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Bioorganic & medicinal chemistry letters

New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.


PMID 20483608

Abstract

A novel series of pyrazolo[1,5a]pyrimidines was optimized to target lymphocyte-specific kinase (Lck). An efficient synthetic route was developed and SAR studies toward activity and selectivity are described, leading to Lck inhibitors with enzymatic, cellular and in vivo potency.