility to find new compounds or new compound classes that kill TB bacteria Increase throughput up to 20,000 compounds at a time Develop novel screens using conditions that mimic those the TB bacteria encounters in the human body Utilize medical chemistry to optimize the structures of compounds so that they kill TB bacteria in a more potent fashion and are non-toxic Meet the challenges from industry</p>1 aManek, Hardik1 aNawale, Laxman1 aJadhav, Nandadeep, J.1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/high-throughput-screening-inhibitors-tuberculosis-ncl-novel-drug-discovery-initiative-csir01185nas a2200157   4500008004100000245010300041210006900144260005100213520053400264100001700798700001900815700001900834700001700853700002100870856013600891       2015                        eng d00aMechanistic understanding of rapid gelation of silk fibroin using a biosurfactant – sophorolipid0 aMechanistic understanding of rapid gelation of silk fibroin usin  aNational Chemical Laboratory, Pune  IndiacFEB3 a<p>3D polymeric hydrogels find use in biomedical applications as scaffolds and drug delivery vehicle • Silk fibroin a structural protein is a promising candidate (excellent thermo-mechanicals, biocompatibility, biodegradability) • Sophorolipid (SL)-a biosurfactant is known to exhibit antimicrobial, anti cancerous and cell differentiating. • Use of SL as gelling agent can enhance the applicability of SF hydrogels • SF-SL scaffolds obtained by lyophilization of hydrogels can find application in tissue regeneration</p>1 aDubey, Parul1 aNawale, Laxman1 aSarkar, Dhiman1 aNisal, Anuya1 aPrabhune, Asmita  uhttps://library.ncl.res.in/content/mechanistic-understanding-rapid-gelation-silk-fibroin-using-biosurfactant-%E2%80%93-sophorolipid02175nas a2200301   4500008004100000022001400041245010200055210006900157260009200226300001400318490000700332520111600339653001501455653002301470653002201493653001901515653001701534653002201551100002301573700002901596700001901625700001801644700002101662700002401683700001901707700002101726856012601747       2015                        eng d  a1478-641900aNew butenolide cinnamate and other biological active chemical constituents from Polygonum glabrum0 aNew butenolide cinnamate and other biological active chemical co  a4 PARK SQUARE, MILTON PARK, ABINGDON OX14 4RN, OXON, ENGLANDbTAYLOR & FRANCIS LTDcNOV  a2080-20860 v293 a<p>Phytochemical investigation of the methanol extract of the aerial parts of Polygonum glabrum afforded one new natural product (-)-2-methoxy-2-butenolide-3-cinnamate (1) along with six known compounds, -hydroxyfriedalanol (2), 3-hydroxy-5-methoxystilbene (3), (-) pinocembrin (4), sitosterol-(6-O-palmitoyl)-3-O–d-glucopyranoside (5), (-) pinocembrin-5-methyl ether (6) and sitosterol-3-O–d-glucopyranoside (7). Compound 1 showed promising in vitro anti-HIV-1 activity against primary isolates HIV-1(UG070) (X4, subtype D) and HIV-1(VB59) (R5, subtype C) assayed using TZM-bl cell line with IC50 in the range of 15.68-22.43g/mL. The extract showed TI in the range of 19.19-27.37 with IC50 in the range of 10.90-15.55g/mL. Compounds 1, 3 and 4 exhibited in vitro anti-mycobacterium activity against Mycobacterium tuberculosis H37Ra with IC50 values of 1.43, 3.33 and 1.11g/mL in dormant phase and 2.27, 3.33 and 1.21g/mL in active phase, respectively. Compound 4 was found to be the most active antiproliferative with IC50 values of 1.88-11.00g/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines.</p>10aanti-HIV-110aanti-mycobacterium10aantiproliferative10aphytochemicals10aPolygonaceae10aPolygonum glabrum1 aSaid, Madhukar, S.1 aChinchansure, Ashish, A.1 aNawale, Laxman1 aDurge, Ankita1 aWadhwani, Ashish1 aKulkarni, Smita, S.1 aSarkar, Dhiman1 aJoshi, Swati, P.  uhttps://library.ncl.res.in/content/new-butenolide-cinnamate-and-other-biological-active-chemical-constituents-polygonum-001235nas a2200145   4500008004100000245010400041210006900145260006300214520060900277100001600886700001900902700002500921700002000946856012300966       2015                        eng d00aPurification and characterization of an agglutinin from datura innoxia with antineoplastic activity0 aPurification and characterization of an agglutinin from datura i  aCSIR-National Chemical Laboratory, Pune 411008, IndiacFEB3 a<p>Lectins are carbohydrate binding proteins of non-immune origin. Due to their multivalency, lectins can be easily detected using agglutination. Lectins are reported to induce cytotoxicity or inhibition of growth in various cancer cells., hence good therapeutic startegy against cancer. Factors such as specificity, stability, assay rapidity, and costs combine to make lectins attractive diagnostic reagents. Datura innoxia belongs to family of Solanaceae.All parts of the plant are hallucinogenic, hypnotic and narcotic. Application: at low dose acts as pain killer, relieves asthma and rheumatism.