0000000001080705

AUTHOR

Diana Patrizia

showing 3 related works from this author

Pyrano[2,3-e]isoindol-2-ones, new angelicin heteroanalogues

2009

A convenient synthesis of the pyrano[2,3-e]isoindol-2-one ring system, an heteroanalogue of angelicin, is reported. Our synthetic approach consists of the annelation of the pyran ring on the isoindole moiety using 5-dialkylamino- or 5-hydroxymethylene intermediates as building blocks. The photoantiproliferative activity of the new derivatives was studied. Some of them bearing the benzyl group at the 8 position were active with IC(50) in the micromolar range. Cell cytotoxicity involves apoptosis, alteration of cell cycle profile and membrane photodamage.

AnnulationPyrano-isoindolesStereochemistryChemistry PharmaceuticalClinical BiochemistryPharmaceutical ScienceApoptosisIsoindolesRing (chemistry)BiochemistryChemical synthesisInhibitory Concentration 50Jurkat CellsStructure-Activity Relationshipchemistry.chemical_compoundAngelicinCell Line TumorFurocoumarinsDrug DiscoveryHumansMoietyMolecular BiologyPyransMolecular StructurePyrano-isoindoleChemistryPhotochemotherapeutic activityOrganic ChemistryPyrano-isoindoles; Angelicin heteroanalogues; Photochemotherapeutic activity; ApoptosisSettore CHIM/08 - Chimica FarmaceuticaAngelicin heteroanaloguesOxygenModels ChemicalPyranDrug DesignBenzyl groupMolecular MedicineK562 CellsIsoindoleAngelicin heteroanalogueBioorganic & Medicinal Chemistry Letters
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Nobiletin and xanthohumol sensitize colorectal cancer stem cells to standard chemotherapy

2021

Simple Summary Colorectal cancer stem cells (CR-CSCs) play a pivotal role in the therapy resistance and relapse of CRC patients. Herein we demonstrate that new treatment approaches comprising polymethoxyflavones and prenylflavonoids extracted from Citrus sinensis and Humulus lupulus, respectively, hamper the viability of CR-CSCs as well as synergizing with 5-fluorouracil and oxaliplatin (FOX)-based chemotherapy. Extract fractions containing Nobiletin and Xanthohumol, in combination with chemotherapy, decreased stemness properties of CR-CSCs and restrained the outgrowth of chemoresistant metastatic CR-CSCs. These data pinpoint Nobiletin and Xanthohumol as efficacious anti-cancer compounds in…

0301 basic medicinecancer stem cellCancer ResearchAnti-cancer therapyColorectal cancermedicine.medical_treatmentArticleNobiletin03 medical and health sciences0302 clinical medicineCancer stem cellSettore MED/04 - PATOLOGIA GENERALEMedicineflavonoidClonogenic assayRC254-282FlavonoidsChemotherapybusiness.industryCancer stem cellsWnt signaling pathwayXanthohumolNeoplasms. Tumors. Oncology. Including cancer and carcinogensCell cyclemedicine.diseaseColorectal cancerOxaliplatin030104 developmental biologyOncologyflavonoids; nobiletin; xanthohumol; anti-cancer therapy; cancer stem cells; colorectal cancer; natural biofunctional molecules030220 oncology & carcinogenesisCancer researchNatural biofunctional moleculesStem cellbusinessanti-cancer therapy; cancer stem cells; colorectal cancer; flavonoids; natural biofunctional molecules; nobiletin; xanthohumolmedicine.drug
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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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