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, Qizhuang Ye, Jia Li, Fa Jun Nan

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

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
Volume15
Issue number18
DOIs
StatePublished - Sep 15 2005
Externally publishedYes

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Thiazoles
Metal ions
Metals
Ions
Derivatives
alkoxyl radical

Keywords

  • Bioisosteric replacement
  • Type I MetAPs inhibitors

ASJC Scopus subject areas

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

Cite this

Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2 : SAR studies of 5-heteroalkyl substituted TCAT derivatives. / Cui, Yong Mei; Huang, Qing Qing; Xu, Jie; Chen, Ling Ling; Li, Jing Ya; Ye, Qizhuang; Li, Jia; Nan, Fa Jun.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 18, 15.09.2005, p. 4130-4135.

Research output: Contribution to journalArticle

Cui, Yong Mei ; Huang, Qing Qing ; Xu, Jie ; Chen, Ling Ling ; Li, Jing Ya ; Ye, Qizhuang ; Li, Jia ; Nan, Fa Jun. / Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2 : SAR studies of 5-heteroalkyl substituted TCAT derivatives. In: Bioorganic and Medicinal Chemistry Letters. 2005 ; Vol. 15, No. 18. pp. 4130-4135.
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