</p>1 aSingh, Ruby1 aNawale, Laxman1 aGaikwad, Sushama, M.1 aSuresha, C., G.  uhttps://library.ncl.res.in/content/purification-and-characterization-agglutinin-datura-innoxia-antineoplastic-activity01479nas a2200121   4500008004100000245010000041210006900141260009100210520088800301100001901189700001901208856013001227       2015                        eng d00aQuantitative, automated, high content screening assay approach to anti-angiogenicdrug discovery0 aQuantitative automated high content screening assay approach to   aCombi Chem-Bio Resource Center, OCD, National Chemical Laboratory, Pune - 411 008cFEB3 a<p>Angiogenesisenhancescancer,maculardegeneration,etc.. Currentangiogenicassays--indirect,manual,timeconsuming,laborintensive,difficulttoquantify,andexpensive. Wedevelopedanautomated,quantitative,HighContentScreeningangiogenictubeformationassaywouldbenefitdrugdiscoveryforseveraltherapeuticareas. Humanendothelialcellswereseededwithpro-oranti-angiogeniccompoundsonaMatrigelTMlayerina96-wellplate.Afterangiogenictubesformation,thepositivecontrolsandthetestsampleswerefixed,fluorescentlylabeled,automaticallyimagedonCellomics’ArrayScan®HCSReader,andquantitativelyanalyzedon-the-flybytheTubeFormationBioApplicationsoftwaremodule. Multiplefeaturesrelevantforangiogenesisandangiogenictubeformationwereautomaticallymeasured. Thisrobustandreliableassaythusenabledthelarge-scale,quantitative,screeningandcharacterizationofcompoundsaffectingbothpro-andanti-angiogenicpathways.</p>1 aNawale, Laxman1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/quantitative-automated-high-content-screening-assay-approach-anti-angiogenicdrug-discovery01897nas a2200193   4500008004100000022001400041245010500055210006900160260011000229300001600339490000600355520112300361100001701484700001901501700001901520700001701539700002101556856012601577       2015                        eng d  a2046-206900aSophorolipid assisted tunable and rapid gelation of silk fibroin to form porous biomedical scaffolds0 aSophorolipid assisted tunable and rapid gelation of silk fibroin  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcMAR  a33955-339620 v53 a<p>Three dimensional polymer hydrogels, based on both natural and synthetic polymers, are increasingly being used as scaffolds and drug delivery vehicles for biomedical applications. Fibrous protein, silk fibroin (SF), obtained from the Bombyx mori silkworm is a promising candidate in this area. However, SF has a long gelation time of about a few weeks that can only be reduced by non-physiological treatments (e. g. high temperature, ultrasonication and low pH) or by addition of a chemical and non-biodegradable polymer and/or surfactant. We report here accelerated gelation of SF under physiological conditions using a biosurfactant, sophorolipid (SL) as a gelling agent. SL and SF are completely miscible and form a very clear solution upon mixing. Hence it is interesting to see that this clear solution gels in a time span of just a few hours. The hydrogels so formed have pore architecture, porosities and mechanical stability ideally suited for tissue culture applications. Here we also demonstrate that mouse fibroblast cells not only adhere to but also extensively proliferate on these SF-SL scaffolds.</p>1 aDubey, Parul1 aNawale, Laxman1 aSarkar, Dhiman1 aNisal, Anuya1 aPrabhune, Asmita  uhttps://library.ncl.res.in/content/sophorolipid-assisted-tunable-and-rapid-gelation-silk-fibroin-form-porous-biomedical-001969nas a2200193   4500008004100000245011800041210006900159260000800228300001400236490000700250520126100257100003001518700002401548700001901572700001701591700001901608700002601627856012201653       2016                        eng d00a[Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their antitubercular activity0 aEt3NHHSO4 catalyzed efficient synthesis of 5arylidenerhodanine c  cAUG  a6607-66260 v423 a<p>We have described a highly efficient, safer protocol for the synthesis of 5-arylidene-rhodanine conjugates catalyzed by Bronsted acidic ionic liquid [Et3NH][HSO4] in excellent yields. The protocol offers cost-effective, environmentally benign, solvent-free conditions and recycle-reuse of the catalyst. The synthesized 5-arylidene-rhodanine conjugates were characterized on the basis of (1) H NMR, C-13 NMR and HRMS spectral data. A series of 5-arylidene-rhodanine derivatives 3a-h, 4a-h were synthesized and evaluated for their in vitro antitubercular activity against dormant Mycobacterium tuberculosis H37Ra and M. bovis BCG strains. Moreover, compounds 3a, 3b, 3e, 3f, 3g, 3h and 4f exhibited good antitubercular activity and were also evaluated for anti-proliferative activity against MCF-7, A549 and HCT116 cell lines using modified MTT assay and found to be noncytotoxic. Compounds 3a-h and 4f were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards M. tuberculosis. Furthermore, in silico ADME prediction of all the tested compounds followed the criteria for orally active drug and, therefore, these compounds may have a good potential for eventual development as oral agents.</p>1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aNawale, Laxman1 aYeware, Amar1 aSarkar, Dhiman1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/et3nhhso4-catalyzed-efficient-synthesis-5-arylidene-rhodanine-conjugates-and-their02255nas a2200289   4500008004100000022001400041245010400055210006900159260010600228300001400334490000700348520119600355653001501551653001901566653001701585653001801602653002601620100003001646700002401676700001901700700001701719700001901736700002601755700003101781700002601812856012701838       2016                        eng d  a0960-894X00aNovel tetrazoloquinoline-rhodanine conjugates: highly efficient synthesis and biological evaluation0 aNovel tetrazoloquinolinerhodanine conjugates highly efficient sy  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcMAY  a2278-22830 v263 a<p>In search of new active molecules against Mycobacterium tuberculosis (MTB) H37Ra and Mycobacterium bovis BCG, a small focused library of rhodanine incorporated tetrazoloquinoline has been efficiently synthesized by using [HDBU][HSO4] acidic ionic liquid. The compound 3c found to be promising inhibitor of MTB H37Ra and M. bovis BCG characterized by lower MIC values 4.5 and 2.0 mu g/mL, respectively. The active compounds were further tested for cytotoxicity against HeLa, THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Again, the synthesized compounds were found to have potential antifungal activity. Furthermore, to rationalize the observed biological activity data, the molecular docking study also been carried out against a potential target Zmp1 enzyme of MTB H37Ra, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of in vitro and in silico study suggest that these compounds possess ideal structural requirement for the further development of novel therapeutic agents. (C) 2016 Elsevier Ltd. All rights reserved.