Search results for " Antitumor activity"

showing 3 items of 33 documents

Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity

2011

Abstract A novel synthetic approach to the synthesis of 3-substituted isoindoles through nucleophilic substitution of 3-halo derivatives by charged carbon, and neutral nitrogen, oxygen, and sulfur nucleophiles, assisted by a 1-acyl group, is reported. Aryl-thio-isoindoles, obtained through a direct nucleophilic substitution with sulfur nucleophiles, showed cytotoxic activity, with GI50 values from micromolar to sub-micromolar concentrations, against the total number of cell lines investigated.

chemistry.chemical_classificationKetoneIsoindolesTertiary amineStereochemistryChemistryIsoindoles Nucleophilic substitutionsColchicine analoguesOrganic ChemistryIsoindoles Nucleophilic substitutions; Antitumor activity; Docking; Colchicine analoguesBiochemistryCombinatorial chemistryChemical synthesisSettore CHIM/08 - Chimica FarmaceuticaDockingchemistry.chemical_compoundIsoindoles Nucleophilic substitutionNucleophileColchicine analogueDrug DiscoveryNucleophilic substitutionAcid hydrolysisIsoindoleAntitumor activity
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In vitro antitumor effects of the cold-water extracts of Mediterranean species of genus Pleurotus (higher Basidiomycetes) on human colon cancer cells

2014

The aim of this study was to evaluate whether the cold-water extracts of Pleurotus eryngii var. ferulae (CWE-Pef) and Pleurotus nebrodensis (CWE-Pn), 2 of the most prized wild and cultivated edible mushrooms, can affect the tumor phenotype of human colon cancer HCT116 cells. Our results showed that treatment with CWE- Pef and CWE-Pn resulted in a significant inhibition of the viability of HCT116 cells and promoted apoptosis, as also demonstrated by the increase of Bax-to-Bcl-2 messenger RNA ratio. Moreover, we observed that both extracts were able to inhibit cell migration and to affect homotypic and heterotypic cell-cell adhesion. It also was found that treatment with CWE-Pef and CWE-Pn ne…

medicinal mushrooms Pleurotus eryngii var. ferulae Pleurotus nebrodensis human colon cancer antitumor activityCell SurvivalApoptosisPleurotusApplied Microbiology and BiotechnologySettore BIO/13 - Biologia ApplicataCell Line TumorVegetablesDrug DiscoveryExtracellularHumansPleurotus eryngiiCell Proliferationbcl-2-Associated X ProteinPharmacologyPleurotus nebrodensisPleurotusbiologyPlant ExtractsKinasebiology.organism_classificationAntineoplastic Agents PhytogenicIn vitroProto-Oncogene Proteins c-bcl-2BiochemistryApoptosisColonic NeoplasmsPhosphorylation
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Structural Manipulations of Marine Natural Products Inspire a New Library of 3-Amino-1,2,4-Triazine PDK Inhibitors Endowed with Antitumor Activity in…

2023

Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types of cancer, characterized by late prognosis and drug resistance. Among the main factors sustaining PDAC progression, the alteration of cell metabolism has emerged to have a key role in PDAC cell proliferation, invasion, and resistance to standard chemotherapeutic agents. Taking into account all these factors and the urgency in evaluating novel options to treat PDAC, in the present work we reported the synthesis of a new series of indolyl-7-azaindolyl triazine compounds inspired by marine bis-indolyl alkaloids. We first assessed the ability of the new triazine compounds to inhibit the enzymatic activity of pyruvate de…

nortopsentin analoguespancreatic ductal adenocarcinoma (PDAC); nortopsentin analogues; antitumor activity; pyruvate dehydrogenase kinases (PDKs); cytotoxic activity; metabolic alterations; ligand-based homology modeling; KRASDrug Discoveryligand-based homology modelingKRASPharmaceutical Scienceantitumor activitymetabolic alterationspancreatic ductal adenocarcinoma (PDAC)Pharmacology Toxicology and Pharmaceutics (miscellaneous)cytotoxic activitypyruvate dehydrogenase kinases (PDKs)
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