… . Structure-activity relationships for 2-phenylbenzimidazole-4-carboxamides, a new class of minimal DNA-intercalating agents which may not act via topoisomerase II

…, GW Rewcastle, BC Baguley

文献索引：Denny, William A.; Rewcastle, Gordon W.; Baguley, Bruce C. Journal of Medicinal Chemistry, 1990 , vol. 33, # 2 p. 814 - 819

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被引用次数: 269

摘要

A series of substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and evaluated for in vitro and in vivo antitumor activity. These compounds represent the logical conclusion to our search for" minimal" DNA-intercalating agents with the lowest possible DNA-binding constants. Such'2-1" tricyclic chromophores, of lower aromaticity than the structurally similar 2-phenylquinolines, have the lowest DNA binding affiiity yet seen in the ...