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

Wei-Min Dai; Yukihiro Tachi; Sei-ichi Nishimoto; Xiaofen Zhong; Zhihong Guo

doi:10.2174/1570180043485699

ISSN: 1570-1808
E-ISSN: 1875-628X

Synthesis and Cytotoxicity of Enediyne Prodrugs with 3-Hydroxy-4- (arylmethylidene)cyclodeca-1,5-diyne Scaffolds
Authors: Wei-Min Dai¹, Yukihiro Tachi², Sei-ichi Nishimoto³, Xiaofen Zhong⁴ and Zhihong Guo⁵
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¹ Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. ² Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. ³ Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. ⁴ Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. ⁵ Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China.
Source: Letters in Drug Design & Discovery, Volume 1, Issue 1, Jan 2004, p. 69 - 72
DOI: https://doi.org/10.2174/1570180043485699
- Available online: 01 Jan 2004

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.

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2004-01-01

2025-09-30

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Article Type: Review Article

Keyword(s): allylic; anticancer; enediyne; nozaki-hiyama-kishi reaction; prodrug; rearrangement

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

Abstract

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