Search results for "Thiazolidinone"

showing 3 items of 3 documents

Study of novel anticancer 4-thiazolidinone derivatives

2016

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, hydrocor…

0301 basic medicineCell SurvivalCytotoxicityAntineoplastic AgentsApoptosisToxicology01 natural sciencesAnticancer activity03 medical and health sciencesCell Line TumormedicineHumansViability assayCytotoxicitychemistry.chemical_classificationReactive oxygen speciesL-Lactate Dehydrogenase010405 organic chemistryChemistryCaspase 3ThiazolothiopyranesBiological activityGeneral MedicineMetabolism0104 chemical sciencesSquamous carcinomaThiazoles030104 developmental biologyMechanism of actionBiochemistryMicroscopy FluorescenceCell cultureThiazolidinonemedicine.symptomReactive Oxygen SpeciesChemico-Biological Interactions
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Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ)

2017

Peroxisome proliferator-activated receptors (PPARs) play an important role in numerous chronic diseases such as diabetes, obesity, atherosclerosis and cancer, and PPAR modulators are among the approved drugs and drug-candidates for their treatment. The aim of this study was to elucidate the involvement of PPARs in the mechanism of cytotoxic and pro-apoptotic action of novel anticancer 4-thiazolidinone derivatives (Les-2194, Les-3377, Les-3640) and approved 4-thiazolidinones (Rosiglitazone, Pioglitazone) towards the human squamous carcinoma (SCC-15) cell line. Experiments with 4-thiazaolidinone derivatives and PPAR-specific siRNA were conducted and PPARα, PPARβ and PPARγ mRNA expression was …

0301 basic medicinePPARsCytotoxicityPeroxisome proliferator-activated receptorAntineoplastic AgentsApoptosisPharmacologySCC-1503 medical and health sciencesStructure-Activity Relationship0302 clinical medicineCell Line TumorDrug DiscoverymedicineGene silencingHumansViability assayRNA MessengerReceptorCell ProliferationPharmacologychemistry.chemical_classificationGene knockdownDose-Response Relationship DrugMolecular StructureThiazolothiopyranesOrganic ChemistryGeneral MedicineSquamous carcinomaPPAR gamma030104 developmental biologychemistryCell cultureThiazolidinone030220 oncology & carcinogenesisThiazolidinesDrug Screening Assays AntitumorRosiglitazonemedicine.drugEuropean Journal of Medicinal Chemistry
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Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance.

2020

Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical applicati…

Drug resistanceMicrobial Sensitivity Tests01 natural sciences03 medical and health scienceschemistry.chemical_compoundStructure-Activity RelationshipAntibiotic resistanceDrug DiscoveryStructure–activity relationshipAnimalsHumansThiazole030304 developmental biology0303 health sciencesThiazolidinones Antibiotic resistance BiofilmBenzeneDrug Resistance MicrobialBenzothiazoleAntimicrobialCombinatorial chemistry0104 chemical sciencesAnti-Bacterial Agents010404 medicinal & biomolecular chemistryThiazoleschemistryBiofilmsPerspectiveMolecular MedicineThiazolidinesThiazoleJournal of medicinal chemistry
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