Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-pyridinylguanidines

被引：24

作者：

Barber, CG ^{[1
]}

Dickinson, RP ^{[1
]}

Horne, VA ^{[1
]}

机构：

[1] Pfizer Ltd, Global Res & Dev, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)00701-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification of 2-pyridinylguanidines (e.g. 27 and 28) as selective inhibitors of urokinase-type plasminogen activator (uPA) is described. The X-ray crystal structure of 27 has been determined, and modelling has been used to predict binding in the enzyme active site. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：181 / 184

页数：4

共 28 条

[1]

ALLEN D, Patent No. 0035886

[2]

Bridges A J, 1993, Bioorg Med Chem, V1, P403, DOI 10.1016/S0968-0896(00)82150-1

[3]

COLLEN D, 1995, THROMB HAEMOSTASIS, V74, P161

[4]

Evans DM, 1997, DRUG NEWS PERSPECT, V10, P85

[5] UROKINASE-TYPE PLASMINOGEN-ACTIVATOR AND ITS RECEPTOR - NEW TARGETS FOR ANTIMETASTATIC THERAPY [J].

FAZIOLI, F ;

BLASI, F .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1994, 15 (01) :25-29

[6] AMIDINO-SUBSTITUTED AROMATIC HETEROCYCLES AS PROBES OF THE SPECIFICITY POCKET OF TRYPSIN-LIKE PROTEASES [J].

GERATZ, JD ;

STEVENS, FM ;

POLAKOSKI, KL ;

PARRISH, RF ;

TIDWELL, RR .

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1979, 197 (02) :551-559

[7] INHIBITORY EFFECT OF AMIDINO-SUBSTITUTED HETEROCYCLIC-COMPOUNDS ON THE AMIDASE ACTIVITY OF PLASMIN AND OF HIGH AND LOW-MOLECULAR WEIGHT UROKINASE AND ON UROKINASE-INDUCED PLASMINOGEN ACTIVATION [J].

GERATZ, JD ;

SHAVER, SR ;

TIDWELL, RR .

THROMBOSIS RESEARCH, 1981, 24 (1-2) :73-83

[8]

GERATZ JD, 1975, THROMB DIATH HAEMO, V33, P220

[9]

ILLIG CR, 2000, 218 ACS NAT M

[10] PROBING STRUCTURE-FUNCTION-RELATIONSHIPS OF TISSUE-TYPE PLASMINOGEN-ACTIVATOR BY SITE-SPECIFIC MUTAGENESIS [J].

MADISON, EL .

FIBRINOLYSIS, 1994, 8 :221-236

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