Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice.
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).
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Rangaswamy
R
Roopashree
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Chakrabhavi Dhananjaya
CD
Mohan
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Toreshettahally Ramesh
TR
Swaroop
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Swamy
S
Jagadish
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Byregowda
B
Raghava
Department of Biotechnology, Teresian College, Mysore 570 011, India.
Kyathegowdanadoddi Srinivas
KS
Balaji
Department of Biotechnology, Teresian College, Mysore 570 011, India.
Shankar
S
Jayarama
Laboratory of Chemical Biology, Department of Chemistry, Bangalore University, Bangalore 560 001, India.
Basappa
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India. Electronic address: rangappaks@gmail.com.
Kanchugarakoppal Subbegowda
KS
Rangappa
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001201:Ascites; D006690:Bisbenzimidazole / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D001835:Body Weight / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D015536:Down-Regulation / Q000187:drug effects; D045325:HCT116 Cells; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism; D014709:Vero Cells
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D042461:Vascular Endothelial Growth Factor A; D006690:Bisbenzimidazole
Angiogenesis; Antiproliferative; Bisbenzimidazole; Ehrlich ascites tumor; Micro vessel density; Vascular Endothelial Growth Factor