Hydroxamic Acid-Based Histone Deacetylase (HDAC) Inhibitors Bearing a Pyrazole Scaffold and a Cinnamoyl Linker.
HDAC inhibitors
N1-H-pyrazole
N1-aryl-pyrazole
antiproliferative activity
hydroxamic acid
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
21 Feb 2019
21 Feb 2019
Historique:
received:
31
01
2019
revised:
15
02
2019
accepted:
18
02
2019
entrez:
24
2
2019
pubmed:
24
2
2019
medline:
30
5
2019
Statut:
epublish
Résumé
Genetic abnormalities have been conventionally considered as hallmarks of cancer. However, recent studies have demonstrated that epigenetic mechanisms are also implicated in the insurgence and development of cancer. Patterns of the epigenetic component include DNA methylation and histone modifications. Acetylation of histones is controlled by histone acetyltransferases (HATs) and histone deacetylases (HDACs). Imbalance of these two enzymatic systems is known to be a key factor in tumor progression. Because HDACs have been found to function incorrectly in cancer, various HDAC inhibitors (HDACIs) are being investigated to act as cancer chemotherapeutics. Herein, we report the synthesis, docking studies and biological activity of a series of hydroxamic acid-based HDACIs bearing an
Identifiants
pubmed: 30795625
pii: ijms20040945
doi: 10.3390/ijms20040945
pmc: PMC6412695
pii:
doi:
Substances chimiques
Coumaric Acids
0
Histone Deacetylase Inhibitors
0
Hydroxamic Acids
0
Pyrazoles
0
Histone Deacetylases
EC 3.5.1.98
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : MIUR
ID : FFABRA2017_MICALE_NICOLA_RI
Déclaration de conflit d'intérêts
The authors declare no conflict of interest.
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