Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors

被引：81
|
作者：
Baxter, A
Brough, S
Cooper, A
Floettmann, E
Foster, S
Harding, C
Kettle, J
McInally, T
Martin, C
Mobbs, M
Needham, M
Newham, P
Paine, S
St-Gallay, S
Salter, S
Unitt, J
Xue, YF
机构：
[1] AstraZeneca R&D, Loughborough LE11 5RH, Leics, England
[2] AstraZeneca R&D Alderley Pk, Macclesfield SK10 4TG, Cheshire, England
[3] AstraZeneca R&D, Struct Chem Lab, S-43183 Molndal, Sweden
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期
关键词：
hit-to-lead; IKK inhibitor; kinase;
D O I：
10.1016/j.bmcl.2004.03.058
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2817 / 2822
页数：6
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