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Versatile synthesis of new cytotoxic agents structurally related to hemiasterlins. | LitMetric

Versatile synthesis of new cytotoxic agents structurally related to hemiasterlins.

Bioorg Med Chem Lett

Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17/19, 44100, Ferrara, Italy.

Published: June 2010

AI Article Synopsis

Article Abstract

A representative series of structural analogues of the antimitotic tripeptides hemiasterlins have been synthesized. The key-step of this synthetic strategy consists of an Ag(2)O-promoted nucleophilic substitution on a common precursor, a chiral non-racemic 2-bromoacyl derivative. Simple variation of nucleophile substituents allows a rapid and stereocontrolled development of new series of derivatives. Some reported compounds showed potent biological activity as growth inhibitors of cancer cell lines and tubulin polymerization inhibitors.

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Source
http://dx.doi.org/10.1016/j.bmcl.2010.03.098DOI Listing

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