Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors-Hit to lead exploration

被引：17

作者：

Oza, Vibha ^{[1
]}

Ashwell, Susan ^{[1
]}

Brassil, Patrick ^{[1
]}

Breed, Jason ^{[2
]}

Deng, Chun ^{[1
]}

Ezhuthachan, Jay ^{[1
]}

Haye, Heather ^{[2
]}

Horn, Candice ^{[1
]}

Janetka, James ^{[1
]}

Lyne, Paul ^{[1
]}

Newcombe, Nicholas ^{[2
]}

Otterbien, Ludo ^{[2
]}

Pass, Martin ^{[2
]}

Read, Jon ^{[2
]}

Roswell, Sian ^{[2
]}

Su, Mei ^{[1
]}

Toader, Dorin ^{[1
]}

Yu, Dingwei ^{[1
]}

Yu, Yan ^{[1
]}

Valentine, Anna ^{[2
]}

Webborn, Peter ^{[2
]}

White, Ann ^{[2
]}

Zabludoff, Sonya ^{[1
]}

Zheng, Xiaolan ^{[1
]}

机构：

[1] AstraZeneca R&D Boston, Waltham, MA 02451 USA

[2] AstraZeneca R&D Alderley Pk, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 17期

关键词：

Triazolones; CHK1; Checkpoint Kinase inhibitors; PROTEIN-KINASE; UCN-01;

D O I：

10.1016/j.bmcl.2010.07.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5133 / 5138

页数：6

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