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…

Index: 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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Citation Number: 16

Abstract

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).