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1、Anti-CancerDrugsCancercenter,SunYat-senUniversityQuentinLiuOverviewIntroductionOverall5-yearsurvival:about40%,Mortality:second.OverviewGoaloftreatment:CurePalliationIndicationsoftreatment:Neoplasmsdisseminate;Supplementtosurgeryandradiation.OverviewTumorsusceptibility
2、andcellcycleundifferentiatedandrapidlydividingcellsa.cellcyclespecificityb.tumorgrowthrateOverviewCell-cyclespecificityofdrugs:Cell-cyclespecificdrugsAntimetabolitesBleomycinpeptideAntibioticsVincaalkaloidsetoposideEffectiveforhighgrowthfractionmalignancies,e.g.,hemat
3、ologiccancersCell-cyclenon-specificdrugsAlkylatingagentsAntibioticsCisplatinNitrosoureasEffectiveforbothlowgrowthfractionmalignacies,e.g.,solidtumors,aswellashighgrowthfractionmalignanciesOverviewTreatmentregimentandscheduling:logkillpharmacologicsanctuariesTreatmentp
4、rotocols:combinationsofdrugs;advantagesofdrugcombinations;treatmentprotocolsOverviewProblemsofchemotherapy:ResistanceMultidrugresistanceToxicityADP+PiATPMedicineMedicinea.commonadverseeffectsb.durationofadverseeffectsc.minimizingadeverseeffectsAntimetabolitesFolicacid
5、Antagonists:MTXPurineAntagonists:6-MP6-TGPyrimidineAntagonists:5-FUara-CHU---------Sphase(cell-cycle)specificAntimetabolitesMethotrexate(MTX)Antimetabolites6-Mercaptopurine(6-MP)Siteofaction:inhibitionofpurinesynthesisApplication:Acutelymphoblasticleukemia(ALL)Adverse
6、effects:bonemarrowdepressionAntimetabolites5-Fluorouracil(5-FU)Application:colorectalcancerSiteofaction:inhibitionofthymidylatesynthase(TS)andincorporationofitsmetabolitesintoRNAandDNA.AntibioticsDactinomycinDoxorubicinandDaunorubicinBleomycinPlicamycin----------disru
7、ptionofDNAfunctionAntibioticsDoxorubicinSiteofaction:IntercalationintheDNABindingtocellmembranesGenerationofoxygenradicalsthroughlipidperoxidationAdverseeffects:CardiotoxicityDoxorubicinO2ReducedmetaboliteSuperoxideionHydrogenperoxideCytochromeP-450reductaseStrandbrea
8、ksinDNAAntibioticsBleomycinSiteofaction:DNA-bleomycin-Fe++DNA-bleomycin-Fe+++SuperoxideandhydroxylradicalsStrandbreaksinDNAA
