学科分类
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5 个结果
  • 简介:Inthisreview,weintensivelyfocusontheadvancesinresearchofnaturalproducts(NPs)discoverycarriedoutbydomesticscholarsinChinafrom2015through2017.Ingeneral,atotalof1811publications(1479inEnglishand332inChinese)wereaccumulatedregardingnewlyisolatedNPsfromplants,microorganisms,andmarinesources.Asaresult,277selectedpapersconcerningnaturallyoccurringcompoundswithextraordinaryframeworks,origins,andpromisingactivitieswerediscussedinthisreviewarticle,mainlyorganizedaccordingtotheirstructuralclassesandnovelties.

  • 标签: NATURAL Products CHEMISTRY Novel STRUCTURES RESEARCH
  • 简介:Objective:Therecurrenceorprogressionunderendocrinetherapyinhormonereceptor-positive(HR+)advancedbreastcancer(ABC)remainedacriticalclinicalchallenge.Chidamideisanoralsubtype-selectivehistonedeacetylase(HDAC)inhibitorwithmultiplefunctionsintumorgrowthinhibitionandmicroenvironmentmodulationviaepigeneticreprogramming.Thepurposeofthisstudywastoevaluatethesafety,pharmacokinetics(PK),andpreliminaryefficacyofchidamideincombinationwithexemestaneinHR+ABCpatients.Methods:EligiblepatientswerepostmenopausalwomenwithHR+ABCrecurrentorprogressedtoatleastoneendocrinetherapy.Bloodsampleswereobtainedintherun-inperiodandthefirstdayofcombinationtreatmentforPKanalysis.Incombinationtreatment,patientsweregivenexemestane25mgdailyandchidamide30mgtwiceaweek(BIW)untilprogressionofdiseaseorintolerabletoxicities.Atreatmentcyclewasdefinedas4weeks.Safety,PKparameters,andpreliminaryefficacywereevaluated.Results:Atotalof20patientswereenrolledbetweenJulyandDecember,2015.Themediannumberoftreatmentscyclewas5.2(20.8weeks)with2patientsstillontreatmentatthedatacut-offdateofOctober,2017.Thetreatment-relatedadverseevents(AE)≥grade3inmorethan2patientswereneutropenia(35%),thrombocytopenia(30%),andleucopenia(20%).Theplasmaexposureofexemestanewasconsistentinthepresenceorabsenceofchidamide.Aslightincreaseinchidamideexposurewasnotedinthepresenceofexemestane,probablyduetotheinter-andintra-patientvariations.Thebestresponsein16evaluablepatientswasassessedbyResponseEvaluationCriteriainSolidTumors(RECIST),including4patientswithpartialresponse,10patientswithstabledisease.Themedianprogression-freesurvival(PFS)was7.6months.Conclusions:ThecombinationofchidamidewithexemestanewasgenerallywelltoleratedwithpromisingpreliminaryefficacyinHR+ABCpatients.Theoverallresultsfromthisstudyencouragefurtherpivotaltrialinthispatie

  • 标签: Advanced breast cancer HORMONE receptor-positive CHIDAMIDE