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Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice.

Authors :
Roopashree, Rangaswamy
Mohan, Chakrabhavi Dhananjaya
Swaroop, Toreshettahally Ramesh
Jagadish, Swamy
Raghava, Byregowda
Balaji, Kyathegowdanadoddi Srinivas
Jayarama, Shankar
Basappa, null
Rangappa, Kanchugarakoppal Subbegowda
Source :
Bioorganic & Medicinal Chemistry Letters. Jun2015, Vol. 25 Issue 12, p2589-2593. 5p.
Publication Year :
2015

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-1 H ,3 H -2,5-bibenzo[ d ]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC 50 >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). [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0960894X
Volume :
25
Issue :
12
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
102879693
Full Text :
https://doi.org/10.1016/j.bmcl.2015.04.010