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Bioorg Med Chem Lett. 2009 Oct 1;19(19):5712-5. doi: 10.1016/j.bmcl.2009.08.008. Epub 2009 Aug 7.

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

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  • 1Department of Medicinal Chemistry, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States.


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.

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