Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Masaaki Sawa, Kiriko Kurokawa, Yoshimasa Inoue, Hirosato Kondo, Kohichiro Yoshino

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

A novel series of phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9.

Original languageEnglish
Pages (from-to)2021-2024
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number12
DOIs
Publication statusPublished - Jun 16 2003
Externally publishedYes

All Science Journal Classification (ASJC) codes

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

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