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, Qi Zhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

15 Scopus citations

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

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Keywords

  • Type I MetAPs inhibitors

ASJC Scopus subject areas

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

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