Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA)

…, A Haemers, P Van der Veken, K Augustyns

Index: Venkatraj, Muthusamy; Messagie, Jonas; Joossens, Jurgen; Lambeir, Anne-Marie; Haemers, Achiel; Van Der Veken, Pieter; Augustyns, Koen Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 4 p. 1557 - 1568

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Abstract

Recent drug discovery programs targeting urokinase plasminogen activator (uPA) have resulted in nonpeptidic inhibitors consisting of amidine or guanidine functional groups attached to aromatic or heteroaromatic scaffolds. There is a general problem of poor oral bioavailability of these charged inhibitors. In this paper, we report the synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as uPA inhibitors ...

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