李剑教授博士生导师
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电话:021-64252584；传真:021-64252584
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地址:梅陇路130号实验十八楼1223室
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E-mail:jianli@ecust.edu.cn
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个人简介
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博士，教授，博士生导师。2003年9月毕业于沈阳药科大学，分获工学学士和理学硕士。2006年6月毕业于中科院上海药物研究所，获药物设计博士学位。2006年7月至今在华东理工大学药学院任教，2009年6月至2009年8月赴美国新墨西哥大学做短期访问学者，现为药物化学学科教授，药物科学系系主任，药学硕士专业学位导师组组长。2006年获8^th全国药学青年工作者最新成果一等奖，2007年获10^th中国药学会-施维雅青年药物化学奖和上海市科技启明星称号。2012年获国家自然科学基金委优秀青年基金。作为项目负责人，已完成和正在承担共计10余项国家和省部课题，包括863计划重点项目、国家自然科学基金委重大研究计划和“重大新药创制”科技重大专项等课题。指导学生先后获第七届上海市大学生创业计划大赛金奖(2012.6)和第八届“挑战杯”中国大学生创业计划竞赛铜奖(2012.7)。

李剑主要的研究兴趣在于，发展和应用各种高效药物设计方法，针对重大疾病分子靶标，开展候选药物临床前开发研究，取得了较为系统的创新成果。他已在Nat.Commun.、J.Med.Chem.、Chem.Comm.、Adv.Synth.Catal.、J.Comb.Chem、Bioorg.Med.Chem.等SCI杂志上发表论文四十余篇，申请专利10余项。为中国药学会高级会员，中国化学会会员。


研究方向
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1．抗感染和治疗自身免疫疾病原创候选药物开发；
2．抗肿瘤和降胆固醇Me-better类候选药物开发；
3．有机小分子催化反应研究；
4．蛋白质/多肽的化学合成研究。

获奖成果
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1、第八届全国药学青年工作者最新成果一等奖（2006）
2、上海市药学会青年论文报告会二等奖（2006）
3、第十届中国药学会-施维雅青年药物化学奖（2007）
4、上海市科技启明星（2007）
5、校优秀班导师（2009）
6、上海市青年五四奖章(集体)（2011）
发表文章列表(*为通讯作者)
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组建课题组后

2012年

43.MaoshengLv,TingShi,XiaonaMao,XiLi,YingyiChen,JinZhu,ShuaishuaiNi,XuShen,HualiangJiang,JianLi,JianZhang,JinHuang.
1-(2,6-Dibenzyloxybenzoyl)-3-(9H-fluoren-9-yl)-urea:AnovelcyclophilinAallostericactivator.Biochem.Biophys.Res.Commun.2012,425,938-943.

42.HuangHuang,YingYu,ZhentingGao,YongZhang,ChenjingLi,XingXu,HuiJin,WenzhongYan,RuoqunMa,JinZhu,XuShen,HualiangJiang,LiliChen*,JianLi*.
DiscoveryandOptimizationof1,3,4-Trisubstituted-pyrazoloneDerivativesasNovel,Potent,andNonsteroidalFarnesoidXReceptor(FXR)SelectiveAntagonists.J.Med.Chem.2012,55,7037?7053.

41.YanZhang,JingDeng,ShengMa,LinXue,JinZhu,WeiliangZhu,HualiangJiang,JianLi*,LiyanMiao*.

TheEffectofFirst-in-ClassSmallMoleculeRhoAInhibitor,HL07,onthePhenylephrine-inducedArteryContraction.Curr.Pharm.Design2012,18,4258–4264.

40.JingDeng,NingLi,HongchuanLiu,ZhiliZuo,OiWahLiew,WeijunXu,GangChen,XiankunTong,WeiTang*,JinZhu,JianpingZuo,HualiangJiang,Cai-GuangYang*,JianLi*,WeiliangZhu*.

