Synthesis and biological evaluation of 2-quinolineacrylamides

Shih Wei Wang, Mei Hsiang Lin, Fu Chun Hsu, Mei Chuan Chen, Jing Ping Liou, Yi Ting Liu, Shiou Sheng Chen, Hsueh Yun Lee

Research output: Contribution to journalArticle

Abstract

A series of C6-substituted N-hydroxy-2-quinolineacrylamides (3–15), with four types of bridging groups have been synthesized. Most of these compounds exhibit antiproliferative activity against A549 and HCT116 cells and Western blot analysis revealed that they are able to inhibit HDAC. Measurement of the HDAC isoform activity of ether-containing compounds showed that compound 9 has distinct HDAC6 selectivity, more than 300-fold over other isoforms. This paper describes the development of 6-aryloxy-N-hydroxy-2-quinolineacrylamides as potential HDAC6 inhibitors.

Original languageEnglish
Article number115250
JournalBioorganic and Medicinal Chemistry
Volume28
Issue number3
DOIs
Publication statusPublished - Feb 1 2020

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Protein Isoforms
HCT116 Cells
Ether
Western Blotting
A549 Cells

Keywords

  • 2-Quinolineacrylamide
  • Histone deacetylase
  • Ullmann reaction

ASJC Scopus subject areas

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

Cite this

Synthesis and biological evaluation of 2-quinolineacrylamides. / Wang, Shih Wei; Lin, Mei Hsiang; Hsu, Fu Chun; Chen, Mei Chuan; Liou, Jing Ping; Liu, Yi Ting; Chen, Shiou Sheng; Lee, Hsueh Yun.

In: Bioorganic and Medicinal Chemistry, Vol. 28, No. 3, 115250, 01.02.2020.

Research output: Contribution to journalArticle

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