</p>10aantifungal10aAntitubercular10aCytotoxicity10aDocking study10aRhodanine derivatives1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aNawale, Laxman1 aYeware, Amar1 aSarkar, Dhiman1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/novel-tetrazoloquinoline-rhodanine-conjugates-highly-efficient-synthesis-and-biological01988nas a2200193   4500008004100000245012200041210006900163260000800232300001400240490000600254520126200260100003001522700002401552700002601576700001901602700001901621700002301640856013101663       2016                        eng d00aNovel tetrazoloquinoline-thiazolidinone conjugates as possible antitubercular agents: synthesis and molecular docking0 aNovel tetrazoloquinolinethiazolidinone conjugates as possible an  cJUL  a1832-18480 v73 a<p>A novel approach for the synthesis of a new 4-thiazolidinone scaffold was developed by a one-pot three-component cyclocondensation of various tetrazolo quinoline aldehydes 1a-f, acid hydrazide 2a-c, and thioglycolic acid 3 in the presence of [DBUH].OAc] as a catalyst in high yields. All the conjugates were screened for their antimycobacterial activity against MTB H37Ra and M. bovis BCG strains, with the MIC values ranging from 0.99-13.55 mu mol mL(-1) and 0.14-20.11 mu mol mL(-1), respectively. The 4-thiazolidinone-incorporated tetrazoloquinoline derivatives 4a, 4d, 4g, 4j, 4m, and 4p were highly potent against MTB H37Ra and M. bovis BCG strains. The most active compounds were also evaluated for their cytotoxicity against MCF-7, A549, and HCT 116 cell lines and were found to be non-cytotoxic. Further, molecular docking studies into the active site of the InhA enzyme revealed a similar binding mode to the native ligand in the crystal structure, thereby helping us to understand the ligand-protein binding interaction and establish a structural basis for the inhibition of mycobacterium tuberculosis. The results suggest that the tetrazoloquinoline-thiazolidinone conjugates 4a, 4d, 4g, 4j, 4m, and 4p are promising antitubercular agents.</p>1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aShingate, Bapurao, B.1 aNawale, Laxman1 aSarkar, Dhiman1 aKhedkar, Vijay, M.  uhttps://library.ncl.res.in/content/novel-tetrazoloquinoline-thiazolidinone-conjugates-possible-antitubercular-agents-synthesis03131nas a2200301   4500008004100000022001400041245008900055210006900144260008400213300001600297490000700313520210200320653002802422653001702450653002002467653001702487653001802504653001702522100001702539700001902556700002402575700002102599700002502620700002002645700001902665700002602684856011902710       2016                        eng d  a1178-201300aPhytogenic silver, gold, and bimetallic nanoparticles as novel antitubercular agents0 aPhytogenic silver gold and bimetallic nanoparticles as novel ant  aPO BOX 300-008, ALBANY, AUCKLAND 0752, NEW ZEALANDbDOVE MEDICAL PRESS LTDcMAY  a1889—18970 v113 a<p>Purpose: Multi- and extensively drug-resistant tuberculosis (TB) is a global threat to human health. It requires immediate action to seek new antitubercular compounds and devise alternate strategies. Nanomaterials, in the present scenario, have opened new avenues in medicine, diagnosis, and therapeutics. In view of this, the current study aims to determine the efficacy of phytogenic metal nanoparticles to inhibit mycobacteria. Methods: Silver (AgNPs), gold (AuNPs), and gold-silver bimetallic (Au-AgNPs) nanoparticles synthesized from medicinal plants, such as Barleria prionitis, Plumbago zeylanica, and Syzygium cumini, were tested against Mycobacterium tuberculosis and M. bovis BCG. In vitro and ex vivo macrophage infection model assays were designed to determine minimum inhibitory concentration (MIC) and half maximal inhibitory concentration of nanoparticles. Microscopic analyses were carried out to demonstrate intracellular uptake of nanoparticles in macrophages. Besides this, biocompatibility, specificity, and selectivity of nanoparticles were also established with respect to human cell lines. Results: Au-AgNPs exhibited highest antitubercular activity, with MIC of &lt;2.56 mu g/mL, followed by AgNPs. AuNPs did not show such activity at concentrations of up to 100 mu g/mL. In vitro and ex vivo macrophage infection model assays revealed the inhibition of both active and dormant stage mycobacteria on exposure to Au-AgNPs. These nanoparticles were capable of entering macrophage cells and exhibited up to 45% cytotoxicity at 30 mu g/mL (ten times MIC concentration) after 48 hours. Among these, Au-AgNPs synthesized from S. cumini were found to be more specific toward mycobacteria, with their selectivity index in the range of 94-108. Conclusion: This is the first study to report the antimycobacterial activity of AuNPs, AgNPs, and Au-AgNPs synthesized from medicinal plants. Among these, Au-AgNPs from S. cumini showed profound efficiency, specificity, and selectivity to kill mycobacteria. These should be investigated further to develop novel TB nanoantibiotics.