01500nas a2200193   4500008004100000022001400041245012600055210006900181260011000250300001800360490000600378520067500384100002401059700002501083700002101108700002501129700002401154856012801178       2015                        eng d  a2046-206900aAmmonium persulfate activated DMSO as a one-carbon synthon for the synthesis of methylenebisamides and other applications0 aAmmonium persulfate activated DMSO as a onecarbon synthon for th  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcNOV  a101641-1016460 v53 a<p>Activation of DMSO to work as an economical and environmentally benign one-carbon synthon has been achieved by using a bench-top reagent ammonium persulfate for general and efficient access to symmetrical methylenebisamides from primary amides. This methodology was used to achieve a three-component Mannich reaction using acetophenone, saccharin and DMSO to furnish a beta-amino ketone. It also provided a metal-free synthesis of thiadiazole and bis(phenyl)methane. Effectively, this method uses DMSO as a safer surrogate to formaldehyde. A mechanism for methylenebisamide formation involving radical intermediates has been proposed based on mechanistic studies.</p>1 aMahajan, Pankaj, S.1 aTanpure, Subhash, D.1 aMore, Namita, A.1 aGajbhiye, Jayant, M.1 aMhaske, Santosh, B.  uhttps://library.ncl.res.in/content/ammonium-persulfate-activated-dmso-one-carbon-synthon-synthesis-methylenebisamides-and-001655nas a2200301   4500008004100000022001400041245008300055210006900138260008300207300001400290490000700304520066300311653002100974653001000995653001401005653003101019653001501050653001701065100002101082700002101103700002101124700001601145700002201161700001901183700001501202700002201217856011401239       2015                        eng d  a1054-252300aDiscovery of rimonabant and its potential analogues as anti-TB drug candidates0 aDiscovery of rimonabant and its potential analogues as antiTB dr  a233 SPRING STREET, 6TH FLOOR, NEW YORK, NY 10013 USAbSPRINGER BIRKHAUSERcJUL  a2960-29710 v243 a<p>Rimonabant and its analogues have been synthesized in moderate to good yields using a simple synthetic route. All the newly synthesized compounds were subjected to in vitro screening against M. tuberculosis and M. smegmatis. The most potent analogue JMG-14 exhibits MIC value of 3.13 compared to 3.25 and 50 A mu g/ml for ethambutol and pyrazinamide, respectively. The molecular docking reveals that pyrazole ring, number and position of halogen atoms play a crucial role in deciding interactions with MTCYP-121. These findings open up a new avenue in the search of potent anti-TB drugs with rimonabant and its novel analogue JMG-14 as lead molecules.</p>10aDiaryl pyrazoles10aH37Rv10aMTCYP-12110aMycobacterium tuberculosis10aRimonabant10atuberculosis1 aGajbhiye, J., M.1 aMore, Namita, A.1 aPatil, Manoj, D.1 aUmmanni, R.1 aKotapalli, S., S.1 aYogeeswari, P.1 aSriram, D.1 aMasand, Vijay, H.  uhttps://library.ncl.res.in/content/discovery-rimonabant-and-its-potential-analogues-anti-tb-drug-candidates-002874nas a2200313   4500008004100000022001400041245012400055210006900179260000900248300001100257490000900268520183000277653002402107653001402131653001802145653002702163653001502190653001602205100002102221700002202242700002302264700002002287700002202307700002502329700002602354700002302380700002502403856013202428       2022                        eng d  a0022-286000aNovel 3-fluoro-4-morpholinoaniline derivatives: synthesis and assessment of anti-cancer activity in breast cancer cells0 aNovel 3fluoro4morpholinoaniline derivatives synthesis and assess  cAPR   a1321270 v12533 aHeterocyclic morpholine compounds are well-known for their anti-cancer activity. In this study, novel morpholine and its sulfonamide derivatives were designed and synthesized as potential anti-tumor agents. The new compounds were obtained from amine derivatives via nucleophilic addition reactions, providing the desired products in 70 to 90% yield. The docking analysis was performed for all thirty-one compounds. Out of them, we represent the docking poses for compounds NAM-5 and NAM-7 as representatives. After docking analysis, compounds NAM-5 and NAM- 7 were tested for in vitro antitumor activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and healthy mouse embryonic fibroblast cell line (3T3L-1). Amongst these, sulfonamide group-containing compound NAM-5 showed significant anti-proliferative activity with IC50 of 1.811 mu M and 2.143 mu M for MCF-7 and MDA-MB-231 cells, respectively. On the other hand, NAM-7 showed good anti-proliferative activity against MCF-7 (IC50 1.883 mu M) but slightly lower activity against MDA-MB-231 cells (IC50 4.688 mu M). The activity of both the compound was also tested on 3T3L-1 Cell line which showed activity similar to clinically approved anti-cancer drug doxorubicin (DOX). The cell death analysis by flow-cytometry confirmed apoptosis mediated cell death in 3T3L-1, MCF-7 and MDA-MB-231 cells when treated with the NAM-5 and NAM-7, respectively. The results demonstrated that the synthesized sulfonamide derivatives have significant potential as anti-cancer agents and have a substantial importance in cancer therapeutics with favourable safety profile. Structural analysis of docked poses of sulfonamide derivatives attempts to shed light on the structural basis of sulfonamide derivatives based anti-cancer effect. (C) 2021 Elsevier B.V. All rights reserved.10aAnticancer activity10aApoptosis10aBreast cancer10aHeterocyclic compounds10aMorpholine10aSulfonamide1 aMore, Namita, A.1 aJadhao, Nitin, L.1 aMeshram, Rohan, J.1 aTambe, Prajakta1 aSalve, Rajesh, A.1 aSabane, Jagjivan, K.1 aSawant, Sanskruti, N.1 aGajbhiye, Virendra1 aGajbhiye, Jayant, M.  uhttps://library.ncl.res.in/content/novel-3-fluoro-4-morpholinoaniline-derivatives-synthesis-and-assessment-anti-cancer-activity