auⅲ配合物抗癌机制的研究.docx

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1、ABSTRACTFromthemid-twentiethcentury,thegold-containingdrugshavealreadybeenusedforthetreatmentofrheumatoidarthritis.AlargenumberofAu(I)andAu(III)complexesweresuccessfullysynthesized,amongwhichthemostfamousforAu(I)classisAuranofin・Thesedrugsaremainlyusedforthetrea

2、tmentofactiverheumatoidarthritis.Theycandelaytherheumatoidarthritislesions,improvesymptoms,andhavegoodtolerance・Au(III)andPt(II)haveidentical4fq45d86d°closcd-shcllelectronconfiguration,andtheircoordinationmodestakethesamesquareplanarconfiguration.InasmuchasthePt

3、anti-cancerdrugsproduceaseriesofsideeffects,alargenumberofAu(III)classofgoldcomplexesaresynthesizedasanewpotentialanti-cancerdrugs.Andtheircytotoxicityhasbecomearecentresearchfocus.Au(III)complexesaspotentialanti-cancerdrugshowamorevariablechemicalconfiguration・

4、Theconfigurationsofinterestreportedintheliteraturemaybesummarizedintofourcategories:(i)thesingleligand;(ii)coordinatedbyporphyrin;(iii)coordinatedbyavarietyoforganicmolecules;(iv)coordinatedbybi-dentateligands.AwidevarietyofAu(III)complexesarereportedinthelitera

5、ture,butmostofthemfocusedonthestructuralcharacterizationandinvitroexperiments・Inthefewinvivoexperiments,thechoiceoftumorcelllinesandexperimentalconditionsaredifferent,leadingtothecompounds1anti-canceractivitydonotshowregularityandcomparability.Sofartheanticancer

6、mechanismoftheAu(III)complexesarestillincontroversy,whichincludesthefollowingaspects：(i)Thestructure-activitymechanisms,includingtheimpactoftakingoffgroupsandtheinfluenceofligands•EasilylosingligandsandaromaticconjugategroupsofAu(III)complexeshaveastrongcytotoxi

7、city,(ii)thesulfiir-containingorganicbio-molecularinteractions.SulfhydrylgroupsandthereactivityofAu(lII)complexescanlimittheprogressionofthecancercellgrowth,ofwhichthebiologicaltargetsmaybethethiol-sulfuratom,(iii)theinteractionbetweenproteinsandtheirprotease.Th

8、ecenterofAu(III)complexmayhaveastrongcoordinationwithhistidine,(iv)theinteractionoftheDNAfi-agments.ForAu(III)hastheidenticalelectronicconfigurationwithPt(II)，Au(III)