Structure-activity relationships of benzimidazoles and related heterocycles as topoisomerase I poisons

…, Q Sun, B Gatto, C Yu, A Liu, LF Liu, EJ LaVoie

文献索引：Kim, Jung Sun; Sun, Qun; Gatto, Barbara; Yu, Chiang; Liu, Angela; Liu, Leroy F.; LaVoie, Edmond J. Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 4 p. 621 - 630

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被引用次数: 136

摘要

A series of substituted 2-(4-methoxyphenyl)-1H-benzimidazoles were synthesized and evaluated as inhibitors of topoisomerase I. The presence of a 5-formyl-, 5-(aminocarbonyl)-, or 5-nitro group (ie, substituents capable of acting as hydrogen bond acceptors) correlated with the potential of select derivatives to inhibit topoisomerase I. In contrast to bi-and terbenzimidazoles, the substituted benzimidazoles that were active as topoisomerase I ...