DiscoveryofNovelSmallMoleculeInhibitorsofDengueViralNS2B-NS3ProteaseUsingVirtualScreeningandScaffoldHopping.J.Med.Chem.2012,55,6278–6293.

39.LuLiu,DeyanWu,XiangminLi,SinanWang,HaoLi,JianLi*,WeiWang*.

Organocatalyticenantioselectiveconjugateadditionofketonestoisatylidinemalononitriles.Chem.Commun.2012,48,1692–1694.

38.LuLiu,DeyanWu,ShuZheng,TengfeiLi,XiangminLi,SinanWang,JianLi,HaoLi*,WeiWang*.

SynthesisofHighlyFunctionalizedChiral3,3’-DisubstitutedOxindolesviaanOrganocatalyticEnantioselectiveMichaelAdditionofNitroalkanestoIndolylidenecyanoacetates.Org.Lett.2012,14,134–137.

37.DeyanWu,FangfangJin,WeiqiangLu,JinZhu,CuiLi,WeiWang,YunTang,HualiangJiang,JinHuang*,GuixiaLiu*,JianLi*.

Synthesis,Structure–ActivityRelationship,andPharmacophoreModelingStudiesofPyrazole-3-CarbohydrazoneDerivativesasDipeptidylPeptidaseIVInhibitors.Chem.Biol.DrugDes.2012,79,897–906.

36.JingDeng,FeiWang,WenzhongYan,JinZhu,HualiangJiang,WeiWang*,JianLi*.
Synthesisof3-substitued1,5-aldehydeestersviaanorganocatalytichighlyenantioselectiveconjugateadditionofnewcarbonylmethyl2-pyridinylsulfonetoenals.Chem.Commun.2012,48,148–150.

35.JinZhu,ShuntingYu,WenchaoLu,JingDeng,JianLi,WeiWang.
Directoxidativeconversionof3-arylpropionaldehydesto3-arylacroleinspromotedbySOMOcatalysis.TetrahedronLett.2012,53,1207–1209.

2011年
34.JiangpingLou,ZhenLiu,YanLi,MiZhou,ZhengxiZhang,ShuZheng,RenxiaoWang*,JianLi*.
Synthesisandanti-tumoractivitiesofN’-benzylidene-2-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)acetohydrazonederivatives.Bioorg.Med.Chem.Lett.2011,21,6662–6666.

33.ShileiZhang,HexinXie,AiguoSong,DeyanWu,JinZhu,SihanZhao,JianLi*,XinhongYu*,WeiWang*.
Efficientpreparationoftrans-α,β-unsaturatedaldehydesfromsaturatedaldehydesbyoxidativeenaminecatalysis.Sci.ChinaSerB:Chem.2011,54,1932–1936.

32.JingDeng,EnguangFeng,ShengMa,YanZhang,XiaofengLiu,HonglinLi*,HuangHuang,JinZhu,WeiliangZhu,XuShen,LiyanMiao*,HongLiu,HualiangJiang,JianLi*.
DesignandSynthesisofSmallMoleculeRhoAInhibitors:ANewPromisingTherapyforCardiovascularDiseases?J.Med.Chem.2011,54,4508-4522.(本论文被自然系列刊物SciBX(4(25),doi:10.1038/scibx.2011.710)选为一种有商业潜力的心血管疾病治疗药物推荐报道)

31.WeiqiangLu,PengChe,YanyanZhang,HonglinLi,ShienZou,JinZhu,JingDeng,XuShen,HualiangJiang,JianLi,*JinHuang*.
HL005—AnewselectivePPARγantagonistspecificallyinhibitstheproliferationofMCF-7.J.SteroidBiochem.Mol.Biol.2011,124,112–120.