</p>10aAntimycobacterial agent10aCytotoxicity10adrug resistance10aMycobacteria10aNanoparticles10atuberculosis1 aSingh, Richa1 aNawale, Laxman1 aArkile, Manisha, A.1 aWadhwani, Sweety1 aShedbalkar, Utkarsha1 aChopade, Snehal1 aSarkar, Dhiman1 aChopade, Balu, Ananda  uhttps://library.ncl.res.in/content/phytogenic-silver-gold-and-bimetallic-nanoparticles-novel-antitubercular-agents02733nas a2200361   4500008004100000022001400041245015600055210006900211260008300280300001200363490000700375520148300382653000601865653000601871653001501877653002001892653001801912653001601930653001901946653002001965653001801985100002402003700003002027700002602057700002602083700003102109700002302140700001902163700001902182700002402201700002302225856012302248       2016                        eng d  a1054-252300aSynthesis, biological evaluation and molecular docking of novel coumarin incorporated triazoles as antitubercular, antioxidant and antimicrobial agents0 aSynthesis biological evaluation and molecular docking of novel c  a233 SPRING STREET, 6TH FLOOR, NEW YORK, NY 10013 USAbSPRINGER BIRKHAUSERcAPR  a790-8040 v253 a<p>A series of new coumarin-based 1,2,3-triazole derivatives were designed, synthesized and evaluated for their antitubercular activity in vitro against Mycobacterium tuberculosis H37Ra, antioxidant activity by DPPH radical scavenging assay, antimicrobial activity in vitro against three gram-positive bacteria (Staphylococcus aureus, Micrococcus luteus and Bacillus cereus) and three gram-negative bacteria (Escherichia coli, Pseudomonas fluorescens and Flavobacterium devorans as well as three fungi (Aspergillus niger, Penicillium chrysogenum and Curvularia lunata). The bioactive assay showed that some synthesized coumarin triazoles displayed comparable or even better antitubercular, antioxidant, antibacterial and antifungal efficacy in comparison with reference drugs. Furthermore, docking study has been performed against DprE1 enzyme of M. tuberculosis that showed good binding interactions. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug candidates. New coumarin-based 1,2,3-triazole derivatives were designed, synthesized and evaluated for their antitubercular, antioxidant, antibacterial and antifungal activity. Some of the coumarin-based triazole derivatives displayed comparable or even better efficacy in comparison with reference drugs. Molecular docking study has been performed against DprE1 enzyme of Mycobacterium tuberculosis showed good binding interactions. [GRAPHICS] .</p>10a110a210a3-Triazole10aADME prediction10aAntimicrobial10aAntioxidant10aAntitubercular10aClick chemistry10aDocking study1 aShaikh, Mubarak, H.1 aSubhedar, Dnyaneshwar, D.1 aShingate, Bapurao, B.1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.1 aKhedkar, Vijay, M.1 aNawale, Laxman1 aSarkar, Dhiman1 aNavale, Govinda, R.1 aShinde, Sandip, S.  uhttps://library.ncl.res.in/content/synthesis-biological-evaluation-and-molecular-docking-novel-coumarin-incorporated-102543nas a2200325   4500008004100000022001400041245016900055210006900224260010700293300001400400490000700414520138800421653000601809653000601815653001701821653002801838653001701866653001101883653002201894653001301916100001801929700001901947700001801966700001901984700001902003700002302022700002102045700001902066856013202085       2016                        eng d  a0960-894X00aSynthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents0 aSynthesis biological evaluation and molecular docking study of s  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcAPR   a1776-17830 v263 a<p>A series of indole and pyridine based 1,3,4-oxadiazole derivatives 5a-t were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG both in active and dormant state. Compounds 5b, 5e, 5g and 5q exhibited very good antitubercular activity. All the newly synthesized compounds 5a-t were further evaluated for antiproliferative activity against HeLa, A549 and PANC-1 cell lines using modified MTT assay and found to be noncytotoxic. On the basis of cytotoxicity and MIC values against Mycobacterium bovis BCG, selectivity index (SI) of most active compounds 5b, 5e, 5g and 5q was calculated (SI = GI(50)/MIC) in active and dormant state. Compounds 5b, 5e and 5g demonstrated SI values &gt;= 10 against all three cell lines and were found to safe for advance screening. Compounds 5a-t were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards MTB. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of enoyl reductase (InhA), which in turn helped to establish a structural basis of inhibition of mycobacteria. The potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for further optimization. (C) 2016 Elsevier Ltd. All rights reserved.