Search results for "Derivative"

showing 10 items of 1074 documents

Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole derivatives: as anticancer and antibiofilm agents, and preclinical invest…

2020

antiproliferative activityStaphylococcal biofilm inhibitorhypoxiaAnti-virulence agentpancreatic ductal adenocarcinomachemoresistancemodulation of EMTlactate dehydrogenaseproton-coupled folate transporterspheroids shrinkageSettore CHIM/08 - Chimica Farmaceuticamalignant pleural and peritoneal mesotheliomaanti-biofilm agentimidazo[21-b][134]thiadiazole derivativeinhibition of migrationPTK2/FAKxenograftpemetrexedprognosi
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3-(6-Phenylimidazo [2,1-

2019

A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increa…

antiproliferative activitymigration assayIndolesimidazo[21-b][134]thiadiazole derivativespancreatic cancerAntineoplastic AgentsAdenocarcinomaindole compoundsArticlePancreatic NeoplasmsresistanceStructure-Activity RelationshipTumor Cells CulturedHumansDrug Screening Assays AntitumorCarcinoma Pancreatic DuctalCell ProliferationMolecules (Basel, Switzerland)
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Xanthones and sesquiterpene derivatives from a marine-derived fungus Scopulariopsis sp.

2016

Abstract Two new xanthone derivatives, 12-dimethoxypinselin ( 1 ) and 12- O -acetyl-AGI-B4 ( 2 ), as well as two new phenolic bisabolane-type sesquiterpenes, 11,12-dihydroxysydonic acid ( 15 ) and 1-hydroxyboivinianic acid ( 16 ), together with one new alkaloid, scopulamide ( 21 ) and one new α-pyrone derivative, scopupyrone ( 26 ), in addition to twenty-three known compounds ( 3 – 14 , 17 – 20 , 22 – 25 , 27 – 29 ) were isolated from solid rice cultures of the marine-derived fungus Scopulariopsis sp. obtained from the Red Sea hard coral Stylophora sp. All compounds were unambiguously identified through extensive NMR spectroscopic analyses, and by comparison with the literature. Marfey's re…

biology010405 organic chemistryChemistryStereochemistryMouse LymphomaAlkaloidOrganic ChemistryAbsolute configurationFungusbiology.organism_classificationSesquiterpene01 natural sciencesBiochemistry0104 chemical sciencesXanthone Derivatives010404 medicinal & biomolecular chemistrychemistry.chemical_compoundTermészettudományokDrug DiscoveryXanthoneScopulariopsisKémiai tudományokTetrahedron
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Secondary metabolites of the lichen-associated fungus Apiospora montagnei

2017

Abstract The endolichenic fungus Apiospora montagnei isolated from the lichen Cladonia sp. was cultured on solid rice medium, yielding the new diterpenoid libertellenone L (1), the new pyridine alkaloid, 23-O-acetyl-N-hydroxyapiosporamide (2) and the new xanthone derivative 8-hydroxy-3-hydroxymethyl-9-oxo-9H-xanthene-1-carboxylic acid methyl ether (3) together with 19 known compounds (4–22). The structures of the new compounds were elucidated by 1D and 2D NMR spectra as well as by HRESIMS data. The absolute configuration of the new 6,7-seco-libertellenone derivative 1 was determined by single-crystal X-ray diffraction. Four additional known compounds 23–26 were isolated when NaCl or NH4Cl w…

biology010405 organic chemistryStereochemistryAlkaloidOrganic ChemistryAbsolute configurationEtherbiology.organism_classification01 natural sciencesBiochemistryTerpenoid0104 chemical sciences010404 medicinal & biomolecular chemistrychemistry.chemical_compoundchemistryDrug DiscoveryXanthoneOrganic chemistryApiosporaTwo-dimensional nuclear magnetic resonance spectroscopyDerivative (chemistry)Tetrahedron Letters
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Chemical constituents from Anthocleista liebrechtsiana De Wild & T. Durand (Loganiaceae)

2018

Abstract A new steroid derivative, (24S)-3β-hydroxy-7β-methoxyergost-5-ene (1), was isolated along with eleven known compounds: 7α-hydroxysterol (2), β-sitosterol (3), oleanolic acid (4), betulinic acid (5), lupeol (6), swertiaperennin (7), decussatin (8), tetracosanoic acid (9) β-sitosterol-3-O-β- d -glucopyranoside (10), (2R,3S)-2,3-dihydro-2-(3,4-dimethoxyphenyl)-3-hydroxymethyl-5-(2-formylvinyl)-7-hydroxybenzofuran (11) and acacetin 6-C-β- d -glucopyranoside (12) from the tree bark and leaves of Anthocleista liebrechtsiana De Wild & T. Durand. Their structures were elucidated on the basis of spectroscopic (1D and 2D NMR) and mass spectrometric data. Compounds 2 and 7–10 have already bee…

