Search results for " Cytotoxic activity"

showing 5 items of 15 documents

Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[2E]-3-phenylprop-2-enoylamino}benzamides

2011

Several new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides 12a–s and 17t–v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl)acrylic acid chlorides 11c–k and 11t–v with the appropriate anthranilamide derivatives 10a–c or the 5-iodoanthranilic acid 13. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the mo…

Pyridinesmedicine.drug_classStereochemistryAntineoplastic AgentsCarboxamideChemical synthesisArticlePolymerizationInhibitory Concentration 50Structure-Activity RelationshipTubulinCell Line TumorDrug DiscoverymedicineHumansStructure–activity relationshiportho-AminobenzoatesCytotoxicity2-{[2E]-3-phenylprop-2-enoylamino}benzamides antimitotic agents cytotoxic activityPharmacologyDose-Response Relationship DrugbiologyChemistryTubulin ModulatorsCell CycleOrganic ChemistryGeneral MedicineCell cycleSettore CHIM/08 - Chimica FarmaceuticaTubulin ModulatorsTubulinAcrylatesMechanism of actionBiochemistryBenzamidesbiology.proteinDrug Screening Assays Antitumormedicine.symptom
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Cytotoxic activity of diterpenoids isolated from the aerial parts of Elaeoselinum asclepium subsp. meoides.

2008

The phytochemical investigation of the acetone extract of the aerial parts of Elaeoselinum asclepium (L.) Bertol. subsp. meoides (Desf.) Fiori afforded several known diterpenoids as well as meoidic acid ( 5), new in the literature. The cytotoxic activities of elasclepic acid ( 1), ENT-atis-16-en-19-oic acid ( 2), ent-beyer-15-en-19-oic acid ( 3), ent-kaur-16-en-19-oic acid ( 4) and meoidic acid ( 5) were investigated on rat glioma C6 cells by evaluation of cell growth inhibition.

StereochemistryElaeoselinum asclepium subsp. meoides Umbelliferae diterpenoids meoidic acid cytotoxic activityPharmaceutical ScienceBiologyPharmacognosyAnalytical Chemistrychemistry.chemical_compoundCell Line TumorDrug Discoveryotorhinolaryngologic diseasesAcetoneCytotoxic T cellAnimalsCytotoxicityCell ProliferationPharmacologyMolecular StructureOrganic ChemistrySettore CHIM/06 - Chimica OrganicaElaeoselinum asclepium subsp. meoidesAntineoplastic Agents PhytogenicTerpenoidRatsComplementary and alternative medicinechemistryPhytochemicalMolecular MedicineDiterpeneDiterpenesApiaceaePlanta medica
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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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Synthesis, structural characterization and antitumor activity of di- and tri-organotin(IV) complexes of D-galacturonic acid

2015

organotin(IV) complexes D-Galacturonic acid cytotoxic activitySettore CHIM/03 - Chimica Generale E InorganicaSettore BIO/10 - Biochimica
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Cytotoxic Effect of Eudesmanolides Isolated from Flowers of Tanacetum vulgare ssp. siculum

2012

WOS: 000306752700042

sesquiterpeneeudesmanolidePharmaceutical ScienceFlowersSesquiterpeneArticleChinese hamsterCell LineAnalytical ChemistryHuman lungInhibitory Concentration 50Tanacetumchemistry.chemical_compoundsesquiterpenesDrug DiscoveryBotanymedicineAnimalsHumansCytotoxic T cellSettore BIO/15 - Biologia FarmaceuticaPhysical and Theoretical ChemistryTanacetum vulgarecytotoxic activityCell ProliferationCell DeathbiologyTraditional medicine<em>Tanacetum vulgare</em>; sesquiterpenes; eudesmanolides; cytotoxic activityeudesmanolidesOrganic ChemistrySettore CHIM/06 - Chimica Organicabiology.organism_classificationIn vitroTanacetum vulgare; sesquiterpenes; eudesmanolides; cytotoxic activitymedicine.anatomical_structurechemistryPhytochemicalChemistry (miscellaneous)Molecular MedicineColorimetryFormazanMolecules; Volume 17; Issue 7; Pages: 8186-8195
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