A Pd(0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors
Lucie Vandromme1, Michel Legraverend, Sergio Kreimerman
1UMR 176, Institut Curie, Bât. 110-112, Centre Universitaire, 91405 Orsay, France.
Bioorganic & Medicinal Chemistry
|October 27, 2006
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 IC(50) of 0.9muM for the most active compound (18c).
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