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含脲砌块的4-氨基喹唑啉衍生物的设计、合成及抗肿瘤活性研究（英文）.docx

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含脲砌块的4-氨基喹唑啉衍生物的设计、合成及抗肿瘤活性研究（英文） Title:Design,Synthesis,andAntitumorActivityResearchof4-AminoquinazolineDerivativescontainingUreaMoiety. Abstract: Inrecentyears,therehasbeenagrowinginterestinthedevelopmentofnovelantitumoragentswithenhancedpotencyandselectivity.Inthisstudy,aseriesof4-aminoquinazolinederivativescontainingaureamoietyweredesigned,synthesized,andevaluatedfortheirantitumoractivity.Therationaleforincorporatingtheureamoietywastoexploititspotentialforenhancingthecytotoxiceffectsandselectivityagainstcancercells.Thedesign,synthesis,andantitumoractivityofthesederivativeswereinvestigatedinvitrousingapanelofcancercelllines.Theresultsshowedthatthe4-aminoquinazolinederivativescontainingtheureamoietyexhibitedpromisingantitumoractivity,suggestingtheirpotentialasleadcompoundsforfurtherdevelopmentasanticanceragents. Introduction: Cancerremainsaglobalhealthburden,necessitatingthecontinuoussearchfornewandeffectiveantitumoragents.Quinazolinederivativeshavegainedconsiderableattentioninrecentyearsduetotheirdiversepharmacologicalproperties,includingantitumoractivity.Ureaderivatives,ontheotherhand,havebeenreportedtopossesssignificantanticancerpotentialthroughvariousmechanismsofaction.Therefore,combiningthesetwomoietiesinasinglemoleculecouldpotentiallyleadtothedevelopmentofnovelantitumoragentswithimprovedefficacyandselectivity. Methods: Thesynthesisofthe4-aminoquinazolinederivativescontainingtheureamoietywascarriedoutthroughamultistepsyntheticroute.Thestartingmaterial,4-aminoquinazoline,wasselectivelymodifiedtointroducetheureamoiety.Thestructuresofthesynthesizedcompoundswereconfirmedusingvariousspectroscopictechniques,suchasNMR,IR,andmassspectrometry.Thecompoundswerethenevaluatedfortheirantitumoractivityusingapanelofcancercelllines,includingbreast,lung,colon,andprostatecancercelllines.Cellviabilityassays,suchasMTTandSRBassays,wereperformedtodeterminethecytotoxiceffectsofthecompounds.Theselectivityofthecompoundsagainstcancercellswasassessedbycomparingtheircytotoxiceffectswitht