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

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

Volume: 1 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Dai Wei-Min, Tachi Yukihiro, Nishimoto Sei-ichi, Zhong Xiaofen and Guo Zhihong, Synthesis and Cytotoxicity of Enediyne Prodrugs with 3-Hydroxy-4- (arylmethylidene)cyclodeca-1,5-diyne Scaffolds, Letters in Drug Design & Discovery 2004; 1 (1) . https://dx.doi.org/10.2174/1570180043485699