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Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck

2002; Elsevier BV; Volume: 12; Issue: 10 Linguagem: Inglês

10.1016/s0960-894x(02)00191-9

1464-3405

Ping Chen, Derek Norris, Edwin J. Iwanowicz, Steven H. Spergel, James C. Lin, Henry H. Gu, Zhongqi Shen, John Wityak, Tai-An Lin, Suhong Pang, H. 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,

Bioactive Compounds and Antitumor Agents

We have identified a novel series of 1,5-imidazoquinoxalines as inhibitors of Lck with excellent potency (IC50s<5 nM) as well as good cellular activity against T-cell proliferation (IC50s<1 microM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2,6-disubstituted aniline group.