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ID: ALA1938230
Journal: Bioorg Med Chem Lett
Title: 6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: discovery of nitrile derivatives with picomolar potency.
Authors: Li B, Cociorva OM, Nomanbhoy T, Li Q, Nakamura K, Nomura M, Okada K, Yumoto K, Liyanage M, Zhang MC, Aban A, Szardenings AK, Kozarich JW, Kohno Y, Shreder KR.
Abstract: We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
CiteXplore: 22202172