Effects of netropsin and pentamidine amino analogues on the amidolytic activity of plasmin, trypsin and urokinase.
Inhibitory effects of nine carbocyclic DNA minor groove binders on amidolytic activities of plasmin, trypsin and urokinase were examined. Some of the studied compounds affected plasmin or trypsin activity, but not urokinase activity. One of the pentamidine analogues (5) and two bis-netropsin like compounds (6, 8) were potent inhibitors of plasmin (IC50 equals 90 and 100 microM), whereas an analogue of netropsin (2) was trypsin inhibitor (IC50 = 100 microM).
Pućkowska
Anna
A
Department of Organic Chemistry, Medical University of Bialystok, ul. Kilińskiego 1, 15-089 Bialystok, Poland. pucanka@amb.edu.pl
Midura-Nowaczek
Krystyna
K
Bruzgo
Irena
I
D000588:Amines / Q000494:pharmacology*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D009429:Netropsin / Q000031:analogs & derivatives* / Q000494:pharmacology; D010419:Pentamidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014361:Trypsin Inhibitors / Q000494:pharmacology*; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
D000588:Amines; D014361:Trypsin Inhibitors; D009429:Netropsin; D010419:Pentamidine; D005341:Fibrinolysin; D014568:Urokinase-Type Plasminogen Activator