Identification of orally bioavailable,non-amidine inhibitors of Urokinase Plasminogen Activator (uPA) |
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| Authors: | Christopher W West Marc Adler Danny Arnaiz Deborah Chen Kieu Chu Giovanna Gualtieri Elena Ho Christoph Huwe David Light Gary Phillips Rebecca Pulk Drew Sukovich Marc Whitlow Shendong Yuan Judi Bryant |
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| Institution: | 1. Department of Medicinal Chemistry, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States;2. Department of Biophysics, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States;3. Department of Molecular Pharmacology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States;4. Department of Animal Pharmacology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States;5. Department of Antibody Technology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, United States |
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| Abstract: | 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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