| Literature DB >> 20207053 |
Ravi Kumar1, Leena Gupta, Pooja Pal, Shahnawaz Khan, Neetu Singh, Sanjay Babu Katiyar, Sanjeev Meena, Jayanta Sarkar, Sudhir Sinha, Jitendra Kumar Kanaujiya, Savita Lochab, Arun Kumar Trivedi, Prem M S Chauhan.
Abstract
A series of tetrahydro-beta-carbolines and 1,3,5-triazine hybrids have been synthesized and evaluated for their cytotoxicity against a panel of eight human cancer cell lines and normal human fibroblasts (NIH3T3). It led us to discovery of racemic compounds 69, 71 and 75, which are selectively cytotoxic towards KB (oral cancer) cell line with IC50 values of 105.8, 664.7 and 122.2 nM, respectively; while their enantiopure forms are less active and not selective. Enantiopure compound 42 showed 2.5 times more selectivity towards MCF7 cells over normal fibroblast NIH3T3 cells with an IC50 value of 740 nM, also arrests cell cycle in G1 phase and induces apoptosis in MCF7 and MDA MB231 cell lines. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.Entities:
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Year: 2010 PMID： 20207053 DOI： 10.1016/j.ejmech.2010.02.001
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514