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, M Nagata, M Kitagawa, K Akahane…

Index: Horiuchi, Takao; Nagata, Motoko; Kitagawa, Mayumi; Akahane, Kouichi; Uoto, Kouichi Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 23 p. 7850 - 7860

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Citation Number: 56

Abstract

The design, synthesis and evaluation of novel thieno [2, 3-d] pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl groups, 4- [(methylamino) methyl] benzaldehyde (22) and 5-isoindolinecarbaldehyde (24)(6-tert- butylthieno [2, 3-d] pyrimidin-4-yl) hydrazone derivatives have been identified. In this ...