Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

  • James W. Janetka
  • , Lynsie Almeida
  • , Susan Ashwell
  • , Patrick J. Brassil
  • , Kevin Daly
  • , Chun Deng
  • , Thomas Gero
  • , Roberta E. Glynn
  • , Candice L. Horn
  • , Stephanos Ioannidis
  • , Paul Lyne
  • , Nicholas J. Newcombe
  • , Vibha B. Oza
  • , Martin Pass
  • , Stephanie K. Springer
  • , Mei Su
  • , Dorin Toader
  • , Melissa M. Vasbinder
  • , Dingwei Yu
  • , Yan Yu
  • Sonya D. Zabludoff

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

Original languageEnglish
Pages (from-to)4242-4248
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number14
DOIs
StatePublished - Jul 15 2008

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