A Pd (0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors

L Vandromme, M Legraverend, S Kreimerman…

文献索引：Vandromme, Lucie; Legraverend, Michel; Kreimerman, Sergio; Lozach, Olivier; Meijer, Laurent; Grierson, David S. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 1 p. 130 - 141

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被引用次数: 16

摘要

Two new series of 2-amido-and 2-aminocarbonylpurines have been synthesized using a Pd catalyst cross-coupling reaction either with amides or amines in the presence of CO. Moderate in vitro inhibitory activity against CDK1 and CDK5 was observed with IC50 of 0.9 μM for the most active compound (18c).