Synthesis and Biological Evaluation of Pretubulysin and Derivatives

Abstract

Abstract Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in the subnanomolar range towards various tumor cell lines. Its activity is only slightly less than those of the structurally more complex tubulysins. With a straightforward synthesis to hand, pretubulysin is an ideal lead structure for the development of tubulysin‐based anticancer drugs(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)