Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Cytotoxicity of Enediyne Prodrugs with 3-Hydroxy-4- (arylmethylidene)cyclodeca-1,5-diyne Scaffolds

Author(s): Wei-Min Dai, Yukihiro Tachi, Sei-ichi Nishimoto, Xiaofen Zhong, Zhihong Guo.

Abstract:

A series of enediyne prodrugs with (E)- or (Z)-3-hydroxy-4-(arylmethylidene)cyclodeca-1,5- diyne scaffolds have been synthesized via an intramolecular Nozaki-Hiyama-Kishi reaction as the key step. Cytotoxicity in micro molar range against P388 cancer cell line was observed for selected compounds and a structure-activity relationship is discussed.

Keywords: enediyne, prodrug, nozaki-hiyama-kishi reaction, allylic, rearrangement, anticancer

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Article Details

VOLUME: 1
ISSUE: 1
Year: 2004
Page: [69 - 72]
Pages: 4
DOI: 10.2174/1570180043485699