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.
Mackman
Richard L
RL
Celera, 180 Kimball Way, South San Francisco, CA 94080, USA.
Hui
Hon C
HC
Breitenbucher
J Guy
JG
Katz
Bradley A
BA
Luong
Christine
C
Martelli
Arnold
A
McGee
Danny
D
Radika
Kesavan
K
Sendzik
Martin
M
Spencer
Jeffrey R
JR
Sprengeler
Paul A
PA
Tario
James
J
Verner
Erik
E
Wang
Jing
J
D000578:Amidines / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015195:Drug Design; D008958:Models, Molecular; D011485:Protein Binding; D011956:Receptors, Cell Surface / Q000737:chemistry / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
D000578:Amidines; D001562:Benzimidazoles; D011956:Receptors, Cell Surface; D015842:Serine Proteinase Inhibitors; D014568:Urokinase-Type Plasminogen Activator