Search results for "germacranolide"

showing 10 items of 17 documents

Structure-Activity Relationships of Cytotoxic Lactones as Inhibitors and Mechanisms of Action.

2020

Background: Some lactones prevent protein Myb-dependent gene expression. Objective: The object is to calculate inhibitors of Myb-brought genetic manifestation. Methods: Linear quantitative structure–potency relations result expanded, among sesquiterpene lactones of a variety of macrocycles (pseudoguaianolides, guaianolides, eudesmanolides and germacranolides), to establish which part of the molecule constitutes their pharmacophore, and predict their inhibitory potency on Myb-reliant genetic manifestation, which may result helpful as leads for antileukaemic therapies with a new mechanism of action. Results: Several count indices are connected with structure–activity. The α-methylene-γ-lacto…

0301 basic medicineGermacranolidePaclitaxelStereochemistrySesquiterpeneRing (chemistry)Ligands030226 pharmacology & pharmacy03 medical and health scienceschemistry.chemical_compoundLactonesStructure-Activity Relationship0302 clinical medicineTubulinNeoplasmsDrug DiscoverymedicinePotencyMoleculeHumansEtoposidechemistry.chemical_classification030102 biochemistry & molecular biologyAntineoplastic Agents PhytogenicTubulin ModulatorsMolecular Docking SimulationMechanism of actionchemistryStructural Homology ProteinDrug DesignPharmacophoremedicine.symptomTopotecanSesquiterpenesLactoneCurrent drug discovery technologies
researchProduct

Germacranolides and a monoterpene cyclic peroxide from Artemisia fragrans

1998

Abstract The aerial parts of Artemisia fragrans collected in Armenia yielded a new cyclic monoterpene peroxide with the irregular santolinyl framework, together with several known germacranolides. Comparison with previously published chemical results suggests these may actually have been performed on a different, although closely related species.

GermacranolideCyclic compoundbiologyChemistryStereochemistryMonoterpenePlant ScienceGeneral MedicineHorticulturebiology.organism_classificationBiochemistryArtemisia fragransPeroxidechemistry.chemical_compoundAnthemideaeOrganic chemistryMolecular BiologyPhytochemistry
researchProduct

Influence of conformational factors on acid-catalyzed cyclizations of germacranolides: Molecular structure of the cyclization products of gallicin an…

1995

Acid-catalyzed cyclization of the natural germacranolide gallicin (8) yielded, among other products, the 1,4-epoxyeudes-manolide 9, which has a trans-fused decaline system. Under the same conditions the closely related germacranolide shonachalin A (8α-hydroxygallicin) (3) cyclized to the eudesmanolide 4 with a cis fused decaline system. The structures of these cyclization products were secured by means of chemical correlations and X-ray diffraction analyses.

GermacranolideStereochemistryChemistryAcid catalyzedOrganic ChemistryMoleculeOrganic chemistryGeneral ChemistryPhysical and Theoretical ChemistryLiebigs Annalen
researchProduct

Lipase-catalysed preparation of acyl derivatives of the germacranolide cnicin

2009

Several acyl derivatives of cnicin were obtained through lipase-catalysed acylation and alcoholysis reactions. In most reactions lipases showed a regioselective behaviour affording only one product. Longer chain acyl derivatives were prepared at lower temperature than the used in lipase-catalysed reactions, to preclude side products formation. The enzymatic approach let to prepare a family of novel acetyl and fatty acid derivatives of cnicin which are not obtainable following traditional organic synthetic procedures. Fil: Monsalve, Leandro Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis…

GermacranolideTriacylglycerol lipaseBioengineeringBiochemistryCnicinCatalysisEnzyme catalysisAcylationchemistry.chemical_compoundOrganic chemistryLipasechemistry.chemical_classificationbiologyENZYME CATALYSISChemistryProcess Chemistry and TechnologyCiencias QuímicasRegioselectivityALCOHOLYSISCNICINACYLATIONSESQUITERPENOIDSEnzymeQuímica Orgánicabiology.proteinCIENCIAS NATURALES Y EXACTAS
researchProduct

Sesquiterpene lactones from Picris echioides

1992

Abstract The aerial parts of Picris echioides yielded the new germacranolide 3β-hydroxybalchanolide and the known guaianolides hieracin I, hieracin II, 8-deoxylactucin, jacquilenin and 11 -epijacquilenin.

