Abstract

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.

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