Naphthyl ketones: A new class of Janus kinase 3 inhibitors

被引：54

作者：

Brown, GR ^{[1
]}

Bamford, AM ^{[1
]}

Bowyer, J ^{[1
]}

James, DS ^{[1
]}

Rankine, N ^{[1
]}

Tang, E ^{[1
]}

Torr, V ^{[1
]}

Culbert, EJ ^{[1
]}

机构：

[1] AstraZeneca, Resp & Inflammat Res, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)00051-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent inhibition of Janus kinase 3 was found for a series of naphthyl(beta-aminoethyl)ketones (e.g. 7, pIC(50) = 7.1 +/- 0.3). Further studies indicated that these compounds fragment in less than 1 h by retro-Michael reaction in the Jak3 in vitro ELISA assay procedure. The breakdown product of 7,2-naphthylvinyl ketone (22, pIC(50) = 6.8 +/- 0.3) showed very similar inhibitory activity to 7. Compounds 7 (in neutral buffer) and 22 will be useful pharmacological tools for the investigation of the Janus tyrosine kinase Jak3. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：575 / 579

页数：5

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