160522-85-0Relevant articles and documents
Trisbenzimidazoles useful as topoisomerase I inhibitors
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, (2008/06/13)
The present invention provides anti-neoplastic topoisomerase I inhibitors of the formula: STR1 wherein Ar is (C6 -C12)aryl or (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with (C1 -C4)alkyl; X is H, CN, CHO, OH, acetyl, CF3, O(C1 -C4)alkyl, NO2, NH2, halogen or halo-(C1 -C4)alkyl; each Y is individually H, (C1 -C4)alkyl or aralkyl; Y' is H or (C1 -C4)alkyl; n is 0 or 1; and each Z is individually H, (C1 -C4)alkyl, halogen or halo(C1 -C4)alkyl; or a pharmaceutically acceptable salt therein.
Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors
Sun,Gatto,Yu,Liu,Liu,LaVoie
, p. 3638 - 3644 (2007/10/03)
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.
