Novel xanthone derivatives as potent sirtuin 2 inhibitors

[Display omitted] Six amino derivatives of xanthone were obtained via chemical synthesis. Biochemical studies revealed their SIRT2 inhibitory activity ranging from 48.5 % (compound 4, 5-chloro-2-((4-(3-methoxyphenyl)piperazin-1-yl)methyl)-9H-xanthen-9-one hydrochloride) to 93.2 % (compound 3, 5-chlo...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2024-03, Vol.100, p.129620-129620, Article 129620
Main Authors: Mazur, Gabriela, Pańczyk-Straszak, Katarzyna, Krysińska, Karolina, Niemiec, Karolina, Waszkielewicz, Anna
Format: Article
Language:English
Subjects:
Amines
Lipophilicity
SIRT2
Sirtuins
Xanthone
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] Six amino derivatives of xanthone were obtained via chemical synthesis. Biochemical studies revealed their SIRT2 inhibitory activity ranging from 48.5 % (compound 4, 5-chloro-2-((4-(3-methoxyphenyl)piperazin-1-yl)methyl)-9H-xanthen-9-one hydrochloride) to 93.2 % (compound 3, 5-chloro-2-(((2-methoxyphenethyl)amino)methyl)-9H-xanthen-9-one hydrochloride). The structure–activity analysis showed favourable properties of secondary amines relative to tertiary piperazine derivatives. The tested compounds do not possess additional SIRT1 activating activity and no antioxidant activity (DPPH in vitro assay). Comprehensive analysis of the lipophilicity of the obtained compounds was also performed. For compound 3 potential molecular targets and similar active compounds were predicted in order to facilitate further research in this group of compounds.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2024.129620