Angiogenesis inhibitors derived from thalidomide

Tomomi Noguchi, Haruka Fujimoto, Hiroko Sano, Atsushi Miyajima, Hiroyuki Miyachi, Yuichi Hashimoto

Research output: Contribution to journalArticlepeer-review

52 Citations (Scopus)

Abstract

5-Hydroxy-2-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33: 10), which was obtained during our previous structural development studies on thalidomide, was revealed to possess potent anti-angiogenic activity in a human umbilical vein endothelial cell (HUVEC) assay. Thalidomide (1) and its metabolite, 5-hydroxythalidomide (5-HT: 2), which possesses a hydroxyl group at the position corresponding to that of 5HPP-33, as well as IMiDs (immunomodulatory derivatives of thalidomide: 3 and 5), also showed weak or moderate activity in the same assay.

Original languageEnglish
Pages (from-to)5509-5513
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number24
DOIs
Publication statusPublished - Dec 15 2005

Keywords

  • Angiogenesis
  • HUVEC
  • Phthalimide
  • Structural development
  • Thalidomide

ASJC Scopus subject areas

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

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