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

Richard L Mackman; Hon C Hui; J Guy Breitenbucher; Bradley A Katz; Christine Luong; Arnold Martelli; Danny McGee; Kesavan Radika; Martin Sendzik; Jeffrey R Spencer; Paul A Sprengeler; James Tario; Erik Verner; Jing Wang

doi:10.1016/s0960-894x(02)00311-6

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

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22. doi: 10.1016/s0960-894x(02)00311-6.

Authors

Richard L Mackman¹, Hon C Hui, J Guy Breitenbucher, Bradley A Katz, Christine Luong, Arnold Martelli, Danny McGee, Kesavan Radika, Martin Sendzik, Jeffrey R Spencer, Paul A Sprengeler, James Tario, Erik Verner, Jing Wang

Affiliation

¹ Celera, 180 Kimball Way, South San Francisco, CA 94080, USA.

PMID: 12113832
DOI: 10.1016/s0960-894x(02)00311-6

Abstract

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.

MeSH terms

Amidines / chemistry
Amidines / pharmacology*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Binding Sites
Crystallography, X-Ray
Drug Design
Models, Molecular
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*

Substances

Amidines
Benzimidazoles
Receptors, Cell Surface
Serine Proteinase Inhibitors
Urokinase-Type Plasminogen Activator