Synthesis and biological evaluation of benzimidazole fused ellipticine derivatives as anticancer agents

摘要

A series of ten novel benzimidazole fused ellipticine derivatives have been synthesized and these compounds were evaluated for their antiproliferative activity against four human cancer cell lines (Zr-75-1, MCF-7, HeLa, and A-549). It is observed that all the synthesized compounds showed significant antiproliferative activity with GI(50) values ranging from <0.1 to 34.6 mu M, while the positive control, etoposide demonstrated the GI(50) in the range of 0.2-3.08 mu M, respectively. Some of the compounds were distinctly more potent than etoposide, with GI(50) concentrations in the submicromolar level on certain cell lines.