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Updated: Jun 13, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Versatile synthesis of new cytotoxic agents structurally related to hemiasterlins
Daniele Simoni1, Ray M Lee, David E Durrant
1Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17/19, 44100, Ferrara, Italy.
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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