4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described. The structure-based design of potent and selective inhibitors of uPA with 4-aminoarylamidine or 4-aminoarylguanidi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-08, Vol.12 (15), p.2023-2026
Hauptverfasser:	Spencer, Jeffrey R, McGee, Danny, Allen, Darin, Katz, Bradley A, Luong, Christine, Sendzik, Martin, Squires, Neil, Mackman, Richard L
Format:	Artikel
Sprache:	eng
Schlagworte:	Amines - chemistry Amines - pharmacology Antineoplastic agents Benzamidines - chemical synthesis Benzamidines - chemistry Benzamidines - pharmacology Binding Sites Biological and medical sciences Crystallography, X-Ray General aspects Guanidine - analogs & derivatives Guanidine - chemical synthesis Guanidine - pharmacology Medical sciences Models, Molecular Pharmacology. Drug treatments Protein Binding Receptors, Cell Surface - chemistry Receptors, Cell Surface - metabolism Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Structure-Activity Relationship Urokinase-Type Plasminogen Activator - antagonists & inhibitors Urokinase-Type Plasminogen Activator - metabolism
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Zusammenfassung:	The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described. The structure-based design of potent and selective inhibitors of uPA with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00312-8