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

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.

Graphical abstractNew analogues of thieno[2,3-d]pyrimidin-4-yl hydrazone compounds as Cyclin D1/CDK4 inhibitors have been synthesized and evaluated their enzyme inhibitory activity and antiproliferative activity. The potency, selectivity profile, and structure–activity relationship trends of this class of compounds are discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide