Synthesis and biological evaluation of 2-quinolineacrylamides

Bioorg Med Chem. 2020 Feb 1;28(3):115250. doi: 10.1016/j.bmc.2019.115250.

Shih-Wei Wang ¹, Mei-Hsiang Lin ², Fu-Chun Hsu ², Mei-Chuan Chen ³, Jing-Ping Liou ², Yi-Ting Liu ², Shiou-Sheng Chen ⁴, Hsueh-Yun Lee ⁵

Affiliations

1 Department of Medicine, Mackay Medical College, New Taipei City, Taiwan; Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.
2 School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan.
3 Ph.D. Program for the Clinical Drug Discovery from Botanical Herbs, College of Pharmacy, Taipei Medical University, Taiwan.
4 Department of Urology, National Yang-Ming University School of Medicine, Taipei, Taiwan; Division of Urology, Taipei City Hospital HepingFuyou Branch, Taipei, Taiwan.
5 School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan; Ph.D Program in Biotechnology Research and Development, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan. Electronic address: [email protected].

PMID: 31924504 DOI: 10.1016/j.bmc.2019.115250

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.

Keywords

2-Quinolineacrylamide; Histone deacetylase; Ullmann reaction.

Products

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Description

Target

Research Area
HY-150694

HDAC6-IN-11

HDAC6 Inhibitor

HDAC

Cancer

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