Search results for "HCT116"

showing 4 items of 54 documents

Synthesis of 5H-pyrido[3,2-b]pyrrolizin-5-one tripentone analogs with antitumor activity

2018

Abstract Pyrrolizinones represent an interesting class of compounds with varied degrees of structural complexity and pharmacological activity. Among these, 9H-pyrido[2,3-b]pyrrolizin-9-one, tripentone analogs, recently reported by us, showed significant antiproliferative activity against human tumor cell lines, inducing apoptosis and not affecting viability of Caco-2 differentiated in normal intestinal-like cells. Considering their interesting biological activity, their 5H-pyrido[3,2-b]pyrrolizin-5-one analogs were efficiently synthesized in good to excellent yields (61–91%). All tripentone derivatives were tested to assess their cytotoxicity against two human tumor cell lines, HCT-116 (hum…

TripentonesPyridinesAntineoplastic AgentsApoptosisAntiproliferative activity5H-pyrido[3; 2-b]pyrrolizin-5-ones; Antiproliferative activity; Antitumor; Apoptosis; Tripentones; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry010402 general chemistry01 natural sciencesStructure-Activity Relationship2-b]pyrrolizin-5-onesCell Line TumorNeoplasmsDrug DiscoverymedicineHumansCytotoxic T cellPyrrolesCytotoxicityMitosisIC505H-pyrido[32-b]pyrrolizin-5-onePharmacology010405 organic chemistryChemistryDrug Discovery3003 Pharmaceutical ScienceOrganic Chemistry5H-pyrido[3ApoptosiTripentoneCancerBiological activityAntitumorGeneral MedicineHCT116 Cellsmedicine.disease0104 chemical sciencesCell cultureApoptosisMCF-7 CellsCancer researchCaco-2 CellsDrug Screening Assays AntitumorEuropean Journal of Medicinal Chemistry
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New 1,2,4-oxadiazole nortopsentin derivatives with cytotoxic activity

2019

New analogs of nortopsentin, a natural 2,4-bis(3&prime

anti-cancer agentCell SurvivalAnti-cancer agentsPharmaceutical ScienceAntineoplastic AgentsAntiproliferative activity01 natural sciencesArticlechemistry.chemical_compoundStructure-Activity RelationshipMarine alkaloidsSettore BIO/10 - BiochimicaDrug DiscoveryMoietyHumansPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Cell ProliferationIndole testMolecular Structure010405 organic chemistryAcridine orangeImidazoles2 4-oxadiazole derivativesnortopsentin analogs2 4-oxadiazole derivatives; Anti-cancer agents; Antiproliferative activity; Marine alkaloids; Nortopsentin analogs 1; Antineoplastic Agents; Caco-2 Cells; Cell Cycle Checkpoints; Cell Proliferation; Cell Survival; HCT116 Cells; Humans; Imidazoles; MCF-7 Cells; Molecular Structure; Structure-Activity RelationshipPhosphatidylserineCell Cycle CheckpointsNortopsentin analogs 1HCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciences124-oxadiazole derivative010404 medicinal & biomolecular chemistrychemistryBiochemistry124-oxadiazole derivativeslcsh:Biology (General)ApoptosisCell cultureCancer cellMCF-7 CellsMarine alkaloid2 4-oxadiazole derivativeCaco-2 CellsEthidium bromide
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Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

2016

New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S ph…

antiproliferative activitybis-indolyl alkaloidsIndolesStereochemistryPopulationPharmaceutical ScienceAntineoplastic AgentsAntiproliferative activity; Apoptosis; Bis-indolyl alkaloids; Marine alkaloids; Thiazolyl-indolesBis-indolyl alkaloid010402 general chemistry01 natural sciencesArticlechemistry.chemical_compoundCell Line TumorDrug DiscoveryHumansCytotoxic T cellThiazolyl-indoleThiazoleMode of actioneducationlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Antitumor activityIndole testeducation.field_of_study010405 organic chemistryChemistryCell CycleImidazolesapoptosisApoptosiHCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesThiazoleslcsh:Biology (General)BiochemistryApoptosisCell cultureMCF-7 Cellsmarine alkaloidsMarine alkaloidthiazolyl-indolesDrug Screening Assays Antitumormarine alkaloids; bis-indolyl alkaloids; thiazolyl-indoles; apoptosis; antiproliferative activityMarine Drugs
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EGF-Induced Acetylation of Heterogeneous Nuclear Ribonucleoproteins Is Dependent on KRAS Mutational Status in Colorectal Cancer Cells.

2015

KRAS mutational status is considered a negative predictive marker of the response to anti-EGFR therapies in colorectal cancer (CRC) patients. However, conflicting data exist regarding the variable response to EGFR-targeted therapy. The effects of oncogenic KRAS on downstream targets were studied in cell lines with different KRAS mutations. Cells harboring a single KRASG13D allele showed the most tumorigenic profile, with constitutive activation of the downstream pathway, rendering them EGF-unresponsive. Conversely, KRASA146T cells showed a full EGF-response in terms of signal transduction pathways, cell proliferation, migration or adhesion. Moreover, the global acetylome of CRC cells was al…

lcsh:MedicineBiologymedicine.disease_causeHeterogeneous-Nuclear RibonucleoproteinsProto-Oncogene Proteins p21(ras)Epidermal growth factorCell Line TumormedicineHumansCell adhesionlcsh:ScienceMutationMultidisciplinaryEpidermal Growth FactorCell growthlcsh:RAcetylationCell migrationHCT116 CellsGene Expression Regulation NeoplasticDrug Resistance NeoplasmAcetylationMutationCancer researchlcsh:QKRASSignal transductionColorectal NeoplasmsResearch ArticleSignal TransductionPLoS ONE
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