Total Synthesis of the Potent Antitumor Macrolides Pladienolide B and D

摘要

In 2004 Sakai et al.reported the identification of seven 12-membered macrolides (pladienolides A-G),from Strepto-myces platensis Mer-11107 by way of a cell-based assay that evaluated the suppression of hypoxia-induced gene expression controlled by the human VEGF promoter.The most potent pladienolides (B (2) and D (3)) have IC50 values in the low nanomolar range (Scheme 1).