Synthesis and biological evaluation of 2-quinolineacrylamides

Bioorganic & Medicinal Chemistry
2020.0

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.

Knowledge Graph

Similar Paper

Synthesis and biological evaluation of 2-quinolineacrylamides
Bioorganic & Medicinal Chemistry 2020.0
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
Bioorganic & Medicinal Chemistry 2015.0
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2015.0
Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors
European Journal of Medicinal Chemistry 2017.0
Potent Histone Deacetylase Inhibitors Derived from 4-(Aminomethyl)-N-hydroxybenzamide with High Selectivity for the HDAC6 Isoform
Journal of Medicinal Chemistry 2013.0
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif
Bioorganic & Medicinal Chemistry 2018.0
Development of N -hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity
Bioorganic & Medicinal Chemistry 2017.0
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs)
Bioorganic & Medicinal Chemistry 2008.0
(N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo
Journal of Medicinal Chemistry 2018.0
Quinazolin-4-one Derivatives as Selective Histone Deacetylase-6 Inhibitors for the Treatment of Alzheimer’s Disease
Journal of Medicinal Chemistry 2013.0