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• W2337390718 startingPage "9238" @default.
• W2337390718 abstract "Urokinase plasminogen activator (uPA) is a biomarker and therapeutic target for several cancer types. Its inhibition is regarded as a promising, noncytotoxic approach in cancer therapy by blocking growth and/or metastasis of solid tumors. Earlier, we reported the modified substrate activity screening (MSAS) approach and applied it for the identification of fragments with affinity for uPA’s S1 pocket. Here, these fragments are transformed into a novel class of uPA inhibitors with an imidazo[1,2-a]pyridine scaffold. The SAR for uPA inhibition around this scaffold is explored, and the best compounds in the series have nanomolar uPA affinity and selectivity with respect to the related trypsin-like serine proteases (thrombin, tPA, FXa, plasmin, plasma kallikrein, trypsin, FVIIa). Finally, the approach followed for translating fragments into small molecules with a decorated scaffold architecture is conceptually straightforward and can be expected to be broadly applicable in fragment-based drug design." @default.
• W2337390718 created "2016-06-24" @default.
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• W2337390718 date "2015-12-01" @default.
• W2337390718 modified "2023-10-16" @default.
• W2337390718 title "Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-<i>a</i>]pyridine Scaffold" @default.
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• W2337390718 doi "https://doi.org/10.1021/acs.jmedchem.5b01171" @default.
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• W2337390718 hasPublicationYear "2015" @default.
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