| Literature DB >> 27965178 |
Konrad A Szychowski1, Marcin L Leja2, Danylo V Kaminskyy3, Urszula E Binduga2, Oleh R Pinyazhko4, Roman B Lesyk3, Jan Gmiński2.
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.Entities:
Keywords: Anticancer activity; Apoptosis; Cytotoxicity; Thiazolidinone; Thiazolothiopyranes
Mesh:
Substances:
Year: 2016 PMID: 27965178 DOI: 10.1016/j.cbi.2016.12.008
Source DB: PubMed Journal: Chem Biol Interact ISSN: 0009-2797 Impact factor: 5.192