Synthesis, characterization, and in vivo biological evaluation of novel benzimidazoles as potential anticancer agents

Roopashree, R. and Mohan, C. D. and Swaroop, T. R. and Jagadish, S. and Rangappa, K. S. (2014) Synthesis, characterization, and in vivo biological evaluation of novel benzimidazoles as potential anticancer agents. Asian Journal of Pharmaceutical and Clinical Research, 7 (5). pp. 309-313. ISSN 0974-2441

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Abstract

Objective: Cancer is one of the major causes of death worldwide irrespective of the sex. The aim of the study was to design, synthesize, and identification of novel anti-proliferative agents that can potently target cancer. Methods: We are reporting the synthesis of the new series of N-substituted 2-(2-butyl-4-chloro-1H-imidazole-5-yl)-1H-benzodimidazole derivatives and evaluated for their anti-tumor activity against HeLa cell lines. We identified the lead compound in the series and tested its anti-proliferative and anti-angiogenic properties against Ehrlich ascites tumor (EAT) bearing mice. Results: We identified 2-(2-butyl-4-chloro-1-heptyl-1H-imidazol-5yl)-1H-benzodimidazole as a lead compound with the inhibitory concentration 50\% of 25.3 μM. The lead compound significantly decreases the angiogenesis in peritoneum of EAT bearing mice. Conclusion: Our results clearly demonstrate that benzimidazoles suppress the cell proliferation, peritoneal angiogenesis, and ascites volume. © 2014, Asian Journal of Pharmaceutical and Clinical Research. All rights reserved.

Item Type:	Article
Uncontrolled Keywords:	animal experiment, animal model, antiangiogenic activity, antineoplastic activity, antineoplastic agent, antiproliferative activity, Article, cell viability, controlled study, drug cytotoxicity, drug synthesis, Ehrlich ascites tumor, human, human cell, IC50, in vitro study, in vivo study, mouse, nonhuman, structure activity relation, unclassified drug, drug screening, animal tissue, male, drug mechanism, female, drug design, drug efficacy, minimum inhibitory concentration, sorafenib, cytotoxicity assay, HeLa cell line, cell count, ascites fluid, peritoneum tumor, 2 (1, 2 (1 benzyl 2 butyl 4 chloro 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 (3, 2 (2 butyl 4 chloro 1 (3 methylbenzyl) 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 (4 chlorobenzyl) 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 (4 fluorobenzyl) 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 ethyl 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 heptyl 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1 methyl 1h imidazol 5yl) 1h benzodimidazole, 2 (2 butyl 4 chloro 1h imidazol 5 yl) 1h benzodimidazole derivative, 2 dibutyl 4 chloro 1h imidazol 5yl) 1h benzodimidazole, 4 dichlorobenzyl) 1h imidazol 5yl) 1h benzodimidazole, benzimidazole derivative
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	21 Aug 2019 07:19
Last Modified:	21 Aug 2019 07:19
URI:	http://eprints.uni-mysore.ac.in/id/eprint/4379

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