Designed epothilones: Combinatorial synthesis, tubulin assembly properties, and cytotoxic action against taxol-resistant tumor cells
National Institutes of Health (U.S.)
Research Support as Topic
A library of epothilone A and B analogues, which was constructed by solid-phase combinatorial synthesis using SMART Microreactors and solution chemistry, was screened !n two different tubulin binding assays. Selected compounds were subjected to cytotoxicity studies against a number of cell lines, including Taxol-resistant cells. Important structure-activity relationships emerged from these studies; which sets the stage for further discoveries and developments in the anticancer field.