Aurones A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents英文文献资料.docVIP

Aurones A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents英文文献资料.doc

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Aurones A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents英文文献资料

HindawiPublishingCorporation InternationalJournalofMedicinalChemistry Volume2012,ArticleID196921,8pages doi:10.1155/2012/196921 ResearchArticle Aurones:APromisingHeterocyclicScaffoldfortheDevelopment ofPotentAntileishmanialAgents MarinaRoussaki, So?aCostaLima, Anna-MariaKypreou, PanagiotisKefalas, 1 2 1 3 AnabelaCordeirodaSilva,2,4andAnastasiaDetsi1 1 2 3 4 LaboratoryofOrganicChemistry,SchoolofChemicalEngineering,NationalTechnicalUniversityofAthens, HeroonPolytechniou9,ZografouCampus,15780Athens,Greece ParasiteDiseaseGroup,IBMC-InstituteforMolecularandCellBiology,UniversityofPorto,RuadoCampoAlegre, 823,4150-180Porto,Portugal DepartmentofFoodQualityandChemistryofNaturalProducts,MediterraneanAgronomicInstituteofChania, InternationalCentreforAdvancedMediterraneanAgronomicStudies,73100Chania,Crete,Greece DepartmentofBiologicalSciences,FacultyofPharmacy,UniversityofPorto,RuadeJorgeViterboFerreiera, 228,4050-313Porto,Portugal CorrespondenceshouldbeaddressedtoAnastasiaDetsi,adetsi@chemeng.ntua.gr Received27May2012;Accepted31July2012 AcademicEditor:O.Bruno Copyright?2012MarinaRoussakietal. This is an open access article distributed under the Creative Commons Attribution License,whichpermitsunrestricteduse,distribution,andreproductioninanymedium,providedtheoriginalworkisproperly cited. A series of (Z)-2-benzylidenebenzofuran-3-(2H)-ones (aurones) bearing a variety of substituents on rings A and B were synthesizedandevaluatedfortheirantiparasiticactivityagainsttheintracellularamastigoteformofLeishmaniainfantumandtheir cytotoxicityagainsthumanTHP1-di?erentiatedmacrophages.Ingeneral,auronesbearingnosubstituentsonringA(compounds 4a–4f)exhibithighertoxicitythanauroneswith4,6-dimethoxysubstitution(compounds4g–4l).Amongthelatter,twoaurones possessinga2-methoxyora2-methylgroup(compounds4iand4j)exhibitpotentantileishmanialactivity(IC50=1.3± 0.1μM   andIC50=1.6±0.2μM,resp.),comparabletotheactivityofthereferenced

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