[Mechanisms of cytotoxic action of a series of directionally synthesized heterocyclic hydroxamic acids]. / Mekhanizmy tsitotoksicheskogo deistviia riada tsiklicheskikh gidroksamovykh kislot.
Biomed Khim
; 66(4): 332-338, 2020 Jul.
Article
in Ru
| MEDLINE
| ID: mdl-32893823
ABSTRACT
Cyclic hydroxamic acids based on quinazoline-4(3H)-one and dihydroquinazoline-4(1H)-one have been synthesized. The antioxidant and iron-chelating properties of these compounds, their effect on the activity of the histone deacetylase enzyme, and their cytotoxic effect on cells of various tumor lines have been investigated. We have identified two compounds-hits, which exhibit the multipharmacological type of the antineoplastic activity. Their cytotoxic effect on cells of human lung carcinoma A549 and breast adenocarcinoma MCF-7 is obviously associated with their ability to modulate the level of reactive oxygen species and to chelate Fe(II) ions, as well as to inhibit the metalloenzymes, histone deacetylases, involved in the epigenetic regulation of tumor genesis. Thus, the synthesized hydroxamic acids may be considered as a promising basis for creating potential oncolytics.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Histone Deacetylase Inhibitors
/
Antineoplastic Agents
Limits:
Humans
Language:
Ru
Journal:
Biomed Khim
Year:
2020
Document type:
Article
Affiliation country:
Rusia