2. Academic Validation
  3. Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors

Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors

  • J Med Chem. 1995 Sep 1;38(18):3638-44. doi: 10.1021/jm00018a024.
Q Sun 1,  B Gatto,  C Yu,  A Liu,  L F Liu,  E J LaVoie
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, Rutgers, State University of New Jersey, Piscataway 08855, USA.
PMID: 7658451 DOI: 10.1021/jm00018a024
Abstract

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.

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