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Synthesis of Indoline‐Based Benzhydroxamic Acids as Potential HDAC6 Inhibitors
Author(s) -
Depetter Yves,
Geurs Silke,
Franceus Jorick,
Knez Damijan,
Desmet Tom,
De Bosscher Karolien,
De Wever Olivier,
Gobec Stanislav,
D'hooghe Matthias
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201902042
Subject(s) - indoline , chemistry , hdac6 , stereochemistry , monoamine neurotransmitter , combinatorial chemistry , biochemistry , pharmacology , biology , serotonin , histone deacetylase , histone , receptor , gene
The synthesis of HDAC6 inhibitors has attracted considerable interest in medicinal chemistry because of their drug potential in different therapeutic areas. In this paper, the preparation of two classes of indoline‐based benzhydroxamic acids is presented, bearing either the classical 4‐hydroxycarbamoylbenzyl or a hitherto unexplored 2‐[4‐(hydroxycarbamoyl)phenoxy]ethyl group, which were shown to exhibit complete HDAC6 inhibition at 10 μM. Furthermore, evaluation of these compounds for interaction with cholinesterases (AChE and BChE) and monoamine oxidases (A and B) revealed some of them to be moderate inhibitors in that respect as well.