Structure-activity studies of benzimidazole-based DNA-cleaving agents. Comparison of benzimidazole, pyrrolobenzimidazole, and tetrahydropyridobenzimidazole …

…, I Islam, MJ Heileman, WG Schulz

Index: Skibo, Edward B.; Islam, Imadul; Heileman, Matthew J.; Schulz, William G. Journal of Medicinal Chemistry, 1994 , vol. 37, # 1 p. 78 - 92

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Citation Number: 74

Abstract

The synthesis and cytotoxic properties of benzimidazole-based DNA-cleaving agents are presented herein. These agents include pyrrolo [l, 2-al benzimidazole (PBI), benzimidazole (BI), and tetrahydropyrido [1, 2-~] benzimidazole (TPBI) analogues. As aresult of theaestudies, it is concluded that the pyrrolo ring is not necessary for cytotoxicity (PBI is only slightly more cytotoxic than BI) but that homologation of the pyrrolo ring by one carbon ...