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中科院上海药物研究所导师介绍:龙亚秋


  代表论著:
  Cao,B.;Wang,Y.;Ding,K.;Neamati,N.;Long,Y.-Q.*Synthesisofthepyridinylanaloguesofdibenzylideneacetone(pyr-dba)viaanimprovedClaisen-Schmidtcondensation,displayingdiversebiologicalactivitiesascurcuminanalogues.Org.Biomol.Chem.2011,DOI:10.1039/C1OB06773G.
  Fan,X.;Zhang,F.-H.;Al-Safi,R.I.;Zeng,L.-F.;Shabaik,Y.;Debnath,B.;Sanchez,T.W.;Odde,S.;Neamati,N.andLong,Y.-Q.*DesignofHIV-1IntegraseinhibitorstargetingthecatalyticdomainaswellasitsinteractionwithLEDGF/p75:ascaffoldhoppingapproachusingsalicylateandcatecholgroups.Bioorg.Med.Chem.2011,19(16),4935-4952.
  Huang,S.-X.;Li,H.-Y.;Liu,J.-Y.;Morisseau,C.;Hammock,B.D.Long,Y.-Q.*Incorporationofpiperazinofunctionalityinto1,3-disubstitutedureaasthetertiarypharmacophoreaffordingpotentinhibitorsofsolubleepoxidehydrolasewithimprovedpharmacokineticproperties.J.Med.Chem.2010,53(23),8376-8386.
  Zhang,H.-S.;Feng,D.-Z.;Chen,L.andLong,Y.-Q.*Discoveryofnovel(S)-α-phenyl-γ-aminobutanamidecontainingCCR5antagonistsviafunctionalityinversionapproach.Bioorg.Med.Chem.Lett.2010,20,2219-2223.
  Fan,X.;Zhang,H.-S.;Chen,L.andLong,Y.-Q.*EfficientSynthesisandIdentificationofNovelPropane-1,3-diaminoBridgedCCR5AntagonistswithVariationontheBasicCenterCarrier.Eur.J.Med.Chem.2010,45(7),2827-2840.
  Liu,J.-H.;Jin,Y.;Long,Y.-Q.*SynthesisoftheC5-C30fragmentofcyclodidemniserinoltrisulfateviaI2-mediateddeprotectionandringclosuretandemreaction.Tetrahedron2010,66,1267-1273.
  Liu,J.-H.;Long,Y.-Q.*Studiestowardthetotalsynthesisofcyclodidemniserinoltrisulfate.PartII:3,5,7-Trisubstituted6,8-dioxabicyclo[3.2.1]octanecorestructureconstructionviaI2-mediateddeprotectionandringclosuretandemreaction.TetrahedronLett.2009,50,4592-4594.
  Liu,J.-H.;Song,L.-D.;Long,Y.-Q.*Studiestowardthetotalsynthesisofcyclodidemniserinoltrisulfate.PartI:3,5,7-Trisubstituted6,8-dioxabicyclo[3.2.1]octanecorestructureconstructionviaaconvergentandalinearstereoselectivesynthesis.TetrahedronLett.2009,50,4587-4591.
  Liu,S.,Zeng,L.-F.,Wu,L.,Yu,X.,Xue,T.,Gunawan,A.,Long,Y.-Q.,*andZhang,Z.-Y.*TargetingInactiveEnzymeConformation:ArylDiketoacidDerivativesasaNewClassofPTP1BInhibitors.J.Am.Chem.Soc.2008,130(50),17075-17084.
  Long,Y.-Q.*;Xue,T.;Song,Y.-L.;Liu,Z.-L.;Huang,S.-X.;Yu,Q.Synthesisandutilizationofchiral??-methylated??-aminoacidswithacarboxyalkylsidechaininthedesignofnovelGrb2-SH2peptideinhibitorsfreeofphosphotyrosine.J.Med.Chem.2008,51(20),6371-6380.
  Zeng,L.-F.;Zhang,H.-S.;Wang,Y.-H.;Sanchez,T.;Zheng,Y.-T.;Neamati,N.;Long,Y.-Q.*Efficientsynthesisandutilizationofphenyl-substitutedheteroaromaticcarboxylicacidsasaryldiketoacidisosteresinthedesignofnovelHIV-1integraseinhibitors.Bioorg.Med.Chem.Lett.2008,18(16),4521-4524.
  Zeng,L.-F.;Jiang,X.-H.;Sanchez,T.;Zhang,H.-S.;Dayam,R.;Neamati,N.*;Long,Y.-Q.*NoveldimericaryldiketocontaininginhibitorsofHIV-1integrase:effectsofthephenylsubstituentandthelinkerorientation.Bioorg.Med.Chem.2008,16(16),7777-7787.
  Tao,Y.-M.;Li,Q.-L.;Zhang,C.-F.;Xu,X.-J.;Chen,J.;Ju,Y.-W.;Chi,Z.-Q.;Long,Y.-Q.*;Liu,J.-G.LPK-26,anovelκ-opioidreceptoragonistwithpotentantinociceptiveeffectsandlowdependencepotential.Eur.J.Pharmacol.2008,584(2-3),306-311.
  Fan,X.;Song,Y.-L.andLong,Y.-Q.*AnEfficientandPracticalSynthesisoftheHIVProteaseInhibitor,AtazanavirviaaHighlyDiastereoselectiveReductionApproach.OrganicProcessResearch&Development2008,12(1),69-75.
  Feng,D.-Z.;Song,Y.-L.;Jiang,X.-H.andLong,Y.-Q.*Forward-andreverse-synthesisofpiperazino-piperidineamideanalogs:ageneralaccesstostructurallydiverse4-piperazino-piperidinebasedCCR5antagonists.Org.Biomol.Chem.2007,5(16),2690-2697.
  Jin,Y.;Zhou,Z.-Y.Tian,W.;Yu,Q.;Long,Y.-Q.*4’-Alkoxylsubstitutionenhancingtheanti-mitoticeffectof5-(3’,4’,5’-substituted)aniline-4-hydroxy-8-nitroquinazolinesasanovelclassofanti-microtubuleagents.Bioorg.Med.Chem.Lett.2006,16(22),5864-5869.
  Li,H.-Y.;Zawahir,Z.;Song,L.-D.;Long,Y.-Q.*andNeamati,N.*Sequence-baseddesignanddiscoveryofpeptideinhibitorsofHIV-1integrase:insightintothebindingmodeoftheenzyme.J.Med.Chem.2006,49(15),4477-4486.
  Song,Y.-L.;Peach,M.;Roller,P.P.;Qiu,S.;Wang,S.andLong,Y.-Q.*Discoveryofanovelnon-phosphorylatedpentapeptidemotifdisplayinghighaffinityforGrb2-SH2domainbytheutilizationof3'-substitutedtyrosinederivatives.J.Med.Chem.2006,49(5),1585-1596.
  Li,H.-Y.;Jin,Y.;Morisseau,C.;Hammock,B.D.Long,Y.-Q.*The5-substitutedpiperazineasanovelsecondarypharmacophoregreatlyimprovingthephysicalpropertiesofurea-basedinhibitorsofsolubleepoxidehydrolase.Bioorg.Med.Chem.2006,14(19),6586-6592.
  Song,Y.-L.;Tan,J.;Luo,X.andLong,Y.-Q.*Utilizationof3’-carboxycontainingtyrosinederivativesasanewclassofphosphotyrosylmimeticsinthepreparationofnovelnon-phosphorylatedcyclicpeptideinhibitorsofGrb2-SH2domain.Org.Biomol.Chem.2006,4(4),659-666.

 

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