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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Zhihong Guo

Volume 1, Issue 1, 2004

Page: [69 - 72] Pages: 4

DOI: 10.2174/1570180043485699


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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