Search results for "QUINAZOLINONE"

showing 7 items of 17 documents

SYNTHESIS AND BIOLOGICAL EVALUATION OF 2-PHENYL-3-[INDAZOL-3-YL]-4(3H)-QUINAZOLINONES

2008

Settore CHIM/08 - Chimica FarmaceuticaQUINAZOLINONE
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Electronic ionization mass spectra of 3-(5'-(3'-methylisoxazol))- and 3-(3'-(5'-methylisoxazol)-2-styryl-4(3H)quinazolinones of pharmaceutical intere…

2008

Settore CHIM/08 - Chimica Farmaceuticaisomeric styrylisoxazolylquinazolinones/Electronic ionization mass spectra
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Darstellung, Kristallstruktur und Wirkung von 2-Methyl-3-(4-oxo-3-phenyl-thiazolidin-2-ylidenamino)-4-(3H)-chinazolinon

1984

Quinazolinones. 1. Preparation, crystal structure and action of 2-methyl-3-(4-oxo-3-phenyl-thiazolidine-2-ylidenamino)-4-(3H)- quinazolinone.

chemistry.chemical_compoundchemistryBicyclic moleculeStereochemistryDrug DiscoveryX-ray crystallographyLactamPharmaceutical ScienceMoleculeBiological activityCrystal structureQuinazolinoneArchiv der Pharmazie
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ChemInform Abstract: Synthesis of New 3-(3-Phenyl-isoxazol-5-yl) or 3-[(3-Phenyl-isoxazol-5-yl)amino] Substituted 4(3H)-Quinazolinone Derivatives wit…

2010

A novel series of 3-(3-phenyl-isoxazol-5-yl) or 3-[(3-phenyl-isoxazol-5-yl)amino] substituted 4(3H)-quinazolinone derivatives was synthesized. The compounds were tested for their antineoplastic activity in vitro against Raji (human Burkitt limphoma). K-562 (human chronic myelogeneous leukemia) and U937 (human histiocytic limphoma) cell lines. The most active quinazolinones showed IC50 values in the range 16-30 microM.

chemistry.chemical_compoundchemistryCell cultureStereochemistryIc50 valuesGeneral MedicineQuinazolinoneIn vitroChemInform
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An evaluation of RVX-208 for the treatment of atherosclerosis

2015

Introduction: RVX-208 is a first-in-class, orally active, novel small molecule in development by Resverlogix Corporation (Calgary, AB, Canada). It acts through an epigenetic mechanism by inhibiting the bromodomain and extraterminal (BET) family of proteins, increasing apolipoprotein A-I (apoA-I) and targeting high-density lipoprotein (HDL) metabolism, including generating of nascent HDL and increased larger HDL particles, resulting in the stimulation of reverse cholesterol transport. RVX-208 also has a beneficial effect on inflammatory factors known to be involved in atherosclerosis and plaque stability. New therapeutic strategies are needed for patients with atherosclerosis.Areas covered: …

medicine.medical_specialtyApolipoprotein Bapolipoprotein A-IRVX 208high-density lipoproteinPharmacologyEpigenesis Geneticchemistry.chemical_compoundatherosclerosiHigh-density lipoproteinMetabolic DiseasesInternal medicinemedicineAnimalsHumansPharmacology (medical)QuinazolinonesPharmacologybiologyAnimalCholesterolMedicine (all)Cholesterol HDLReverse cholesterol transportRVX-208QuinazolineGeneral MedicineAtherosclerosisPlaque AtheroscleroticMetabolic DiseaseBromodomainOrally activeEndocrinologyhigh-density lipoprotein particlechemistryQuinazolinesbiology.proteinlipids (amino acids peptides and proteins)HumanLipoproteinExpert Opinion on Investigational Drugs
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Diacylglycerol kinase α mediatses 17-β-estradiol-induced proliferation, motility, and anchorage-independent growth of Hec-1A endometrial cancer cell …

2011

Increased levels of endogenous and/or exogenous estrogens are one of the well known risk factors of endometrial cancer. Diacylglycerol kinases (DGKs) are a family of enzymes which phosphorylate diacylglycerol (DAG) to produce phosphatidic acid (PA), thus turning off and on DAG-mediated and PA-mediated signaling pathways, respectively. DGK α activity is stimulated by growth factors and oncogenes and is required for chemotactic, proliferative, and angiogenic signaling in vitro. Herein, using either specific siRNAs or the pharmacological inhibitor R59949, we demonstrate that DGK α activity is required for 17-β-estradiol (E2)-induced proliferation, motility, and anchorage-independent growth of …

medicine.medical_specialtyGPR30medicine.drug_classCell SurvivalDiacylglycerol kinaseMotilityEstrogen receptorEnzyme AssayEndometrial carcinomaBiologyQuinazolinoneReceptors G-Protein-CoupledPiperidinePiperidinesCell MovementInternal medicineCell Line TumormedicineCell AdhesionHumansEndometrial NeoplasmEnzyme AssaysQuinazolinonesDiacylglycerol kinaseCell ProliferationEstradiolCell growthKinaseCell BiologyDiacylglycerol kinase; Endometrial carcinoma; Estrogen; GPR30; Cell BiologyEstrogenEndometrial NeoplasmsCell biologyEnzyme ActivationLipoprotein LipaseEndocrinologyReceptors EstrogenEstrogenGene Knockdown TechniquesGene Knockdown TechniqueFemaleRNA InterferenceSignal transductionGPERHuman
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1,2,4-OSSADIAZOLI: UTILI SCAFFOLD NEL DESIGN DI NUOVI FARMACI

2021

quinazolinone(di)-acylguanidineneuroprotective agentreduction124-Oxadiazoleantidiabetic agentSARS-CoV2 proteaseSettore CHIM/06 - Chimica Organica
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