01777nas a2200241   4500008004100000022001400041245010600055210006900161260011000230300001400340490000700354520084200361100002601203700001901229700001901248700001701267700002401284700002601308700002301334700002601357700002501383856012701408       2015                        eng d  a1144-054600aSynthesis, DNA interaction and anticancer activity of 2-anthryl substituted benzimidazole derivatives0 aSynthesis DNA interaction and anticancer activity of 2anthryl su  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcAPR  a4882-48900 v393 a<p>2-Anthryl benzimidazole derivatives (5-7) with hydrogen, carboxyl and benzoyl substituents at the 5th position have been synthesized using a silica supported periodic acid catalyst. The DNA cleavage activity of 5-7 was studied in the presence of light using pBR322 plasmid DNA and was shown to vary with substitution at the 5th position of benzimidazole derivatives. DNA binding studies using ethidium bromide displacement assay demonstrated the non-intercalative binding mode of 5-7. The anticancer activity of these target molecules was tested against MCF-7 and HL-60 cell lines, and they exhibited remarkable activity in the micromolar range. Cellular uptake and morphological changes were confirmed by fluorescence and confocal microscopy. A molecular docking study was carried out to explore the DNA binding mechanism of 5-7.</p>1 aSontakke, Vyankat, A.1 aKate, Anup, N.1 aGhosh, Sougata1 aMore, Piyush1 aGonnade, Rajesh, G.1 aKumbhar, Navanath, M.1 aKumbhar, Anupa, A.1 aChopade, Balu, Ananda1 aShinde, Vaishali, S.  uhttps://library.ncl.res.in/content/synthesis-dna-interaction-and-anticancer-activity-2-anthryl-substituted-benzimidazole-001789nas a2200205   4500008004100000245014600041210006900187260000800256300001400264490000600278520103400284100002401318700001601342700001701358700002201375700001901397700002501416700001801441856012401459       2016                        eng d00aEngineering and in vitro evaluation of acid labile cholesterol tethered MG132 nanoparticle fortargeting ubiquitin-proteasome system in cancer0 aEngineering and in vitro evaluation of acid labile cholesterol t  cOCT  a5099-51060 v13 aIn recent years, proteasome has evolved as one of the important alternative targets in cancer chemotherapy. However, selective targeting of proteasome system in cancer cells still remains a major challenge. To address this, a potent peptide based proteasome inhibitor MG132 was chemically conjugated with biocompatible-biodegradable cholesterol by acid cleavable hydrazone linkage. Spherical nanoparticles (MG132-NPs) were engineered from cholesterol-MG132 conjugate. Increased amount of free MG132 was released from these nanoparticles in acidic environment compared to physiological milieu in a slow and controlled manner. These MG132-NPs were taken up by breast cancer MCF7 cells into lysosomes within 6 h. Proteasome system was inhibited by these MG132-NPs leading to stabilization of beta-catenin, cyclin A and cyclin B in HEK-293T cells. Interestingly, MG132-NPs induced much improved cell death in drug resistant MDA-MB-231 cells with insignificant toxicity in healthy cells (HEK293 and L929) even in higher concentration.1 aGhosh, Chandramouli1 aGupta, Neha1 aMore, Piyush1 aSengupta, Poulomi1 aMallick, Abhik1 aSantra, Manas, Kumar1 aBasu, Sudipta  uhttps://library.ncl.res.in/content/engineering-and-vitro-evaluation-acid-labile-cholesterol-tethered-mg132-nanoparticle01296nas a2200193   4500008004100000245012000041210006900161260000800230300001400238490000700252520059900259100001700858700001900875700001700894700002200911700002100933700001800954856013000972       2017                        eng d00aCisplatin-induced self-assembly of graphene oxide sheets into spherical nanoparticles for damaging sub-cellular DNA0 aCisplatininduced selfassembly of graphene oxide sheets into sphe  cJAN  a1409-14120 v533 aThis report describes the hitherto unobserved cisplatin induced self-assembly of 2D-graphene oxide sheets into 3D-spherical nano-scale particles. These nanoparticles can encompass dual DNA damaging drugs simultaneously. A combination of confocal microscopy, gel electrophoresis and flow cytometry studies clearly demonstrated that these novel nanoparticles can internalize into cancer cells by endocytosis, localize into lysosomes, and damage DNA, leading to apoptosis. Cell viability assays indicated that these nanoparticles were more cytotoxic towards cancer cells compared to healthy cells.1 aNandi, Aditi1 aMallick, Abhik1 aMore, Piyush1 aSengupta, Poulomi1 aBallav, Nirmalya1 aBasu, Sudipta  uhttps://library.ncl.res.in/content/cisplatin-induced-self-assembly-graphene-oxide-sheets-spherical-nanoparticles-damaging-sub