Thiazolo [5, 4-f] quinazolin-9-ones, inhibitors of glycogen synthase kinase-3

…, B Léger, JM Robert, O Lozach, M Blairvacq…

文献索引：Testard, Alexandra; Loge, Cedric; Leger, Benoit; Robert, Jean-Michel; Lozach, Olivier; Blairvacq, Melina; Meijer, Laurent; Thiery, Valerie; Besson, Thierry Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 13 p. 3419 - 3423

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被引用次数: 52

摘要

In an effort to identify new protein kinase inhibitors with increased potency and selectivity, we have developed the microwave-assisted synthesis of thiazolo [5, 4-f] quinazolin-9-ones. The effects of eighteen derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3 were investigated. Several turned out to inhibit GSK-3 in the micromolar range. Molecular modeling studies suggest that the most selective GSK-3 inhibitors 7a–d bind into the ATP- ...