30.ShileiZhang,HexinXie,JinZhu,HaoLi,XinshuaiZhang,JianLi,*WeiWang,*
Organocatalyticenantioselectiveβ-functionalizationofaldehydesbyoxidationofenaminesandtheirapplicationincascadereactions.Nat.Commun.2011,2,211(本论文分别被美国Chemical&EngineeringNews作为专家评述和德国化学评论期刊SYNFACTS作为有机合成亮点评述)

2010年
29.RuoqunMa,JinZhu,JieLiu,LiliChen*,XuShen,HualiangJiang,JianLi,*
Microwave-AssistedOne-PotSynthesisofPyrazoloneDerivativesunderSolvent-FreeConditions.Molecules2010,15,3593-3601.

28.JingDeng,ShileiZhang,PengDing,HualiangJiang,WeiWang*,JianLi*.
Facilecreationof3-indolyl-3-hydroxy-2-oxindolesbyanorganocatalyticenantioselectiveFriedel-Craftsreactionofindoleswithisatins.Adv.Synth.Catal.2010,352,833-838.

27.ShileiZhang,JianLi*,ShihangZhao,WeiWang*.
1,3-Benzodithiole-1,1,3,3-tetraoxide(BDT)asaversatilemethylationreagentincatalyticenantioselectiveMichaeladditionreactionwithenals.TetrahedronLett.2010,51,1766-1769.

26.JieLiu,JinZhu,HualiangJiang,WeiWang*,JianLi*.

Pd-catalyzedcascadeHeck-Saegusa:directsynthesisofenalsfromaryliodidesandallylalcohol.Chem.Comm.2010,46,415-417.

25.HaoLi,YafeiJi,JianLi,ShileiZhang,ChenguangYu,WeiWang*.
OrganocatalyticenantiodelectiveMichaeladditionreactionsoffluoronalonateswitha,b-unsaturatedaldehydes.Sci.ChinaSerB:Chem.,2010,53,135-139.
2009年
24.ShuaishuaiNi,YaxiaYuan,JinHuang,XiaonaMao,MaoshengLv,JinZhu,XuShen,JianfengPei*,LuhuaLai,HualiangJiang,JianLi*.
DiscoveringPotentSmallMoleculeInhibitorsofCyclophilinAUsingdeNovoDrugDesignApproach.J.Med.Chem.2009,52,5295-5298.

23.JieLiu,JinZhu,HualiangJiang,WeiWang,*JianLi*.
DirectOxidationofb-ArylSubstitutedAldehydestoa,b-UnsaturatedAldehydesPromotedbyao-Anisidine-Pd(OAc)₂Co-catalyst.Chemistry-AnAsianJournal.2009,4,1712-1716.

22.HonglinLi,JinHuang,LiliChen,XiaofengLiu,TongChen,JinZhu,WeiqiangLu,XuShen,JianLi*,RolfHilgenfeld*,HualiangJiang*.
IdentificationofNovelFalcipain-2InhibitorsasPotentialAntimalarialAgentsthroughStructure-BasedVirtualScreening.J.Med.Chem.2009,52,4936-4940.

21.JinZhu,JieLiu,RuoqunMa,HexinXie,JianLi*,HualiangJiang,WeiWang*.
ADirectAmine-Pd(OAc)2Co-catalyzedSaegusaOxidationReactionofUnmodifiedAldehydestoα,β-UnsaturatedAldehydes.Adv.Synth.Catal.2009,351,1229-1232.

20.FengFan,JinZhu,ShuaishuaiNi,JiagaoCheng*,YunTang,CongminKang,JianLi*,HualiangJiang
PharmacophoreRefinementand3D-QSARStudiesofInhibitorsofCyclophilinAContainingAmideLinker.QSAR&Comb.Sci.2009,28,183-193.

19.JinZhu,TongChen,LiliChen,WeiqiangLu,PengChe,JinHuang*,HonglinLi*,JianLi*,HualiangJiang.
2-Amido-3-(1H-Indol-3-yl)-N-Substitued-PropanamidesasaNewClassofFalcipain-2Inhibitors.1.Design,Synthesis,BiologicalEvaluationandBindingModelStudies.Molecules2009,14,494-508.
18.JinZhu,TongChen,JieLiu,RuoqunMa,WeiqiangLu,JinHuang*,HonglinLi*,JianLi*,HualiangJiang.
2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio)AcetamidesasaNewClassofFalcipain-2Inhibitors.3.Design,SynthesisandBiologicalEvaluation.Molecules2009,14,785-797.

