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, Qizhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

8 Citations (Scopus)

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

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Enzyme Inhibitors
pyridine-2-carboxylic acid thiazol-2-ylamide
pyridine

Keywords

  • Inhibitors
  • Type I MetAPs

ASJC Scopus subject areas

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

Cite this

Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2 : SAR studies on the pyridine ring 3-substituent. / Luo, Qun Li; Li, Jing Ya; Chen, Ling Ling; Li, Jia; Ye, Qizhuang; Nan, Fa Jun.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 3, 01.02.2005, p. 639-644.

Research output: Contribution to journalArticle

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AU - Ye, Qizhuang

AU - Nan, Fa Jun

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