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Bioorg Med Chem Lett
; 20(23): 6998-7003, 2010 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20965724
RESUMO
A series of novel compound libraries inhibiting interleukin-2 inducible T cell kinase (ITK) were designed, synthesized and evaluated. In the first design cycle two library scaffolds were identified showing low micromolar inhibition of ITK. Further iterative design cycles including crystal structure information of ITK and structurally related kinases led to the identification of indolylindazole and indolylpyrazolopyridine compounds with low nanomolar ITK inhibition.