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

页码：2817 / 2822

页数：6

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