Synthesis of macrosphelides with a thiazole side chain: new antitumor candidates having apoptosis-inducing property.
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.
Matsuya
Yuji
Y
Faculty of Pharmaceutical Sciences, and Department of Radiological Sciences, Faculty of Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.
Kawaguchi
Takanori
T
Ishihara
Kentaro
K
Ahmed
Kanwal
K
Zhao
Qing-Li
QL
Kondo
Takashi
T
Nemoto
Hideo
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D003500:Cyclization; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry*
D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D013844:Thiazoles