0000000000390424

AUTHOR

Ornella Gia

showing 3 related works from this author

Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

2007

A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the re…

Cell typeIndolescyclizationHL60StereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsThiophenesBiochemistryChemical synthesisInhibitory Concentration 50chemistry.chemical_compoundAlkaloids5-bis(3'-indolyl)thiophenesCell Line TumorDrug DiscoverymedicineAnimalsHumansantitumor activityMolecular BiologyCell Proliferationbis-indolylthiopheneCell growthNortopsentinMelanomaOrganic ChemistryImidazolesCancerBiological activityDNAmedicine.diseasediketonesTopoisomerase II5-bis(3'-indolyl)thiophenes; antitumor activity; Topoisomerase II; NortopsentinDNA Topoisomerases Type IIchemistryCell cultureMolecular Medicine
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Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d[pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2

2015

Vascular Endothelial Growth Factor (VEGF) pathway has emerged as one of the most important positive modulators of Angiogenesis, a central process implicated in tumour growth and metastatic dissemination. This led to the design and development of anti-VEGF monoclonal antibodies and small-molecule ATP-competitive VEGFR-inhibitors. In this study, we describe the synthesis and the biological evaluation of novel 2-aryl substituted benzothiopyrano-fused pyrimidines 1a-i, 2a-i and 3a-i. The ability of the compounds to target the VEGF pathway was determined in vitro exploiting the compounds' antiproliferative efficacy against HUVEC cells. The VEGFR-2 inhibition was confirmed by enzymatic assays on …

Models MolecularAngiogenesisReceptor tyrosine kinaseCellAntineoplastic AgentsReceptor tyrosine kinaseBenzothiopyranopirimidines; Kinase inhibitors; Receptor tyrosine kinases; Tumor angiogenesis; VEGFR;Tumor angiogenesisStructure-Activity Relationshipchemistry.chemical_compoundVEGFRBenzothiopyranopirimidineCell Line TumorReceptor tyrosine kinasesDrug DiscoveryHuman Umbilical Vein Endothelial CellsmedicineHumansProtein Kinase InhibitorsCell ProliferationPyransTumor angiogenesiPharmacologyKinase inhibitorDose-Response Relationship DrugMolecular StructurebiologyKinaseCell growthOrganic ChemistryKinase insert domain receptorGeneral MedicineVascular Endothelial Growth Factor Receptor-2Molecular biologyVascular endothelial growth factorPyrimidinesmedicine.anatomical_structureBenzothiopyranopirimidineschemistryBenzothiopyranopirimidines; Kinase inhibitors; Receptor tyrosine kinases; Tumor angiogenesis; VEGFRKinase inhibitorsCancer researchbiology.proteinDrug Screening Assays AntitumorEx vivo
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3,5-bis(3'-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: synthesis and antitumor properties.

2007

A series of 10 bis-indolylpyrazoles of type 9, 10 were obtained by cyclization of diketones 8 using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Derivatives 9a,c,d were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, 9d, the most active compound was effective against all the tested cell lines with a GI(50) mean value of 3.23 microM; TGI and LC(50) values were 14.5 and 58.9 microM having positive response on 91% and 41% of the tested cell lines, respectively.

MethylhydrazineIndolesStereochemistry3Clinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBiochemistryChemical synthesisNortopsentin; 3; 5-Bis(3'-indolyl)pyrazoles; antitumor activity; Topoisomerase IIAcetic acidchemistry.chemical_compoundAlkaloidsCell Line TumorDrug DiscoveryHumansantitumor activityMolecular BiologyCell Proliferationchemistry.chemical_classificationCell growthAlkaloidNortopsentinOrganic ChemistryImidazolesBiological activity5-Bis(3'-indolyl)pyrazolesTopoisomerase IIEnzymechemistryCell cultureMolecular MedicinePyrazolesDrug Screening Assays AntitumorBioorganicmedicinal chemistry letters
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