Synthesis of a cyclic analogue of galardin

Da Wei Ma, Wen Gen Wu, Jing Qian, Shen Hui Lang, Qi Zhuang Ye

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

A cyclic analogue 4 of galardin, a known MMP inhibitor, is designed to improve its selectivity. The synthesis of 4 starts from dimethyl (S)-malate using diaselective alkylation and subsequent cyclization and amide formation as key steps. The compound 4 showed MMP inhibitory activity on all MMPs tested with IC50 ranging from 20.1 μM to 104 μM.

Original languageEnglish (US)
Pages (from-to)286-290
Number of pages5
JournalChinese Journal of Chemistry
Volume19
Issue number3
DOIs
StatePublished - 2001

Keywords

  • Alkylation
  • Amide
  • Cyclization
  • Matrix metalloproteinases inhibitor

ASJC Scopus subject areas

  • Chemistry(all)

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