Germacranolidechemistry.chemical_classificationStereochemistryPlant ScienceGeneral MedicineHorticulturePicris echioidesSesquiterpeneBiochemistrychemistry.chemical_compoundchemistryOrganic chemistryMolecular BiologyLactonePhytochemistry
researchProduct

Sesquiterpene lactones from Artemisia species

1993

Abstract The aerial parts of Artemisia spicigera yielded two new eudesmanolides as well as three known ones. The aerial parts of Artemisia verlotiorum yielded four known germacranolides and two known eudesmanolides.

Germacranolidechemistry.chemical_classificationbiologyArtemisia spicigeraArtemisia verlotiorumPlant ScienceGeneral MedicineHorticulturebiology.organism_classificationSesquiterpeneBiochemistrychemistry.chemical_compoundchemistryBotanyArtemisiaMolecular BiologyLactonePhytochemistry
researchProduct

Sesquiterpene lactones from Artemisia herba-alba

1990

Abstract The aerial parts of Artemisia herba-alba subsp. valentine yielded, in addition to known compounds, a new germacranolide, six new eudesmanolides and ilicic acid methyl ester.

Germacranolidechemistry.chemical_classificationbiologyChemistryArtemisia herba-albafood and beveragesPlant ScienceGeneral MedicineHorticulturebiology.organism_classificationSesquiterpeneBiochemistryTerpenoidchemistry.chemical_compoundAnthemideaeBotanyArtemisiaMedicinal plantsMolecular BiologyLactonePhytochemistry
researchProduct

Sesquiterpene lactones and lignans from Centaurea species

1992

Abstract The aerial parts of Centaurea calcitrapa yielded cnicin, cnicin 4′-acetate, melitensin, a related elemanolide, the two new germacranolides 11α,13- and 11β,13-dihydrosalonitenolide, and the lignans arctigenin, pinoresinol and 7′( S )-hydroxyarctigenin. The latter compound is described for the first time as a natural product. The aerial parts of Centaurea pabotii yielded 11,13-dihydrodeacylcynaropicrin, aguerin A and a new guaianolide related to cynaropicrin.

LignanGermacranolideStereochemistryPlant ScienceGeneral MedicineHorticultureBiologybiology.organism_classificationBiochemistryCnicinCynaropicrinchemistry.chemical_compoundCentaurea calcitrapachemistryPinoresinolCentaureaOrganic chemistryMolecular BiologyCynareaePhytochemistry
researchProduct

Acid rearrangment of epoxy-germacranolides and absolute configuration of 1beta, 10alpha-epoxy-salonitenolide

2010

The acid-catalyzed cyclization of mono epoxides of cnicin acetonide (3) was investigated. Several 6,12-eudesmanolides were obtained, and their stereochemistry established by extensive spectroscopic analyses. Chemical correlations also led to the assignment of the absolute configuration of 1beta,10alpha-epoxy-salonitenolide (13), a previously isolated natural product. The cytotoxic activities of some compounds were determined against A549 and MCF-7 tumor cell lines. The esterified germacranolides 2-6 were selectively cytotoxic against the MCF-7 breast cancer cell line.

Magnetic Resonance SpectroscopyMolecular StructurePlant ExtractsCentaureaSettore CHIM/06 - Chimica Organicagermacranolides epoxygermacranolides cyclization eudesmanolides absolute configuration cytotoxicityAntineoplastic Agents PhytogenicSesquiterpenes GermacraneCell Line TumorHumansDrug Screening Assays AntitumorSesquiterpenesSicilyCell Proliferation
researchProduct

Sesquiterpene lactones from Artemisia lucentica

1997

Abstract The aerial parts of Artemisia lucentica yielded, in addition to several known compounds, a bicyclic monoterpene ketone, two germacranolides, an eudesmanolide, a 10- epi neudesmanolide, a 2-norelemanolide and three bisabolene derivatives. The stereochemistry of a germacranolide, described as 2α-hydroxyartemorin in a previous investigation of the species, has now been corrected and the compound has been renamed lucentolide.

chemistry.chemical_classificationGermacranolideKetoneBicyclic moleculebiologyChemistryStereochemistryMonoterpenePlant ScienceGeneral MedicineHorticultureSesquiterpenebiology.organism_classificationBiochemistrychemistry.chemical_compoundOrganic chemistryArtemisiaBisaboleneMolecular BiologyLactonePhytochemistry
researchProduct