0000000000409199

AUTHOR

Roberta Loddo

showing 2 related works from this author

Pyrrolo[1,2-f]phenanthridines and related non-rigid analogues as antiviral agents.

2002

Abstract The pyrrolo[1,2- f ]phenanthridines 8 – 22 and the corresponding non-rigid analogues 23 – 41 were synthesised and their ability to inhibit the replication of HIV-1 was tested. Only the polycyclic derivatives 10 , 11 , and 13 showed a weak anti -HIV activity, whereas several pyrrolo-phenanthridines ( 8 , 10 , 16 – 18 ) were found to stimulate the multiplication of MT-4 cells at low concentrations. Derivative 10 demonstrated to possess the unique property of stimulating the multiplication of lymphocytes joined to HIV inhibition.

PharmacologyModels MolecularMolecular modelChemistryStereochemistryAnti-HIV AgentsCell SurvivalOrganic ChemistryHuman immunodeficiency virus (HIV)HIV InfectionsGeneral Medicinemedicine.disease_causeChemical synthesisIn vitroVirusCell LinePhenanthridinesStructure-Activity RelationshipDrug DiscoverymedicineHIV-1HumansPyrrolesVolume concentrationEuropean journal of medicinal chemistry
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3-Aryl-2-[1H-benzotriazol-1-yl]acrylonitriles: a novel class of potent tubulin inhibitors.

2011

During a screening for compounds that could act against Mycobacterium tuberculosis, a series of new cellular antiproliferative agents was identified. The most cytotoxic molecules were evaluated against a panel of human cell lines derived from hematological and solid human tumors. In particular, (E)-2-(1H-benzo[d] [1,2,3]triazol-1-yl)-3-(4-methoxyphenyl)acrylonitrile (1) was found to be of a potency comparable to etoposide and greater than 6-mercaptopurine in all cell lines tested. Accordingly, a synthesis of a new series of (E)-2-(5,6-dichloro-1H-benzo[d] [1,2,3]triazol-1-yl)-3-(4-R-phenyl)acrylonitriles was conducted in order to extend the studies of structure-activity relationship (SAR) f…

Models MolecularMagnetic Resonance SpectroscopyMolecular modelStereochemistryAnti-cancer drugsBinding CompetitiveGas Chromatography-Mass SpectrometryAnti-cancer drugchemistry.chemical_compoundStructure-Activity RelationshipTubulinAnti-cancer drugs; drug design and development; computer assisted drug designDrug DiscoveryK562 CellmedicineStructure–activity relationshipHumansdrug design and developmentPharmacologybiologyAcrylonitrileChemistryArylOrganic ChemistryCell Cyclecomputer assisted drug designGeneral MedicineCell cycleTriazolesTubulinPodophyllotoxinCell cultureTubulin Binding Agentbiology.proteinTriazoleColchicineK562 CellsHumanmedicine.drugEuropean journal of medicinal chemistry
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