Bioorganic and Medicinal Chemistry Letters p. 2589 - 2593 (2015)
Update date:2022-08-11
Topics:
Roopashree, Rangaswamy
Mohan, Chakrabhavi Dhananjaya
Swaroop, Toreshettahally Ramesh
Jagadish, Swamy
Raghava, Byregowda
Balaji, Kyathegowdanadoddi Srinivas
Jayarama, Shankar
Basappa
Rangappa, Kanchugarakoppal Subbegowda
Abstract Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50 μM). Additionally, we evaluated the efficacy of lead compound against Ehrlich ascites tumor (EAT) bearing mice for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature and production of Vascular Endothelial Growth Factor (VEGF).
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