Design and synthesis of subtype-selective cyclooxygenase (COX) inhibitors derived from thalidomide

Hiroko Sano, Tomomi Noguchi, Aya Tanatani, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticlepeer-review

78 Citations (Scopus)


A series of substituted indoline and indole derivatives with cyclooxygenase (COX)-inhibitory activity was prepared during our structural development studies based on thalidomide as a multi-template lead compound. Structure-activity relationship studies indicated that the nature of the substituent introduced at the benzene ring of the indoline (indole) backbone, and the length and type of the linking group between the nitrogen atom of indoline (indole) and the N-substituent are important for the activity. This study has led to the identification of COX-1-selective inhibitors, and these should be useful not only as pharmacological tools to investigate the physiology and pathophysiology of COX, but also as sophisticated leads for the development of novel drugs to treat COX-associated diseases, such as inflammatory diseases, and cancer.

Original languageEnglish
Pages (from-to)3079-3091
Number of pages13
JournalBioorganic and Medicinal Chemistry
Issue number9
Publication statusPublished - May 1 2005


  • COX-1
  • COX-1 selectivity
  • Indole derivatives
  • Indoline derivatives

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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