</p>10a110a310a4-Oxadiazole10aAntitubercular activity10aCytotoxicity10aIndole10aMolecular docking10aPyridine1 aDesai, N., C.1 aSomani, Hardik1 aTrivedi, Amit1 aBhatt, Kandarp1 aNawale, Laxman1 aKhedkar, Vijay, M.1 aJha, Prakash, C.1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/synthesis-biological-evaluation-and-molecular-docking-study-some-novel-indole-and-pyridine-002253nas a2200181   4500008004100000022001400041245014600055210006900201260009100270300002900361490000700390520147700397100001601874700001901890700001901909700001901928856012401947       2016                        eng d  a1932-620300aTwo chitotriose-specific lectins show anti-angiogenesis, induces caspase-9-mediated apoptosis and early arrest of pancreatic tumor cell cycle0 aTwo chitotriosespecific lectins show antiangiogenesis induces ca  a1160 BATTERY STREET, STE 100, SAN FRANCISCO, CA 94111 USAbPUBLIC LIBRARY SCIENCEcJAN  aArticle Number: e01461100 v113 a<p>The antiproliferative activity of two chito-specific agglutinins purified from Benincasa hispida (BhL) and Datura innoxia (DiL9) of different plant family origin was investigated on various cancer cell lines. Both lectins showed chitotriose specificity, by inhibiting lectin hemagglutinating activity. On further studies, it was revealed that these agglutinins caused remarkable concentration-dependent antiproliferative effect on human pancreatic cancerous cells but not on the normal human umbilical vein endothelial cells even at higher doses determined using MTT assay. The GI(50) values were approximately 8.4 mu g ml(-1) (0.247 mu M) and 142 mu g ml(-1) (14.8 mu M) for BhL and DiL9, respectively, against PANC-1 cells. The growth inhibitory effect of these lectins on pancreatic cancer cells were shown to be a consequence of lectin cell surface binding and triggering G(0)/G(1) arrest, mitochondrial membrane depolarization, sustained increase of the intracellular calcium release and the apoptotic signal is amplified by activation of caspases executing cell death. Interestingly, these lectins also showed anti-angiogenic activity by disrupting the endothelial tubulogenesis. Therefore, we report for the first time two chito-specific lectins specifically binding to tumor glycans; they can be considered to be a class of molecules with antitumor activity against pancreatic cancer cells mediated through caspase dependent mitochondrial apoptotic pathway.</p>1 aSingh, Ruby1 aNawale, Laxman1 aSarkar, Dhiman1 aSuresh, C., G.  uhttps://library.ncl.res.in/content/two-chitotriose-specific-lectins-show-anti-angiogenesis-induces-caspase-9-mediated-102007nas a2200181   4500008004100000245012400041210006900165260000800234300001300242490000800255520133400263100001901597700001701616700002301633700001901656700002101675856012901696       2017                        eng d00aAnti-proliferative effect of novel primary cetyl alcohol derived sophorolipids against human cervical cancer cells HeLa0 aAntiproliferative effect of novel primary cetyl alcohol derived   cAPR  ae01742410 v12 3 aSophorolipids (SLs) are glycolipid biosurfactants that have been shown to display anticancer activity. In the present study, we report anti-proliferative studies on purified forms of novel SLs synthesized using cetyl alcohol as the substrate (referred as SLCA) and their anticancer mechanism in human cervical cancer cells. Antiproliferative effect of column purified SLCA fractions (A, B, C, D, E and F) was examined in panel of human cancer cell lines as well as primary cells. Among these fractions, SLCA B and C significantly inhibited the survival of HeLa and HCT 116 cells without affecting the viability of normal human umbilical vein endothelial cells (HUVEC). The two fractions were identified as cetyl alcohol sophorolipids with non-hydroxylated tail differing in the degree of acetylation on sophorose head group. At an IC50 concentration SLCA B (16.32 mu g ml(-1)) and SLCA C (14.14 mu g ml(-1)) blocked the cell cycle progression of HeLa cells at G1/S phase in time-dependent manner. Moreover, SLCA B and SLCA C induced apoptosis in HeLa cells through an increase in intracellular Ca2+ leading to depolarization of mitochondrial membrane potential and increase in the caspase-3, -8 and -9 activity. All these findings suggest that these SLCAs could be explored for their chemopreventive potential in cervical cancer.1 aNawale, Laxman1 aDubey, Parul1 aChaudhari, Bhushan1 aSarkar, Dhiman1 aPrabhune, Asmita  uhttps://library.ncl.res.in/content/anti-proliferative-effect-novel-primary-cetyl-alcohol-derived-sophorolipids-against-human00768nas a2200193   4500008004100000245016500041210006900206260000800275300001400283490000700297100002300304700002200327700002000349700002800369700001900397700002000416700001900436856011900455       2017                        eng d00aClick-chemistry-based multicomponent condensation approach for design and synthesis of spirochromene-tethered 1,2,3-triazoles as potential antitubercular agents0 aClickchemistrybased multicomponent condensation approach for des  cOCT  a5675-56900 v431 aChavan, Pramod, V.1 aPandit, Kapil, S.1 aDesai, Uday, V.1 aWadgaonkar, Prakash, P.1 aNawale, Laxman1 aBhansali, Sujit1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/click-chemistry-based-multicomponent-condensation-approach-design-and-synthesis01956nas a2200217   4500008004100000245008100041210006900122260000800191300001400199490000800213520120400221100003001425700002401455700002601479700001901505700001901524700002301543700002601566700003101592856011501623       2017                        eng d00aQuinolidene-rhodanine conjugates: facile synthesis and biological evaluation0 aQuinolidenerhodanine conjugates facile synthesis and biological   cJAN  a385–3990 v1253 a<p>A series of rhodanine incorporated quinoline derivatives were efficiently synthesized using reusable DBU acetate as ionic liquid and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) both in active and dormant state. Compounds 3e, 3f, 3g, 3h and 3i exhibited very good antitubercular activity. The active compounds were studied for cytotoxicity against HUVEC, THP-1, macrophages, A549, PANC-1 and HeLa cell lines using modified MTT assay and were found to be noncytotoxic. Inactivity of all these compounds against Gram positive and Gram negative bacteria indicates their specificity towards the MTB. Further, the synthesized compounds have been screened for their in vitro antifungal activity. