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  • Discovery and initial SAR o...
    Chen, Ping; Norris, Derek; Iwanowicz, Edwin J.; Spergel, Steven H.; Lin, James; Gu, Henry H.; Shen, Zhongqi; Wityak, John; Lin, Tai-An; Pang, Suhong; De Fex, Henry F.; Pitt, Sidney; Shen, Ding Ren; Doweyko, Arthur M.; Bassolino, Donna A.; Roberge, Jacques Y.; Poss, Michael A.; Chen, Bang-Chi; Schieven, Gary L.; Barrish, Joel C.

    Bioorganic & medicinal chemistry letters, 2002, Volume: 12, Issue: 10
    Journal Article

    We have identified a novel series of 1,5-imidazoquinoxalines as inhibitors of Lck with excellent potency (IC 50s<5 nM) as well as good cellular activity against T-cell proliferation (IC 50s<1 μM). Structure–activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2,6-disubstituted aniline group. We have identified a novel series of 1,5-imidazoquinoxalines as inhibitors of Lck with excellent potency (IC 50s<5 nM) as well as good cellular activity against T-cell proliferation (IC 50s<1 μM). Structure–activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2,6-disubstituted aniline group.