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Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Oza V,Ashwell S,Brassil P,Breed J,Deng C,Ezhuthachan J,Haye H,Horn C,Janetka J,Lyne P,Newcombe N,Otterbien L,Pass M,Read J,Roswell S,Su M,Toader D,Yu D,Yu Y,Valentine A,Webborn P,White A,Zabludoff S,Zheng X

doi

10.1016/j.bmcl.2010.07.015

subject

Has Abstract

pub_date

2010-09-01 00:00:00

pages

5133-8

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00971-6

journal_volume

20

pub_type

杂志文章

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