Designed Epothilones: Combinatorial Synthesis, Tubulin Assembly Properties, abd Cytotoxic Action against Taxol‐Resistant Tumor Cells

A library of epothilone A and B analogues , which was constructed by solid‐phase combinatorial synthesis using SMART Microreactors and solution chemistry, was screened in 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 relationship emerged from these studies, which sets the stage for further discoveries and developments in the anticancer field.