Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives

Yong Mei Cui, Qing Qing Huang, Jie Xu, Ling Ling Chen, Jing Ya Li, Qi Zhuang Ye, Jia Li, Fa Jun Nan

Research output: Contribution to journalArticle

15 Scopus citations

Abstract

A series of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT, 4) derivatives were designed and synthesized according to simple bioisosteric replacement from previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors. The preliminary SAR studies demonstrated that these TCAT series of compounds showed different activity and selectivity compared with those of the corresponding PCAT compounds. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.

Original languageEnglish (US)
Pages (from-to)3732-3736
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number16
DOIs
StatePublished - Aug 15 2005
Externally publishedYes

ASJC Scopus subject areas

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

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