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of Zmp1 enzyme, which in turn helped to establish a structural basis of inhibition of mycobacteria. The results of present study clearly indicate the identification of some novel, selective and specific inhibitors against MTB that can be explored further for potential antitubercular drug.</p>1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aShingate, Bapurao, B.1 aNawale, Laxman1 aSarkar, Dhiman1 aKhedkar, Vijay, M.1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.  uhttps://library.ncl.res.in/content/quinolidene-rhodanine-conjugates-facile-synthesis-and-biological-evaluation01753nas a2200229   4500008004100000245008300041210006900124260000800193300001200201490000800213520098800221100002301209700002101232700002401253700002501277700002501302700002001327700001901347700001901366700002301385856011501408       2017                        eng d00aSynthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives0 aSynthesis and antimycobacterial screening of new thiazolyloxazol  cMAY  a333-3400 v1323 a<p>In the present study a series of 4-methyl-2-aryl-5-(2-aryl/benzyl thiazol-4-yl) oxazole (4a-v) have been synthesized and evaluated for their preliminary antitubercular, antimicrobial and cytotoxicity activity. Among all the synthesized compounds, 4v reported comparable activity against dormant M. tuberculosis H37Ra and M. bovis BCG strains with respect to standard drug rifampicin. The active compounds from the antitubercular study were further tested for anti-proliferative activity against HeLa, A549 and PANC-1 cell lines using MU assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activities with MIC range of 2.1-26.8 mu g/mL. High potency, lower cytotoxicity and promising antimycobacterial activity suggested that these compounds could serve as good leads for further optimisation and development. (C) 2017 Elsevier Masson SAS. All rights reserved.</p>1 aAbhale, Yogita, K.1 aSasane, Amit, V.1 aChavan, Abhijit, P.1 aShekh, Saddam, Husen1 aDeshmukh, Keshav, K.1 aBhansali, Sujit1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C.  uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-screening-new-thiazolyl-oxazole-derivatives01938nas a2200217   4500008004100000245016700041210006900208260000800277300001400285490000700299520111000306100002201416700002301438700001901461700002301480700002201503700002401525700001901549700002201568856013001590       2017                        eng d00aSynthesis, biological evaluation, and molecular docking studies of novel 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles derivatives targeting Mycobacterium tuberculosis0 aSynthesis biological evaluation and molecular docking studies of  cDEC  a1206-12140 v903 aA small library of new 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles was synthesized and screened for the antimycobacterial potency against Mycobacterium tuberculosis H37Ra strain and Mycobacterium bovis BCG both in active and dormant stage. Among the synthesized library, 25 compounds exhibited promising anti-TB activity in the range of IC(50)0.03-5.88g/ml for dormant stage and 20 compounds in the range of 0.03-6.96g/ml for active stage. Their lower toxicity (>100g/ml) and higher selectivity (SI=>10) against all cancer cell lines screened make them interesting compounds with potential antimycobacterial effects. Furthermore, to rationalize the observed biological activity data and to establish a structural basis for inhibition of M.tuberculosis, the molecular docking study was carried out against a potential target MTB CYP121 which revealed a significant correlation between the binding score and biological activity for these compounds. Cytotoxicity and in vivo pharmacokinetic studies suggested that 1,2,4-triazole analogues have an acceptable safety index, in vivo stability and bio-availability.1 aRode, Navnath, D.1 aSonawane, Amol, D.1 aNawale, Laxman1 aKhedkar, Vijay, M.1 aJoshi, Ramesh, A.1 aLikhite, Anjali, P.1 aSarkar, Dhiman1 aJoshi, Rohini, R.  uhttps://library.ncl.res.in/content/synthesis-biological-evaluation-and-molecular-docking-studies-novel-3-aryl-5-alkyl-thio-1h01001nas a2200205   4500008004100000245014600041210006900187260000800256490000700264520019900271100002400470700003000494700002600524700003100550700001900581700002400600700001900624700002600643856012600669       2017                        eng d00aSynthesis of novel triazole-incorporated isatin derivatives as antifungal, antitubercular, and antioxidant agents and molecular docking study0 aSynthesis of novel triazoleincorporated isatin derivatives as an  cJAN0 v543 a<p>A library of 1,2,3-triazoles efficiently prepared via click chemistry and evaluated for their antifungal, antitubercular, antioxidant, cytotoxicity, molecular docking and ADME prediction.