Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck
作者:Ping Chen、Derek Norris、Edwin J. Iwanowicz、Steven H. Spergel、James Lin、Henry H. Gu、Zhongqi Shen、John Wityak、Tai-An Lin、Suhong Pang、Henry F. De Fex、Sidney Pitt、Ding Ren Shen、Arthur M. Doweyko、Donna A. Bassolino、Jacques Y. Roberge、Michael A. Poss、Bang-Chi Chen、Gary L. Schieven、Joel C. Barrish
DOI:10.1016/s0960-894x(02)00191-9
日期:2002.5
We have identified a novel series of 1,5-imidizoquinoxalines as inhibitors of Lck with excellent potency (IC(50)s less than or equal to 5 nM) as well as good cellular activity against T-cell proliferation (IC(50)s < 1 muM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2.6-disubstituted aniline group. (C) 2002 Published by Elsevier Science Ltd.