作者:David J Carini、Robert F Kaltenbach、Jie Liu、Pamela A Benfield、John Boylan、Michael Boisclair、Leonardo Brizuela、Catherine R Burton、Sarah Cox、Robert Grafstrom、Barbara A Harrison、Kimberly Harrison、Emeka Akamike、Jay A Markwalder、Yuki Nakano、Steven P Seitz、Diane M Sharp、George L Trainor、Thais M Sielecki
DOI:10.1016/s0960-894x(01)00416-4
日期:2001.8
A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition
已经确定了一种新型的激酶抑制剂,其包含苯并咔唑核。该系列的成员对抑制细胞周期蛋白依赖性激酶家族的酶具有选择性。尽管cdks高度同源,但该系列的代表显示了cdk内选择性,尤其是对于cdk4。SAR研究阐明了抑制分子的重要特征。