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6-取代喹唑啉衍生物的合成及抗肿瘤活性研究进展.docx

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6-取代喹唑啉衍生物的合成及抗肿瘤活性研究进展 Title:ProgressintheSynthesisandAntitumorActivityStudiesof6-SubstitutedQuinoxalineDerivatives Introduction: Quinoxalinederivativeshavegainedsignificantattentioninmedicinalchemistryduetotheirdiversebiologicalactivities,includingantitumorproperties.Amongthevariousapproachestomodifythequinoxalinescaffold,substitutionatthe6-positionhasdemonstratedpromisingresults,leadingtoimprovedpharmacologicalprofilesandenhancedantitumoractivities.Thispaperaimstoprovideanoverviewofthesyntheticmethodsemployedforthepreparationof6-substitutedquinoxalinederivativesanddiscusstheiremergingroleaspotentialanticanceragents. SyntheticMethodsfor6-SubstitutedQuinoxalineDerivatives: Severalsyntheticrouteshavebeenemployedfortheintroductionofdiversesubstituentsatthe6-positionofquinoxaline.Oneofthewidelyusedmethodsisthecondensationofthecorresponding1,2-diaminewithα-dicarbonylcompounds,suchasdiketonesorβ-ketoesters.Thisreactionproceedsthroughanucleophilicsubstitutionreaction,resultingintheformationoffunctionalizedquinoxalines.Additionally,transitionmetal-catalyzedcross-couplingreactions,includingSuzuki-Miyaura,Sonogashira,andStillereactions,havebeenutilizedtointroducearyloralkylgroupsatthe6-position.Theseversatilesyntheticapproachesenablethesynthesisofadiverserangeof6-substitutedquinoxalinederivativeswithimprovedpharmacologicalprofiles. AntitumorActivityof6-SubstitutedQuinoxalineDerivatives: Numerousstudieshavedemonstratedthepotentialanticanceractivitiesof6-substitutedquinoxalinederivatives.Thesecompoundsexhibitcytotoxiceffectsagainstvariouscancercelllines,includinglung,breast,colon,andprostatecancer.AstudybyZhangetal.demonstratedthat6-fluoro-2-(4-methoxyphenyl)quinoxalineinducedcellcyclearrestandapoptosisinbreastcancercellsthroughthemodulationofp53andBcl-2familyproteins.Similarly,6-chloro-2-(4-ethoxyphenyl)quinoxalineexhibitedsignificantantitumoractivityagainsthumannon-smallcelllungcancercellsbyinhibitingthePI3K/Akt/mTORsignalingpathway. Inadditiontotheircytotoxiceffects,6-subs