Novel 9-oxo-thiazolo [5, 4-f] quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis …

…, A Testard, V Thiéry, O Lozach, M Blairvacq…

文献索引：Loge, Cedric; Testard, Alexandra; Thiery, Valerie; Lozach, Olivier; Blairvacq, Melina; Robert, Jean-Michel; Meijer, Laurent; Besson, Thierry European Journal of Medicinal Chemistry, 2008 , vol. 43, # 7 p. 1469 - 1477

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被引用次数: 36

摘要

Continuous efforts in microwave-assisted synthesis and the structure–activity relationships'(SARs) studies of novel modified 9-oxo-thiazolo [5, 4-f] quinazoline-2- carbonitriles, allowed identification of new amidine and imidate derivatives as potent and dual CDK1/GSK-3 inhibitors. Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with ...