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Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation, and structure–activity relationships
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2008-11-27 , DOI: 10.1016/j.bmcl.2008.11.090
Takao Horiuchi , Jun Chiba , Kouichi Uoto , Tsunehiko Soga

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.



中文翻译:

发现新型基于噻吩并[2,3- d ]嘧啶-4-基zone的Cyclin D1-CDK4抑制剂:合成,生物学评估和结构-活性关系

描述了噻吩并[2,3 - d ]嘧啶-4-基的新类似物的合成和评价。2- Pyrdinecarboxaldehyde [6 - 丁基)噻吩并[2,3- d ]嘧啶-4-基]腙衍生物已被鉴定为细胞周期蛋白依赖性激酶4(CDK4)抑制剂。讨论了该系列化合物的效价,选择性分布以及结构-活性关系。

更新日期:2008-11-27
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