Design, Synthesis, and Biological Properties of Highly Potent Epothilone B Analogues

Abstract

A number of rationally designed epoxide and cyclopropane epothilone B (1) analogues with substituted side chains were prepared and their biological activities were evaluated against a series of human cancer cell lines. The cyclopropane analogue 2 with a methylsulfanylthiazole ring stands out as the most potent compound and is sixfold more active than 1. The methylsulfanyl group enhances the potency of these compounds.