</p>1 aShaikh, Mubarak, H.1 aSubhedar, Dnyaneshwar, D.1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.1 aNawale, Laxman1 aArkile, Manisha, A.1 aSarkar, Dhiman1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/synthesis-novel-triazole-incorporated-isatin-derivatives-antifungal-antitubercular-and01695nas a2200181   4500008004100000245008700041210006900128260000800197300001200205490000800217520106500225100002301290700001901313700002101332700001901353700002401372856011701396       2018                        eng d00aAntibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life0 aAntibacterial and antiTB tatpeptidomimetics with improved effica  cMAY  a358-3690 v1523 aNon-natural antimicrobial peptides are ideal as next-generation antibiotics because of their ability to circumvent the problems of drug resistance and in vivo instability. We report novel all-alpha- and alpha,gamma-mixed Tat peptide analogues as potential antibacterial and anti-TB agents. These peptides have broad spectrum antibacterial activities against Gram-positive (MICs 0.61 +/- 0.03 to 1.35 +/- 0.21 mu M with the peptide gamma TatM4) and Gram-negative (MICs 0.71 +/- 0.005 to 1.26 +/- 0.02 M with gamma TatM4) bacteria and are also effective against active and dormant forms of Mycobacterium tuberculosis, including strains that are resistant to rifampicin and isoniazid. The introduction of the non-natural amino acids of the study in the Tat peptide analogues results in increased resistance to degradation by proteolysis, significantly increasing their half-life. The peptides appear to inhibit bacteria by a membrane disruption mechanism, and have only a low cytotoxic effect on mammalian cells. (C) 2018 Elsevier Masson SAS. All rights reserved.1 aBhosle, Govind, S.1 aNawale, Laxman1 aYeware, Amar, M.1 aSarkar, Dhiman1 aFernandes, Moneesha  uhttps://library.ncl.res.in/content/antibacterial-and-anti-tb-tat-peptidomimetics-improved-efficacy-and-half-life02150nas a2200313   4500008004100000022001400041245010200055210006900157260000800226300001300234490000800247520118500255653000601440653000601446653001701452653000601469653002401475653001701499653002701516653001701543653002201560100002001582700002201602700001901624700001901643700002701662700001801689856012901707       2018                        eng d  a0365-623300aDesign, synthesis, and pharmacological evaluation of fluorinated azoles as anti-tubercular agents0 aDesign synthesis and pharmacological evaluation of fluorinated a  cFEB  ae17002940 v3513 a<p>Design, synthesis, and biological screening of 2,2-dimethyl-2,3-dihydrobenzofuran tethered 1,3,4-oxadiazole derivatives as anti-tubercular agents were described. The synthesis of the target compounds was conducted by a series of reaction schemes. All the synthesized compounds were characterized by IR, H-1 NMR, C-13 NMR, and mass spectrometry. The therapeutic potential of the synthesized compounds was confirmed by molecular docking studies. Among the synthesized compounds, 12a, 12c, 12d, 12e, 12g, and 12j were found to be more active against non-replicating than against replicating cultures of Mycobacterium tuberculosis H37Ra ex vivo and in vitro. These compounds exhibit minimum inhibitory concentration (MIC) values in the range of 2.31-23.91g/mL. The cytotoxicity study was conducted against the cell lines THP-1, A549 and PANC-1, and the compounds were observed to be non-toxic to host cells. Molecular docking was conducted with InhA (FabI/ENR) and suggested the antimycobacterial potential of the synthesized compounds. The investigation presented here was found to be adventitious for the development of new therapeutic agents against Mycobacterium infection.</p>10a110a210a2-dimethyl-210a310a3-dihydrobenzofuran10a4-Oxadiazole10aanti-tubercular agents10aCytotoxicity10aMolecular docking1 aGholap, Somnath1 aTambe, Macchindra1 aNawale, Laxman1 aSarkar, Dhiman1 aSangshetti, Jaiprakash1 aDamale, Manoj  uhttps://library.ncl.res.in/content/design-synthesis-and-pharmacological-evaluation-fluorinated-azoles-anti-tubercular-agents01993nas a2200193   4500008004100000245011500041210006900156260000800225490000700233520126600240100002401506700002601530700001901556700001901575700002601594700002701620700002601647856012601673       2018                        eng d00aNovel benzylidenehydrazide-1,2,3-triazole conjugates as antitubercular agents: synthesis and molecular docking0 aNovel benzylidenehydrazide123triazole conjugates as antitubercul  cJUL0 v183 aNovel 1,2,3-triazole based benzylidenehydrazide derivatives were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra, M. bovis BCG and cytotoxic activity. Most of the derivatives exhibited promising in vitro potency against MTB characterized by lower MIC values. Among all the synthesized derivatives, compound 6a and 6j were the most active against active and dormant MTB H37Ra, respectively. Compound 6d was significantly active against dormant and active M. bovis BCG. The structure activity relationship has been explored on the basis of anti-tubercular activity data. The active compounds were also tested against THP-1, A549 and Panc-1 cell lines and showed no significant cytotoxicity. Further, the synthesized compounds were found to have potential antioxidant with IC50 range = 11.19-56.64 μg/mL. The molecular docking study of synthesized compounds was performed against DprE1 enzyme of MTB to understand the binding interactions. Moreover, synthesized compounds were also analysed for ADME properties and from all the experimental results, the potency of compounds indicate that, this series considered as starting point for the developement of novel and more potent anti-tubercular agents in future.1 aShaikh, Mubarak, H.1 aSubhedar, Dnyaneshwar1 aNawale, Laxman1 aSarkar, Dhiman1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/novel-benzylidenehydrazide-123-triazole-conjugates-antitubercular-agents-synthesis-and01951nas