Synthesis of macrosphelides with a thiazole side chain: new antitumor candidates having apoptosis-inducing property |
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Authors: | Matsuya Yuji Kawaguchi Takanori Ishihara Kentaro Ahmed Kanwal Zhao Qing-Li Kondo Takashi Nemoto Hideo |
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Affiliation: | Faculty of Pharmaceutical Sciences, and Department of Radiological Sciences, Faculty of Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. |
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Abstract: | Hybrid compounds of macrosphelides and epothilones, both of which are natural macrolides having a 16-membered skeleton, were designed and synthesized using a ring-closing metathesis (RCM) strategy. Some of these hybrids were found to exhibit notable apoptosis-inducing activity against human lymphoma cells with higher potency than parent natural macrosphelides, and to be a promising lead compound for development of a new antitumor agent. |
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