Search results for "Fluoropyrimidine"

showing 10 items of 10 documents

Efficacy of trifluridine and tipiracil (TAS-102) versus placebo, with supportive care, in a randomized, controlled trial of patients with metastatic …

2016

[Purpose] TAS-102 is a combination of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil. Efficacy and safety of TAS-102 in patients with metastatic colorectal cancer (mCRC) refractory or intolerant to standard therapies were evaluated in the phase 3 RECOURSE trial. Results of RECOURSE demonstrated significant improvement in overall survival (OS) and progression-free survival (PFS) with TAS-102 versus placebo [hazard ratio (HR) = 0.68 and 0.48 for OS and PFS, respectively; both P < 0.001]. The current analysis evaluates efficacy and safety of TAS-102 in the RECOURSE Spanish subgroup.

Male0301 basic medicineOncologyCancer ResearchPyrrolidinesColorectal cancerTrifluridineHelsinki declarationlaw.inventionTrifluridinechemistry.chemical_compound0302 clinical medicineRandomized controlled triallawMedicineAged 80 and overMetastatic colorectal cancerPalliative CareHazard ratioGeneral MedicineMiddle AgedPrognosisTAS-102Survival RateDrug CombinationsOncology030220 oncology & carcinogenesisDrug Therapy CombinationFemaleColorectal NeoplasmsFluoropyrimidineResearch Articlemedicine.drugAdultmedicine.medical_specialtyanimal structuresSubgroup analysisPlaceboAntiviral Agents03 medical and health sciencesDouble-Blind MethodInternal medicineHumansTipiracil hydrochlorideUracilAgedNeoplasm StagingTipiracilbusiness.industrymedicine.diseaseSurgery030104 developmental biologychemistrySpainbusinessThymineFollow-Up StudiesClinical and Translational Oncology
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PML as a potential predictive factor of oxaliplatin/fluoropyrimidine-based first line chemotherapy efficacy in colorectal cancer patients

2012

PML regulates a wide range of pathways involved in tumorigenesis, such as apoptosis, which is also one of the main mechanisms through which oxaliplatin and fluoropyrimidine exert their antineoplastic activity. The present study aims to investigate PML expression as a predictive factor of oxaliplatin/fluoropyrimidine therapy efficacy. Seventy-four metastatic colorectal cancer patients who received oxaliplatin/floropyrimidine-based first line therapy have been included in this retrospective study. PML expression was assessed by immunohistochemistry. PML down-regulation was detected in 39 (52.7%) patients (14 complete and 25 partial PML loss). RR was significantly lower (25.6%) in patients wit…

OncologyMaleOrganoplatinum CompoundsOxaloacetatesPhysiologyColorectal cancerSettore MED/06 - Oncologia MedicavirusesClinical BiochemistryCellLeucovorinPromyelocytic Leukemia Proteinmedicine.disease_causeDeoxycytidineAntineoplastic Combined Chemotherapy Protocolsbiologyvirus diseasesNuclear ProteinsMiddle AgedOxaliplatinSurvival Ratemedicine.anatomical_structureImmunohistochemistryoxaliplatin/fluoropyrimidineFemaleFluorouracilColorectal Neoplasmsmedicine.drugAdultmedicine.medical_specialtyAntimetabolites AntineoplasticPML; oxaliplatin/fluoropyrimidine; colorectal cancerAntineoplastic Agentscolorectal cancerPromyelocytic leukemia proteinPredictive Value of TestsInternal medicinemedicineHumansCapecitabineAgedRetrospective StudiesPMLbusiness.industryTumor Suppressor ProteinsRetrospective cohort studyCell Biologymedicine.diseaseOxaliplatinApoptosisDrug Resistance Neoplasmbiology.proteinCarcinogenesisbusinessTranscription Factors
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CCDC 1516757: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallography4-((13-benzodioxol-5-ylmethyl)(1-methylcyclopropyl)amino)-5-fluoropyrimidine-2-carbonitrileCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1516756: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallography4-((13-benzodioxol-5-ylmethyl)(2-(pyridin-2-yl)ethyl)amino)-5-fluoropyrimidine-2-carbonitrileCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1516758: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallography4-((13-benzodioxol-5-ylmethyl)(4-fluorophenyl)amino)-5-fluoropyrimidine-2-carbonitrileCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1839834: Experimental Crystal Structure Determination