biologyAcacetin010405 organic chemistryStereochemistryAnthocleistaLoganiaceaebiology.organism_classificationAntimicrobial01 natural sciencesBiochemistry0104 chemical sciences010404 medicinal & biomolecular chemistrychemistry.chemical_compoundchemistryBetulinic acidOleanolic acidEcology Evolution Behavior and SystematicsDerivative (chemistry)LupeolBiochemical Systematics and Ecology
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ChemInform Abstract: Non-Steroidal Antiinflammatory Agents. Part 23. Synthesis and Pharmacological Activity of Enaminones which Inhibit Both Bovine C…

2010

biologyChemistryArachidonate 5-lipoxygenasebiology.proteinBiological activityGeneral MedicineCyclooxygenasePharmacologyPyrrole derivativesNon steroidalChemInform
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A germacrane derivative from Pallenis spinosa

1991

Abstract Extraction of aerial parts of Pallenis spinosa and chromatographic separation have yielded a new germacrane derivative and the known sesquiterpenes shiromool and α-cadinol.

biologyChemistryExtraction (chemistry)Pallenis spinosaPlant ScienceGeneral MedicineHorticulturebiology.organism_classificationSesquiterpeneBiochemistryChromatographic separationchemistry.chemical_compoundInuleaeMoleculeOrganic chemistryMolecular BiologyDerivative (chemistry)Phytochemistry
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Induction of cryptic metabolites of the endophytic fungus Trichocladium sp. through OSMAC and co-cultivation

2019

The endophytic fungus Trichocladium sp. isolated from roots of Houttuynia cordata was cultured on solid rice medium, yielding a new amidepsine derivative (1) and a new reduced spiro azaphilone derivative (3) together with eight known compounds (4–11). Co-cultivation of Trichocladium sp. with Bacillus subtilis resulted in induction of a further new compound (2) and a 10-fold increase of 11 compared to the axenic fungal culture. Moreover, when the fungus was cultivated on peas instead of rice, a new sesquiterpene derivative (13) and two known compounds (12 and 14) were obtained. Addition of 2% tryptophan to rice medium led to the isolation of a new bismacrolactone (15). The structures of the …

biologyStereochemistryGeneral Chemical EngineeringTryptophan02 engineering and technologyGeneral ChemistryFungusBacillus subtilis010402 general chemistry021001 nanoscience & nanotechnologybiology.organism_classificationSesquiterpene01 natural sciences0104 chemical sciencesHouttuynia cordatachemistry.chemical_compoundchemistryCell culture0210 nano-technologyAxenicDerivative (chemistry)RSC Advances
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Polyketides and nitrogenous metabolites from the endophytic fungus Phomopsis sp. D15a2a

2019

Abstract Three new polyketides, phomopones A−C (1–3), one new cyclic tetrapeptide, 18-hydroxydihydrotentoxin (4), and a new amide, 6-hydroxyenamidin (5) together with a known derivative, enamindin (6) were obtained from the endophytic fungus Phomopsis sp. D15a2a isolated from the plant Alternanthera bettzickiana. The structures of the new compounds were elucidated by 1D, 2D NMR and HRMS data. The absolute configurations of the isolated metabolites were determined either by X-ray crystallography, Marfey’s method or by converting the compounds to Mosher esters.

biologyTetrapeptide010405 organic chemistryStereochemistryOrganic ChemistryEndophytic fungus010402 general chemistrybiology.organism_classification01 natural sciencesBiochemistry0104 chemical scienceschemistry.chemical_compoundchemistryAmideDrug DiscoveryPhomopsis sp.Alternanthera bettzickianaTwo-dimensional nuclear magnetic resonance spectroscopyDerivative (chemistry)Tetrahedron Letters
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Cytotoxic alkaloids from the root of Zanthoxylum paracanthum (mildbr) Kokwaro

2021

Chemical investigation of the root of Zanthoxylum paracanthum afforded 1 new alkamide derivative, (2E,4E)-6-oxo-N-isobutyldeca-2,4-dienamide (1) together with 10 known congeners including one pheno...

biologyTraditional medicine010405 organic chemistryOrganic ChemistryPlant Sciencebiology.organism_classification01 natural sciencesBiochemistry0104 chemical sciencesAnalytical Chemistry010404 medicinal & biomolecular chemistrychemistry.chemical_compoundRutaceaeZanthoxylumchemistryCytotoxic T cellCytotoxicityDerivative (chemistry)Natural Product Research
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