嘧啶
化学
细胞周期蛋白依赖激酶
调节器
立体化学
分子模型
激酶
组合化学
生物化学
计算生物学
细胞周期
细胞
生物
基因
作者
Marc Labroli,Kamil Paruch,Michael P. Dwyer,Carmen Álvarez,Kartik Keertikar,Cory Poker,Randall R. Rossman,José S. Duca,Thierry Fischmann,Vincent Madison,David Parry,Nicole R. Davis,Wolfgang Seghezzi,Derek Wiswell,Timothy J. Guzi
标识
DOI:10.1016/j.bmcl.2010.10.114
摘要
Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo[1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors.
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