2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

The development of potent and selective urokinase-type plasminogen activator (uPA) inhibitors based on the lead molecule 2-(2-hydroxy-3-ethoxyphenyl)-1H-benzimidazole-5-carboxamidine (3a) is described.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2002-08, Vol.12 (15), p.2019-2022
Hauptverfasser: MACKMAN, Richard L, HUI, Hon C, SPRENGELER, Paul A, TARIO, James, VERNER, Erik, JING WANG, BREITENBUCHER, J. Guy, KATZ, Bradley A, LUONG, Christine, MARTELLI, Arnold, MCGEE, Danny, RADIKA, Kesavan, SENDZIK, Martin, SPENCER, Jeffrey R
Format: Artikel
Sprache:eng
Schlagworte:
Amidines - chemistry
Amidines - pharmacology
Antineoplastic agents
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Binding Sites
Biological and medical sciences
Crystallography, X-Ray
Drug Design
General aspects
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Protein Binding
Receptors, Cell Surface - chemistry
Receptors, Cell Surface - metabolism
Serine Proteinase Inhibitors - chemistry
Serine Proteinase Inhibitors - pharmacology
Stereoisomerism
Structure-Activity Relationship
Urokinase-Type Plasminogen Activator - antagonists & inhibitors
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Zusammenfassung:The development of potent and selective urokinase-type plasminogen activator (uPA) inhibitors based on the lead molecule 2-(2-hydroxy-3-ethoxyphenyl)-1H-benzimidazole-5-carboxamidine (3a) is described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00311-6