Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)

…, C Huwe, D Light, G Phillips, R Pulk, D Sukovich…

文献索引：West, Christopher W.; Adler, Marc; Arnaiz, Danny; Chen, Deborah; Chu, Kieu; Gualtieri, Giovanna; Ho, Elena; Huwe, Christoph; Light, David; Phillips, Gary; Pulk, Rebecca; Sukovich, Drew; Whitlow, Marc; Yuan, Shendong; Bryant, Judi Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 19 p. 5712 - 5715

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被引用次数: 6

摘要

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.