2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

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Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22.

PubMed ID

12113832 [ View in PubMed

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Abstract

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.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
6-fluoro-2-(2-hydroxy-3-isobutoxy-phenyl)-1H-benzoimidazole-5-carboxamidine	Urokinase-type plasminogen activator	Ki (nM)	190	N/A	N/A	Details