From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl) maleimides as glycogen synthase kinase 3β inhibitors that …

…, T Kurome, S Guo, D Holzle, DN Luchini…

Index: Gaisina, Irina N.; Gallier, Franck; Ougolkov, Andrei V.; Kim, Ki H.; Kurome, Toru; Guo, Songpo; Holzle, Denise; Luchini, Doris N.; Blond, Sylvie Y.; Billadeau, Daniel D.; Kozikowski, Alan P. Journal of Medicinal Chemistry, 2009 , vol. 52, # 7 p. 1853 - 1863

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Citation Number: 70

Abstract

Recent studies have demonstrated that glycogen synthase kinase 3β (GSK-3β) is overexpressed in human colon and pancreatic carcinomas, contributing to cancer cell proliferation and survival. Here, we report the design, synthesis, and biological evaluation of benzofuran-3-yl-(indol-3-yl) maleimides, potent GSK-3β inhibitors. Some of these compounds show picomolar inhibitory activity toward GSK-3β and an enhanced selectivity ...