A series of novel compounds, substituted 2,4-diaminopyrimidine-5-amides, were designed and synthesized based on X-Ray co-structure of pyrazolopyrimidine on Mer kinase. The Structure Aactivity Relationships (SAR) on this new scaffold has been studied; lead compounds with nanomolar to subnanomolar IC50 activity against Mer kinase in both enzymatic and cell-based assays were identified for further development. Structure modification for further improvement of the DMPK of the lead compounds is currently ongoing.

Design and synthesis substituted 2,4-diaminopyrimidine-5-amides as novel Mer inhibitors for the treatment of acute lymphoblastic leukemia (ALL)

244th National Meeting (2012)

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