Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1

SAR studies on the determination of the key scaffold

Qun Li Luo, Jing Ya Li, Zhi Ying Liu, Ling Ling Chen, Jia Li, Qizhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Systematic SAR studies on the HTS hit pyridine-2-carboxylic acid thiazol-2-ylamide (PACT) analogues revealed that the scaffold of PCAT is indispensable for the inhibition of type I MetAP. For effective inhibition of the enzyme, the most suitable position to modify is the 3-position of the pyridine ring of PCAT, and the best substituents are those containing O or N atoms connected directly with the pyridine ring. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.

Original languageEnglish (US)
Pages (from-to)635-638
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number3
DOIs
StatePublished - Feb 1 2005
Externally publishedYes

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Scaffolds
Atoms
Enzymes
pyridine-2-carboxylic acid thiazol-2-ylamide
pyridine

Keywords

  • Type I MetAPs inhibitors

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 1 : SAR studies on the determination of the key scaffold. / Luo, Qun Li; Li, Jing Ya; Liu, Zhi Ying; Chen, Ling Ling; Li, Jia; Ye, Qizhuang; Nan, Fa Jun.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 3, 01.02.2005, p. 635-638.

Research output: Contribution to journalArticle

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