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

被引：14

作者：

Venkatraj, Muthusamy ^{[1
]}

Messagie, Jonas ^{[1
]}

Joossens, Jurgen ^{[1
]}

Lambeir, Anne-Marie ^{[2
]}

Haemers, Achiel ^{[1
]}

Van der Veken, Pieter ^{[1
]}

Augustyns, Koen ^{[1
]}

机构：

[1] Univ Antwerp, Med Chem Lab, B-2610 Antwerp, Belgium

[2] Univ Antwerp, Med Biochem Lab, B-2610 Antwerp, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 04期

关键词：

Naphthamides; Naphthalene sulfonamides; Urokinase inhibitors; uPA; tPA; SELECTIVE INHIBITORS; FACTOR XA; SYSTEM; CANCER; POTENT; IDENTIFICATION; DERIVATIVES; METASTASIS; REDUCTION; DISCOVERY;

D O I：

10.1016/j.bmc.2011.12.040

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Recent drug discovery programs targeting urokinase plasminogen activator (uPA) have resulted in non-peptidic 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 containing non-basic groups as substitute for amidine or guanidine groups. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1557 / 1568

页数：12

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