A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment A epoxides and chlorohydrins

…, RM Schultz, SL Andis, JH Kennedy…

Index: Patel, Vinod F.; Andis, Sherri L.; Kennedy, Joseph H.; Ray, James E.; Schultz, Richard M. Journal of Medicinal Chemistry, 1999 , vol. 42, # 14 p. 2588 - 2603

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Citation Number: 35

Abstract

Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria. In an effort to increase the potency and water solubility of the molecule, a structure-activity relationship study (SAR) was initiated around the phenyl ring of fragment A. These Cryptophycin 52 analogues were accessed using a Wittig olefination reaction between various triphenylphosphonium salts and a key intermediate aldehyde ...