2 ″-Substituted 5-phenylterbenzimidazoles as topoisomerase I poisons

M Rangarajan, JS Kim, S Jin, SP Sim, A Liu…

Index: Rangarajan, Meera; Kim, Jung Sun; Jin, Song; Sim, Sai-Peng; Liu, Angela; Pilch, Daniel S.; Liu, Leroy F.; Lavoie, Edmond J. Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 6 p. 1371 - 1382

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Citation Number: 21

Abstract

5-Phenylterbenzimidazole (1) is active as a topoisomerase I poison (topo I) and is cytotoxic to human tumor cells. No cross-resistance was observed for 1 when it was evaluated against the camptothecin-resistant cell line, CPT-K5. Derivatives of 1 substituted at the 2 ″-position, however, did exhibit cross-resistance to this cell line. The basis for the resistance of this cell line towards CPT is that it possesses a mutant form of topo I. These results suggest that ...