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Bioorg Med Chem Lett
; 19(19): 5712-5, 2009 Oct 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19703768
RESUMEN
In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, was replaced with a primary amine. Further modifications led to the identification of potent, selective, and orally bioavailable uPA inhibitors.