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Design, Synthesis, and Biological Evaluation of Artificial Macrosphelides in the Search for New Apoptosis-Inducing Agents

✍ Scribed by Yuji Matsuya; Yuta Kobayashi; Takanori Kawaguchi; Ayana Hori; Yuka Watanabe; Kentaro Ishihara; Kanwal Ahmed; Zheng-Li Wei; Da-Yong Yu; Qing-Li Zhao; Takashi Kondo; Hideo Nemoto

Publisher
John Wiley and Sons
Year
2009
Tongue
English
Weight
604 KB
Volume
15
Category
Article
ISSN
0947-6539

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✦ Synopsis

Abstract

A drug of two halves: New artificial compounds composed of a macrosphelide core skeleton and an epothilone side chain were designed and synthesized. These compounds were more potent inducers of apoptosis than the parent natural‐type macrosphelides.magnified image

Various artificial macrosphelides were designed and synthesized, including ring‐enlarged analogues and epothilone‐hybrid compounds. Syntheses were accomplished in an efficient manner by using a ring‐closing metathesis (RCM) strategy in a key macrocyclization step. Biological evaluation of these new macrosphelide‐based derivatives revealed that several epothilone hybrids, in which a thiazole‐containing side chain was incorporated, exhibited potent apoptosis‐inducing activity toward human lymphoma cells. These activities were considerably enhanced relative to those of natural macrosphelide compounds. Structure–activity relationship studies revealed that the “ene‐dicarbonyl” substructure is apparently essential for bioactivity.

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