Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activity

Takanori Nakamura, Tomomi Noguchi, Hisayoshi Kobayashi, Hiroyuki Miyachi, Yuichi Hashimoto

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

Mono- and dihydroxylated metabolites of thalidomide were efficiently prepared and characterized, and their inhibitory activity on tumor necrosis factor (TNF)-α production in the human monocytic leukemia cell line THP-1 was evaluated. 5,N-Dihydroxythalidomide was a much more potent TNF-α production inhibitor than thalidomide.

Original languageEnglish
Pages (from-to)1709-1714
Number of pages6
JournalChemical and Pharmaceutical Bulletin
Volume54
Issue number12
DOIs
Publication statusPublished - Dec 18 2006

Keywords

  • Hydroxythalidomide
  • Metabolite
  • Thalidomide
  • Tumor necrosis factor (TNF)-α modulator

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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