2018

Related Article: Gustavo Portalone, Kari Rissanen|2018|Cryst.Growth Des.|18|5904|doi:10.1021/acs.cgd.8b00662

Space GroupCrystallographyCrystal SystemCrystal Structure26-diaminopyridinium 5-fluoro-26-dioxo-36-dihydro-2H-pyrimidin-1-ide bis(5-fluoropyrimidine-24(1H3H)-dione) NN-dimethylformamide solvateCell ParametersExperimental 3D Coordinates
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CCDC 1516760: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallographyCrystal SystemCrystal Structure4-((13-benzodioxol-5-ylmethyl)(4-(cyclopropylmethoxy)phenyl)amino)-5-fluoropyrimidine-2-carbonitrileCell ParametersExperimental 3D Coordinates
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CCDC 1516759: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallographyCrystal SystemCrystal Structure4-((13-benzodioxol-5-ylmethyl)(4-(trifluoromethyl)cyclohexyl)amino)-5-fluoropyrimidine-2-carbonitrileCell ParametersExperimental 3D Coordinates
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CCDC 1516761: Experimental Crystal Structure Determination

2017

Related Article: Bernd Kuhn, Michal Tichý, Lingle Wang, Shaughnessy Robinson, Rainer E. Martin, Andreas Kuglstatter, Jörg Benz, Maude Giroud, Tanja Schirmeister, Robert Abel, François Diederich, and Jérôme Hert|2017|J.Med.Chem.|60|2485|doi:10.1021/acs.jmedchem.6b01881

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters4-((13-benzodioxol-5-ylmethyl)(2-(2-methyl-4-oxo-6789-tetrahydro-4H-pyrido[12-a]pyrimidin-3-yl)ethyl)amino)-5-fluoropyrimidine-2-carbonitrileExperimental 3D Coordinates
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One-pot synthesis of fluorinated 2-amino-pyrimidine-N-oxides. Competing pathways in the four-atom side-chain rearrangements of 1,2,4-oxadiazoles

2006

Abstract Trifluoromethylated 2-amino-pyrimidine N-oxides have been synthesized by reaction of the 3-amino-5-methyl-1,2,4-oxadiazole with trifluoromethyl-β-diketones in the presence of perchloric acid, followed by hydrolysis. In this ring-to-ring transformation an initial formation of (unisolated) 1,2,4-oxadiazole-pyrimidinium salts, and subsequent ring-opening at the oxadiazole moiety occurs. Isolation of 2-(hydroxyamino)-pyrimidine from the reaction mixture evidenced the presence of a competing pathway where the N(4) nitrogen of the oxadiazole is involved in the formation of a regioisomeric pyrimidinium salt. The effect of the trifluoromethyl group on the product distribution is discussed.…

fluoropyrimidine derivativecrystal structurepyrimidine N-oxidePyrimidinesynthesisStereochemistryOne-pot synthesisOxadiazoleX ray analysis3 diketoneBiochemistryMedicinal chemistryperchloric acidnitrogenchemistry.chemical_compoundside-chain rearrangementDrug DiscoveryStructural isomerSide chainMoietyPerchloric acidring openingfluorinated heterocycle3 diketone fluoropyrimidine derivative ketone derivative nitrogen oxide perchloric acid; article crystal structure hydrolysis priority journal reaction analysis ring opening synthesis X ray analysisTrifluoromethylChemistryOrganic Chemistryarticle124-oxadiazoleketone derivativereaction analysishydrolysispriority journaloxide
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