Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT 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

14 Scopus citations


Systematic SAR studies on the thiazole ring 5-substituent of TCAT derivatives revealed that the introduction of a β-alkoxy or an amino group enhanced the inhibitory activity significantly. The present compounds are representative of specific Co(II)-MetAP1 inhibitors. Before the physiologically relevant metal ions for MetAPs are established, these small molecular compounds could be used as tools for detailed biological studies.

Original languageEnglish (US)
Pages (from-to)4130-4135
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number18
StatePublished - Sep 15 2005



  • Bioisosteric replacement
  • 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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