Literature DB >> 27965178

Study of novel anticancer 4-thiazolidinone derivatives.

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.
Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

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


  13 in total

1.  Synthesis and anticancer activity of novel quinazolinone-based rhodanines.

Authors:  Sherihan El-Sayed; Kamel Metwally; Abdalla A El-Shanawani; Lobna M Abdel-Aziz; Harris Pratsinis; Dimitris Kletsas
Journal:  Chem Cent J       Date:  2017-10-13       Impact factor: 4.215

Review 2.  Thiazoles and Thiazolidinones as COX/LOX Inhibitors.

Authors:  Konstantinos Liaras; Maria Fesatidou; Athina Geronikaki
Journal:  Molecules       Date:  2018-03-18       Impact factor: 4.411

3.  Anticancer properties of 5Z-(4-fluorobenzylidene)-2-(4-hydroxyphenylamino)-thiazol-4-one.

Authors:  Konrad A Szychowski; Danylo V Kaminskyy; Marcin L Leja; Anna P Kryshchyshyn; Roman B Lesyk; Jakub Tobiasz; Maciej Wnuk; Tadeusz Pomianek; Jan Gmiński
Journal:  Sci Rep       Date:  2019-07-23       Impact factor: 4.379

Review 4.  5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.

Authors:  Danylo Kaminskyy; Anna Kryshchyshyn; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2017-09-20       Impact factor: 6.514

5.  Characterisation of Biologically Active Hydrolysates and Peptide Fractions of Vacuum Packaging String Bean (Phaseolus vulgaris L.).

Authors:  Anna Jakubczyk; Monika Karaś; Piotr Stanikowski; Beata Rutkowska; Magdalena Dziedzic; Ewelina Zielińska; Konrad A Szychowski; Urszula E Binduga; Kamila Rybczyńska-Tkaczyk; Barbara Baraniak
Journal:  Foods       Date:  2020-06-28

6.  New Substituted 5-Benzylideno-2-Adamantylthiazol[3,2-b][1,2,4]Triazol-6(5H)ones as Possible Anti-Inflammatory Agents.

Authors:  Christophe Tratrat; Michelyne Haroun; Aliki Paparisva; Charalmpos Kamoutsis; Anthi Petrou; Antonis Gavalas; Phaedra Eleftheriou; Athina Geronikaki; Katharigatta N Venugopala; Hafedh Kochkar; Anroop B Nair
Journal:  Molecules       Date:  2021-01-27       Impact factor: 4.411

7.  Possibility to Biotransform Anthracyclines by Peroxidases Produced by Bjerkandera adusta CCBAS 930 with Reduction of Geno- and Cytotoxicity and Pro-Oxidative Activity.

Authors:  Kamila Rybczyńska-Tkaczyk; Teresa Korniłłowicz-Kowalska; Konrad A Szychowski
Journal:  Molecules       Date:  2021-01-17       Impact factor: 4.411

8.  5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies.

Authors:  Michelyne Haroun; Christophe Tratrat; Aggeliki Kolokotroni; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Marina Kostic; Marina Sokovic; Alejandro Carazo; Přemysl Mladěnka; Nagaraja Sreeharsha; Katharigatta N Venugopala; Anroop B Nair; Heba S Elsewedy
Journal:  Antibiotics (Basel)       Date:  2021-03-17

Review 9.  Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview.

Authors:  Dimitris Matiadis; Marina Sagnou
Journal:  Int J Mol Sci       Date:  2020-07-31       Impact factor: 5.923

10.  Induction of Cyp450 enzymes by 4-thiazolidinone-based derivatives in 3T3-L1 cells in vitro.

Authors:  Konrad A Szychowski; Bartosz Skóra; Anna Kryshchyshyn-Dylevych; Danylo Kaminskyy; Kamila Rybczyńska-Tkaczyk; Roman Lesyk; Jan Gmiński
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2020-11-21       Impact factor: 3.000

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