Abstract
The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.
MeSH terms
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Amidines / chemical synthesis*
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Amidines / pharmacology*
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Drug Design
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Drug Evaluation, Preclinical
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Plasminogen Activators / antagonists & inhibitors*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis
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Thiazoles / pharmacology*
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology
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Urokinase-Type Plasminogen Activator / antagonists & inhibitors*
Substances
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Amidines
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Thiazoles
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Thiophenes
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2-aminothiazole
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Plasminogen Activators
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Urokinase-Type Plasminogen Activator