Sun Q, Gatto B, Yu C, Liu A, Liu L F, LaVoie E J
Department of Pharmaceutical Chemistry, Rutgers, State University of New Jersey, Piscataway 08855, USA.
J Med Chem. 1995 Sep 1;38(18):3638-44. doi: 10.1021/jm00018a024.
The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.
描述了一系列叔苯并咪唑的合成及药理活性。在体外评估了这些衍生物在拓扑异构酶I存在下诱导DNA裂解的能力。还测定了这些类似物在RPMI 8402细胞和喜树碱耐药的CPT-K5细胞中的细胞毒性。此外，还确定了这些化合物作为MDR1底物的可能性。几种叔苯并咪唑对过表达MDR1或对喜树碱耐药的人类肿瘤细胞变体表现出相似的细胞毒性。
