Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 2, Pages 659-669Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.11.046
Keywords
Bisbenzimidazole; MTT; Hoechst 33342; Antitumor activity; Topoisomerase I; Calf Thymus DNA
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Funding
- Swedish International Development Agency (Sweden)
- Department of Biotechnology (India)
- Department of Science and Technology
- Council of Scientific and Industrial Research (New Delhi, India)
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Inhibitors of topoisomerase I constitute a novel family of antitumor agents. The class of benzimidazole derivatives contains compounds possessing affinity to DNA. For example, fluorescent stains Hoechst 33342 and Hoechst 33258 interact with DNA as ligand and produce nonspecific inhibition of the catalytic activity of many enzymes involved in DNA synthesis, including DNA topoisomerase and DNA helicase. Several 2-aryl-5-substituted-2,5-bisbenzimidazole derivatives were synthesized and ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity against U87, MCF7 and HeLa human tumor cells. All the four compounds showed a potent growth inhibitory effect on all the cell lines, with 10(50) in the mu M range. (C) 2010 Elsevier Masson SAS. All rights reserved.
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