Terbenzimidazoles: influence of 2''-, 4-, and 5-substituents on cytotoxicity and relative potency as topoisomerase I poisons

…, C Yu, A Liu, LF Liu, EJ LaVoie

Index: Kim, Jung Sun; Yu, Chiang; Liu, Angela; Liu, Leroy F.; LaVoie, Edmond J. Journal of Medicinal Chemistry, 1997 , vol. 40, # 18 p. 2818 - 2824

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Citation Number: 53

Abstract

Terbenzimidazoles poison the nuclear enzyme topoisomerase I and possess significant cytotoxic activity against several human tumor cell lines. The relative pharmacological activity of 4, 5-and 5, 6-benzoterbenzimidazoles was compared to that of 5- phenylterbenzimidazole (3). 5, 6-Benzoterbenzimidazole is inactive as a topoisomerase I poison and did not exhibit significant cytotoxic activity. In contrast, 4, 5- ...