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.
Celera, 180 Kimball Way, South San Francisco, CA 94080, USA.
Richard L
RL
Mackman
Hon C
HC
Hui
J Guy
JG
Breitenbucher
Bradley A
BA
Katz
Christine
C
Luong
Arnold
A
Martelli
Danny
D
McGee
Kesavan
K
Radika
Martin
M
Sendzik
Jeffrey R
JR
Spencer
Paul A
PA
Sprengeler
James
J
Tario
Erik
E
Verner
Jing
J
Wang
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