A novel series of potent and selective IKK2 inhibitors

被引：48

作者：

Bingham, AH ^{[1
]}

Davenport, RJ ^{[1
]}

Gowers, L ^{[1
]}

Knight, RL ^{[1
]}

Lowe, C ^{[1
]}

Owen, DA ^{[1
]}

Parry, DM ^{[1
]}

Pitt, WR ^{[1
]}

机构：

[1] Celltech R&D Ltd, Cambridge CB1 6GS, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 02期

关键词：

potent; selective; IKK2; inhibitors;

D O I：

10.1016/j.bmcl.2003.10.047

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of ammopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：409 / 412

页数：4

共 20 条

[1]

[Anonymous], MULTIPLE LINEAR REGR

[2] NF-kappa B: Ten years after [J].