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

Jeffrey R Spencer; Danny McGee; Darin Allen; Bradley A Katz; Christine Luong; Martin Sendzik; Neil Squires; Richard L Mackman

doi:10.1016/s0960-894x(02)00312-8

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

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2023-6. doi: 10.1016/s0960-894x(02)00312-8.

Authors

Jeffrey R Spencer¹, Danny McGee, Darin Allen, Bradley A Katz, Christine Luong, Martin Sendzik, Neil Squires, Richard L Mackman

Affiliation

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

PMID: 12113833
DOI: 10.1016/s0960-894x(02)00312-8

Abstract

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.

MeSH terms

Amines / chemistry
Amines / pharmacology
Benzamidines / chemical synthesis
Benzamidines / chemistry*
Benzamidines / pharmacology*
Binding Sites
Crystallography, X-Ray
Guanidine / analogs & derivatives*
Guanidine / chemical synthesis
Guanidine / pharmacology
Models, Molecular
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

Substances

Amines
Benzamidines
Receptors, Cell Surface
Serine Proteinase Inhibitors
Urokinase-Type Plasminogen Activator
Guanidine