Search results for "Inhibition of migration"

showing 4 items of 4 documents

Imidazo[2,1-b] [1,3,4]thiadiazoles with antiproliferative activity against primary and gemcitabine-resistant pancreatic cancer cells

2020

A new series of eighteen imidazo [2,1-b] [1,3,4]thiadiazole derivatives was efficiently synthesized and screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. Two out of eighteen derivatives, compounds 12a and 12h, showed remarkably cytotoxic activity with the half maximal inhibitory concentration values (IC50) ranging from 0.23 to 11.4 μM, and 0.29–12.2 μM, respectively. However, two additional compounds, 12b and 13g, displayed remarkable in vitro antiproliferative activity against pancreatic ductal adenocarcinoma (PDAC) cell lines, including immortalized (SUIT-2, Capan-1, Panc-1), primary (PDAC-3) and gemcitabine-resistant (Panc-1R), elici…

Inhibition of migrationAntimetabolites AntineoplasticEpithelial-Mesenchymal Transition3Modulation of EMTPTK2VimentinAntineoplastic AgentsApoptosisThiophenesAntiproliferative activity1-b][1DeoxycytidinePancreatic ductal adenocarcinomaThiadiazolesSDG 3 - Good Health and Well-beingCell MovementPancreatic cancerDrug DiscoveryThiadiazolesmedicineTumor Cells CulturedImidazo[21-b][134]thiadiazole derivativesHumansPTK2/FAKIC50Cell ProliferationImidazo[2Pharmacologybiology4]thiadiazole derivativesChemistryOrganic ChemistryDrug SynergismGeneral Medicinemedicine.diseaseGemcitabinePancreatic NeoplasmsCell cultureDrug Resistance NeoplasmImidazo[21-b][134]thiadiazole derivatives Pancreatic ductal adenocarcinoma Antiproliferative activity Inhibition of migration Spheroids shrinkage Modulation of EMT PTK2/FAKbiology.proteinCancer research/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_beingPhosphorylationSpheroids shrinkageTyrosine kinaseCarcinoma Pancreatic DuctalEuropean Journal of Medicinal Chemistry
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1,2,4-Oxadiazole Topsentin Analogs with Antiproliferative Activity against Pancreatic Cancer Cells, Targeting GSK3β Kinase.

2021

A new series of topsentin analogs, in which the central imidazole ring of the natural lead was replaced by a 1,2,4- oxadiazole moiety, was efficiently synthesized. All derivatives were pre-screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. The five most potent compounds were further investigated in various pancreatic ductal adenocarcinoma (PDAC) cell lines, including SUIT-2, Capan-1, and Panc-1 cells, eliciting EC50 values in the micromolar and sub-micromolar range, associated with significant reduction of cell migration. These remarkable results might be explained by the effects of these new topsentin analogues on epithelial-to-mesenchy…

Models MolecularIndoles124-oxadiazole topsentin analogs; GSK3β kinase; inhibition of migration; PDAC antiproliferative activity; proapoptotic activityApoptosisDrug Screening Assays01 natural sciencesBiochemistrychemistry.chemical_compound124-oxadiazole topsentin analogs; GSK3β kinase; PDAC antiproliferative activity; inhibition of migration; proapoptotic activity; Antineoplastic Agents; Apoptosis; Cell Proliferation; Cell Survival; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Glycogen Synthase Kinase 3 beta; Humans; Imidazoles; Indoles; Models Molecular; Molecular Structure; Oxadiazoles; Pancreatic Neoplasms; Protein Kinase Inhibitors; Structure-Activity Relationship; Tumor Cells CulturedModelsAnnexinDrug DiscoveryTumor Cells CulturedGSK3β kinaseGeneral Pharmacology Toxicology and Pharmaceutics4-oxadiazole topsentin analogsOxadiazolesCulturedMolecular StructureChemistryKinaseImidazolesCell migrationTumor Cellsinhibition of migrationMolecular MedicineDrugIntracellularPDAC antiproliferative activityproapoptotic activityCell Survival12Antineoplastic AgentsDose-Response RelationshipStructure-Activity RelationshipPancreatic cancermedicineHumansPropidium iodideProtein Kinase InhibitorsCell ProliferationPharmacologyGlycogen Synthase Kinase 3 betaDose-Response Relationship Drug010405 organic chemistryOrganic ChemistryMolecularAntitumormedicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaMolecular biology0104 chemical sciencesPancreatic Neoplasms010404 medicinal & biomolecular chemistryApoptosisCell cultureDrug Screening Assays Antitumor124-oxadiazole topsentin analogChemMedChem
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Development of natural and synthetic compounds as kinase inhibitors targeting cancer cells and cancer stem cells

2023

Pancreatic ductal adenocarcinomaInhibition of migrationantibiotic resistanceImidazo[21-b][134]thiadiazole derivativeskinase inhibitorsanti-biofilm agentsAntiproliferative activityFAK inhibitionSettore CHIM/08 - Chimica Farmaceutica
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Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole derivatives: as anticancer and antibiofilm agents, and preclinical invest…

2020

antiproliferative activityStaphylococcal biofilm inhibitorhypoxiaAnti-virulence agentpancreatic ductal adenocarcinomachemoresistancemodulation of EMTlactate dehydrogenaseproton-coupled folate transporterspheroids shrinkageSettore CHIM/08 - Chimica Farmaceuticamalignant pleural and peritoneal mesotheliomaanti-biofilm agentimidazo[21-b][134]thiadiazole derivativeinhibition of migrationPTK2/FAKxenograftpemetrexedprognosi
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