4-(1,3-Thiazol-2-yl) morpholine derivatives as inhibitors of phosphoinositide 3-kinase

被引：41

作者：

Alexander, Rikki

Balasundaram, Ahrani

Batchelor, Mark

Brookings, Daniel

Crepy, Karen

Crabbe, Tom

Deltent, Marie-France

Driessens, Frank

Gill, Andrew

Harris, Sue

Hutchinson, Gillian

Kulisa, Claire

Merriman, Mark

Mistry, Prakash

Parton, Ted

Turner, James

Whitcombe, Ian

Wright, Sara

机构：

[1] UCB, Dept Med Chem, Slough SL1 3WE, Berks, England

[2] UCB, Dept Biol, Slough SL1 3WE, Berks, England

[3] UCB Pharma SA, CPR, B-1420 Brain Lalleud, Belgium

[4] UCB Pharma SA, ES, B-1420 Brain Lalleud, Belgium

[5] UCB, Dept Pharmacol, Slough SL1 3WE, Berks, England

[6] UCB, Dept DMPK, Slough SL1 3WE, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 15期

关键词：

PI3K; oncology; kinase inhibitor;

D O I：

10.1016/j.bmcl.2008.06.076

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo pro. ling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4316 / 4320

页数：5

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Phosphoinositide 3-kinase signalling pathways in tumor progression, invasion and angiogenesis [J].