a2200265   4500008004100000022001400041245011500055210006900170260000800239300001400247490000700261520109200268653000601360653000601366653001501372653002701387653002801414653001301442100001801455700002201473700002301495700001901518700001901537856012901556       2018                        eng d  a0922-616800aSynthesis and biological evaluation of new 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives0 aSynthesis and biological evaluation of new 2aryl44aryl1H123triaz  cFEB  a1247-12600 v443 a<p>A series of 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives (8a-p) have been synthesized. The structure of the newly synthesized compounds was determined by spectral analysis. The title compounds were screened for their preliminary antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB, ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Further, the synthesized compounds were screened for antimicrobial activity against standard Gram-negative bacteria Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059) and Gram-positive bacteria Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162). Among all the synthesized compounds, 8a-c, f-h, m exhibited good activity against dormant M. bovis BCG strain. Compounds 8h, j exhibited good activity against all tested bacterial strains. All active compounds were screened for cytotoxicity and found inactive. Their high potency and promising antimycobacterial activity suggest that these compounds could serve as good leads for further optimization and development.</p>10a110a210a3-Triazole10aantibacterial activity10aAntitubercular activity10aThiazole1 aShinde, Vikas1 aMahulikar, Pramod1 aMhaske, Pravin, C.1 aNawale, Laxman1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/synthesis-and-biological-evaluation-new-2-aryl-4-4-aryl-1h-123-triazol-1-ylmethylthiazole01775nas a2200265   4500008004100000022001400041245007300055210006900128260000800197300001400205490000700219520094900226653003101175653001701206653001301223653001401236100002301250700002401273700002601297700002001323700001901343700001901362700002301381856010501404       2019                        eng d  a0960-894X00aThiazolyl-pyrazole derivatives as potential antimycobacterial agents0 aThiazolylpyrazole derivatives as potential antimycobacterial age  cMAY  a1199-12020 v293 a<p>Mycobacterium tuberculosis (Mtb) is an obligate aerobe that is capable of long-term persistence under conditions of low oxygen tension. A series of thiazolyl-pyrazole derivatives (6a-f, 7a-f, 8c, 8e) were screened for antimycobacterial activity against dormant M. tuberculosis H37Ra (D-MTB) and M. bovis BCG (D-BCG). Nine thiazolyl- pyrazole analogs, 6c, 6e, 7a, 7b, 7c, 7e, 7f, 8c and 8e exhibited promissing minimum inhibitory concentration (MIC) values (0.20-28.25 mu g/mL) against D-MTB and D-BCG strains of Mtb. Importantly, six compounds (7a, 7b, 7e, 7f, 8c and 8e) exhibited excellent antimycobacterial activity and low cytotoxicity at the maximum evaluated concentration of &gt; 250 mu g/mL. Finally, the promising antimycobacterial activity and lower cytotoxicity profile suggested that, these compounds could be further subjected for optimization and development as a lead, which could have the potential to treat tuberculosis.</p>10aantimycobacterial activity10aCytotoxicity10aPyrazole10athiazoles1 aTakate, Sushma, J.1 aShinde, Abhijit, D.1 aKarale, Bhausaheb, K.1 aAkolkar, Hemant1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C.  uhttps://library.ncl.res.in/content/thiazolyl-pyrazole-derivatives-potential-antimycobacterial-agents02099nas a2200253   4500008004100000022001400041245010600055210006900161260000800230300001100238490000800249520125600257653001701513653003101530653001301561653002201574100002301596700002001619700001901639700001901658700001901677700002301696856012601719       2021                        eng d  a0045-206800aSynthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents0 aSynthesis of new 2thiazol4ylthiazolidin4one derivatives as poten  cOCT  a1051920 v1153 aTo search for potent antimycobacterial lead compounds, a new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one (5a-t) derivatives have been synthesized by the condensation of 2 substituted phenyl thiazole-4-carbaldehyde with aromatic amine followed by cyclocondensation with thioglycolic acid. The structure of the newly synthesized 2-(thiazol-4-yl)thiazolidin-4-one derivatives were characterized by the spectroscopic analysis. The synthesized compounds were screened for antimycobacterial activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Most of the 2-(thiazol-4-yl)thiazolidin-4-one derivatives showed good to excellent antimycobacterial activity against both the Mtb strains. Nine derivatives 5c, 5g, 5j, 5m, 5n, 5o, 5p, 5s, and 5t showed excellent activity against M. bovis BCG with MIC 4.43 to 24.04 mu M were further evaluated for the cytotoxicity activity against HeLa A549, and HCT-116 cell lines and showed no significant cytotoxic activity at the maximum concentration evaluated. The potential antimycobacterial activities enforced that the thiazolyl-thiazolidin-4-one derivatives could lead to compounds that could treat tuberculosis.10aCytotoxicity10aMycobacterium tuberculosis10aThiazole10aThiazolidin-4-one1 aAbhale, Yogita, K.1 aShinde, Abhijit1 aShelke, Monika1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C.  uhttps://library.ncl.res.in/content/synthesis-new-2-thiazol-4-ylthiazolidin-4-one-derivatives-potential-anti-mycobacterial