Rapid assembly of matrix metalloprotease inhibitors using click chemistry

Jun Wang, Mahesh Uttamchandani, Junqi Li, Mingyu Hu, Shao Q. Yao

Research output: Contribution to journalArticle

45 Scopus citations

Abstract

A panel of 96 metalloprotease inhibitors was assembled using "click chemistry" by reacting eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the bidentate compounds against representative metalloproteases provided discerning inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7. The relative ease and convenience of the strategy in constructing focused chemical libraries for rapid in situ screening of MMPs is thereby demonstrated.

Original languageEnglish (US)
Pages (from-to)3821-3824
Number of pages4
JournalOrganic Letters
Volume8
Issue number17
DOIs
StatePublished - Aug 17 2006
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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