Improved Total Synthesis and Structure-Activity Relationship of Arenastatin A, a Potent Cytotoxic Spongean Depsipeptide.

Abstract

An efficient asymmetric synthesis of a cyclic depsipeptide arenastatis A (1) is described. 1, isolated from the marine sponge Dysidea arenaria, exhibited extremely potent cytotoxicity with IC50 of pg/ml for KB cells, and in this context the structure-activity relationship among several stereoisomers of 1 and allied compounds has also been examined.