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Development of pyrazine-anilinobenzamides as histone deacetylase HDAC1-3 selective inhibitors and biological testing against pancreas cancer cell lines.
Methods Mol. Biol. 2589, 145-155 (2023)
Class I histone deacetylase (HDAC) enzymes are key regulators of cell proliferation and are frequently dysregulated in cancer cells. Here we describe the synthesis of a novel series of class-I selective HDAC inhibitors containing anilinobenzamide moieties as ZBG connected with a central (piperazin-1-yl)pyrazine moiety. Compounds were tested in vitro against class-I HDAC1, 2, and 3 isoforms. Some highly potent HDAC inhibitors were obtained and were tested in pancreatic cancer cells and showed promising activity. Moreover, we summarize how the growth-inhibitory effects of these compounds can be determined in murine pancreatic cancer cell lines.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Anilinobenzamides ; Capping Group ; Class-i Histone Deacetylases Inhibitors ; Hdac ; Pancreas Cancer
Language
english
Publication Year
2023
Prepublished in Year
2022
HGF-reported in Year
2022
ISSN (print) / ISBN
1064-3745
e-ISSN
1940-6029
Book Volume Title
HDAC/HAT Function Assessment and Inhibitor Development
Journal
Methods in Molecular Biology
Quellenangaben
Volume: 2589,
Pages: 145-155
Publisher
Springer
Publishing Place
Berlin [u.a.]
Reviewing status
Peer reviewed
Institute(s)
Institute of Experimental Genetics (IEG)
POF-Topic(s)
30201 - Metabolic Health
Research field(s)
Genetics and Epidemiology
PSP Element(s)
G-500600-004
Scopus ID
85140177259
PubMed ID
36255623
Erfassungsdatum
2022-10-26