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

Vibha Oza, Susan Ashwell, Patrick Brassil, Jason Breed, Chun Deng, Jay Ezhuthachan, Heather Haye, Candice Horn, James Janetka, Paul Lyne, Nicholas Newcombe, Ludo Otterbien, Martin Pass, Jon Read, Sian Roswell, Mei Su, Dorin Toader, Dingwei Yu, Yan Yu, Anna ValentinePeter Webborn, Ann White, Sonya Zabludoff, Xiaolan Zheng

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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.

Original languageEnglish
Pages (from-to)5133-5138
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number17
DOIs
StatePublished - Sep 1 2010

Keywords

  • CHK1
  • Checkpoint Kinase inhibitors
  • Triazolones

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