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, Qizhuang Ye, Jia Li, Fa Jun Nan

Research output: Contribution to journalArticle

14 Citations (Scopus)

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

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Thiazoles
Carboxylic Acids
Derivatives
pyridine-2-carboxylic acid thiazol-2-ylamide

ASJC Scopus subject areas

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

Cite this

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. / 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. 16, 15.08.2005, p. 3732-3736.

Research output: Contribution to journalArticle

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