4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
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.
Celera, 180 Kimball Way, South San Francisco, CA 94080, USA.
Jeffrey R
JR
Spencer
Danny
D
McGee
Darin
D
Allen
Bradley A
BA
Katz
Christine
C
Luong
Martin
M
Sendzik
Neil
N
Squires
Richard L
RL
Mackman
D000588:Amines / Q000737:chemistry / Q000494:pharmacology; D001550:Benzamidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D019791:Guanidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D008958:Models, Molecular; D011485:Protein Binding; D011956:Receptors, Cell Surface / Q000737:chemistry / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000588:Amines; D001550:Benzamidines; D011956:Receptors, Cell Surface; D015842:Serine Proteinase Inhibitors; D014568:Urokinase-Type Plasminogen Activator; D019791:Guanidine