Synthesis and evaluation of a series of benzothiophene acrylonitrile analogs as anticancer agents.

ABSTRACT: A new library of small molecules with structural features resembling combretastatin analogs was synthesized and evaluated for anticancer activity against a panel of 60 human cancer cell lines. Three novel acrylonitrile analogs (5, 6 and 13) caused a significant reduction in cell growth in almost all the cell lines examined, with GI₅₀ values generally in the range 10-100 nM. Based on the structural characteristics of similar drugs, we hypothesized that the cytotoxic activity was likely due to interaction with tubulin. Furthermore, these compounds appeared to overcome cell-associated P-glycoprotein (P-gp)-mediated resistance, since they were equipotent in inhibiting OVCAR8 and NCI/ADR-Res cell growth. Given that antitubulin drugs are among the most effective agents f

SUBMITTER: Penthala NR 

PROVIDER: S-EPMC3743125 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature