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Synthesis and biological evaluation of 2-quinolineacrylamides.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2020 Feb 01; Vol. 28 (3), pp. 115250. Date of Electronic Publication: 2019 Dec 19. - Publication Year :
- 2020
-
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.<br /> (Copyright © 2019 Elsevier Ltd. All rights reserved.)
- Subjects :
- A549 Cells
Acrylamides chemical synthesis
Acrylamides chemistry
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HCT116 Cells
Histone Deacetylase 6 metabolism
Histone Deacetylase Inhibitors chemical synthesis
Histone Deacetylase Inhibitors chemistry
Humans
Molecular Structure
Quinolines chemical synthesis
Quinolines chemistry
Structure-Activity Relationship
Tumor Cells, Cultured
Acrylamides pharmacology
Antineoplastic Agents pharmacology
Histone Deacetylase 6 antagonists & inhibitors
Histone Deacetylase Inhibitors pharmacology
Quinolines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 28
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31924504
- Full Text :
- https://doi.org/10.1016/j.bmc.2019.115250