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Study of novel anticancer 4-thiazolidinone derivatives
- Source :
- Chemico-Biological Interactions. 262:46-56
- Publication Year :
- 2017
-
Abstract
- 4-Thiazolidinones are a known class of prospective drug-like molecules, especially in the design of new anticancer agents. Two of the most prominent subtypes of these compounds are 5-ene-2-amino(amino)-4-thiazolidinones and thiopyrano[2,3-d]thiazoles. The latter are considered to be cyclic mimetics of biologically active 5-ene-4-thiazolidinones with similar pharmacological profiles. Therefore, the aim of this study was to evaluate the impact of 4-thiazolidinone-based compounds on cytotoxicity, the apoptotic process, and metabolism in the human squamous carcinoma (SCC-15) cell line. The SCC-15 cells were cultured in phenol red-free DMEM/F12 medium supplemented with 10% FBS, hydrocortisone, and exposed to rising concentrations (1 nM–100 μM) of the studied compounds for 6, 24 and 48 h. Afterwards, reactive oxygen species (ROS) formation, cell viability, caspase-3 activity, and cell metabolism were measured. The obtained results showed that all of the studied compounds in a wide range of concentrations (1 nM–100 μM) increased DCF fluorescence which suggests a stimulation of ROS production. Nevertheless, these new compounds showed cytotoxic and proapoptotic properties only at high (10–100 μM) concentrations. Our studies are the first to be carried out on these compounds and require further investigation to clarify the mechanism of action of their anticancer potential.
- Subjects :
- 0301 basic medicine
Cell Survival
Cytotoxicity
Antineoplastic Agents
Apoptosis
Toxicology
01 natural sciences
Anticancer activity
03 medical and health sciences
Cell Line, Tumor
medicine
Humans
Viability assay
chemistry.chemical_classification
Reactive oxygen species
L-Lactate Dehydrogenase
010405 organic chemistry
Chemistry
Caspase 3
Thiazolothiopyranes
Biological activity
General Medicine
Metabolism
0104 chemical sciences
Squamous carcinoma
Thiazoles
030104 developmental biology
Mechanism of action
Biochemistry
Microscopy, Fluorescence
Cell culture
Thiazolidinone
medicine.symptom
Reactive Oxygen Species
Subjects
Details
- Language :
- English
- ISSN :
- 00092797
- Volume :
- 262
- Database :
- OpenAIRE
- Journal :
- Chemico-Biological Interactions
- Accession number :
- edsair.doi.dedup.....9701b7098a2be0203ab6dc0d300ee3ef
- Full Text :
- https://doi.org/10.1016/j.cbi.2016.12.008