Discovery of novel thieno [2, 3-d] pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation, and structure–activity relationships

T Horiuchi, J Chiba, K Uoto, T Soga

Index: Horiuchi, Takao; Chiba, Jun; Uoto, Kouichi; Soga, Tsunehiko Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 305 - 308

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Citation Number: 74

Abstract

The synthesis and evaluation of new analogues of thieno [2, 3-d] pyrimidin-4-yl hydrazones are described. 2-Pyrdinecarboxaldehyde [6-(tert-butyl) thieno [2, 3-d] pyrimidine-4-yl] hydrazone derivatives have been identified as cyclin-dependent kinase 4 (CDK4) inhibitors. The potency, selectivity profile, and structure–activity relationship of this series of compounds are discussed.