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

研究成果: 雜誌貢獻文章

摘要

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.

原文英語
文章編號115250
期刊Bioorganic and Medicinal Chemistry
28
發行號3
DOIs
出版狀態已發佈 - 二月 1 2020

指紋

Protein Isoforms
HCT116 Cells
Ether
Western Blotting
A549 Cells

ASJC Scopus subject areas

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

引用此文

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.

於: Bioorganic and Medicinal Chemistry, 卷 28, 編號 3, 115250, 01.02.2020.

研究成果: 雜誌貢獻文章

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AU - Chen, Shiou Sheng

AU - Lee, Hsueh Yun

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