The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate

Jane L. Wang, Jeffery Carter, James R. Kiefer, Ravi G. Kurumbail, Jennifer L. Pawlitz, David Brown, Susan J. Hartmann, Matthew J. Graneto, Karen Seibert, John J. Talley

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

Abstract

In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. 5c-(S) (SD-8381) was advanced into clinical studies due to its superior in vivo potency. The high plasma protein binding (>99% bound) of 5c-(S) has resulted in a surprisingly long human half life t1/2 = 360 h.

Original languageEnglish
Pages (from-to)7155-7158
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number23
DOIs
StatePublished - Dec 1 2010

Keywords

  • Benzopyran
  • COX-2 inhibitor
  • Clinical candidate
  • Cyclooxygenase
  • Half-life
  • Plasma protein bound
  • X-ray crystal structure

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