Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines

CG Barber, RP Dickinson, PV Fish

Index: Barber, Christopher G.; Dickinson, Roger P.; Fish, Paul V. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3227 - 3230

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Citation Number: 32

Abstract

A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7- aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivity, and has been selected as a candidate for clinical evaluation.