Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase

被引：30

作者：

Ngu, Khehyong ^{[1
]}

Weinstein, David S. ^{[1
]}

Liu, Wen ^{[1
]}

Langevine, Charles ^{[1
]}

Combs, Donald W. ^{[1
]}

Zhuang, Shaobin ^{[1
]}

Chen, Xing ^{[1
]}

Madsen, Cort S. ^{[1
]}

Harper, Timothy W. ^{[1
]}

Ahmad, Saleem ^{[1
]}

Robl, Jeffrey A. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Res & Dev, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 14期

关键词：

15-Lipoxygenase; Inhibitors; Pyrazole; Sulfonamides; Sulfamides; Arachidonic acid; Linoleic acid; LIPOXYGENASE INHIBITORS; SELECTIVE INHIBITORS; CANCER CELLS; 12-LIPOXYGENASE; 12/15-LIPOXYGENASE; DERIVATIVES; DISCOVERY; DISEASE; DESIGN; ENZYME;

D O I：

10.1016/j.bmcl.2011.05.107

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4141 / 4145

页数：5

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