用于新型激酶抑制剂开发的通用模板：新型CDK抑制剂的发现
Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.
作者信息
Dwyer Michael P, Paruch Kamil, Alvarez Carmen, Doll Ronald J, Keertikar Kerry, Duca Jose, Fischmann Thierry O, Hruza Alan, Madison Vincent, Lees Emma, Parry David, Seghezzi Wolfgang, Sgambellone Nicole, Shanahan Frances, Wiswell Derek, Guzi Timothy J
机构信息
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. doi: 10.1016/j.bmcl.2007.09.018. Epub 2007 Sep 8.
A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.
制备了一系列四种双环核心，并将其作为细胞周期蛋白依赖性激酶-2（CDK2）抑制剂进行评估。通过体外和基于细胞的分析，吡唑并[1,5-a]嘧啶核心（以9代表）成为在新型CDK2抑制剂鉴定中进一步优化的优异核心。
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