Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent

Qun Li Luo, Jing Ya Li, Ling Ling Chen, Jia Li, Qi Zhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

8 Scopus citations

Abstract

Systematic SAR studies on the pyridine ring 3-substituent of PCAT, an inhibitor of EcMetAP1 and ScMetAP1, revealed that 3-substituents have different selectivity for EcMetAP1 and ScMetAP1. The selective inhibitors of type I MetAP are useful tools for investigating the detailed interactions between the enzymes and their inhibitors. In addition, these findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.

Original languageEnglish (US)
Pages (from-to)639-644
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number3
DOIs
StatePublished - Feb 1 2005
Externally publishedYes

Keywords

  • Inhibitors
  • Type I MetAPs

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent'. Together they form a unique fingerprint.

  • Cite this