2008年
17.YanqingLiu,EnkunZhou,KunqianYu,JinZhu,YuZhang,XinXie*,JianLi*,HualiangJiang
DiscoveryofANovelLeadCompoundoftheCCR5AntagonistThroughFragmentAssembly.Molecules2008,2426-2441.

16.YuZhou,JianLi,JianLi,LinxiangZhao,HualiangJiang.
ImprovedSynthesisofZanamivir.ChineseJ.Med.Chem.2008,18,429-433.(inChinese)

15.XishanXiong,HongLiu,LiliFu,LinLi,JianLi,XiaominLuo,ChanglinMei.
AntitumorActivityofaNewN-SubstitutedThioureaDerivative,anEGFRSignaling-TargetedInhibitoragainstaPanelofHumanLungCancerCellLines.Chemotherapy2008,54,463-474.
2007年
14.QiJia,JianLi,LiliChen,XiaofengLiu,HongshengTan,WeiliangZhu.
SynthesisandSARstudiesonhyperinanditsanaloguesas3CLproteaseinhibitorsofhumancoronavirus229E.ChineseJ.Med.Chem.2007,17,288-294.(inChinese)


参加工作之前(2006年7月)
13.JianLi,JingChen,ChunshanGui,LiZhang,YuQin,QiangXu,JianZhang,HongLiu,XuShen,HualiangJiang.
DiscoveringNovelChemicalInhibitorsofHumanCyclophilinA:VirtualScreening,SynthesisandBioassay.Bioorg.Med.Chem.2006,14,2209-2224.

12.JianLi,JianZhang,JingChen,XiaominLuo,WeiliangZhu,JianhuaShen,HongLiu,XuShen,HualiangJiang.
StrategyforDiscoveringChemicalInhibitorsofHumanCyclophilinA:FocusedLibraryDesign,VirtualScreening,ChemicalSynthesisandBioassay.J.Comb.Chem.2006,8,326-337.

11.JianLi,JingChen,LiZhang,FengWang,ChunshanGui,LiZhang,YuQin,HongLiu,FajunNan,JingkangShen,DongluBai,KaixianChen,XuShen,HualiangJiang.
OneNovelQuinoxalineDerivativeasaPotentHumanCyclophilinAInhibitorShowsHighlyInhibitoryActivityAgainstMouseSpleenCellProliferation.Bioorg.Med.Chem.2006,14,5527-5534.

10.JianLi,MingyueZheng,WeiTang,PeilanHe,WeiliangZhu,TianxianLi,JianpingZuo,HongLiu,HualiangJiang.
SynthesesofTriazole-ModifiedZanamivirAnaloguesviaClickChemistryandAnti-AIVActivities.Bioorg.Med.Chem.Lett.2006,16,5009-5013.

9.JianLi,LingChen,HongLiu,XuShen,HualiangJiang.
ProgressinCyclophilinAInhibitorsResearch.J.ChinaPharmaceut.U.2006,37,195-200.(inChinese)
8.JianLi,JinzhiTan,LiliChen,JianZhang,XuShen,ChanglinMei,LiliFu,LipingLin,JianDing,BinXiong,XishanXiong,HongLiu,XiaominLuo,HualiangJiang.
Design,SynthesisandAntitumorEvaluationofNewSeriesofN-Substituted-thioureaDerivatives.ActaPharmacol.Sin.2006,27,1259-1271.
7.LiliChen^¶,JianLi^¶(co-firstauthor),ChengLuo,HongLiu,WeijunXu,GangChen,OiWahLiew,WeiliangZhu,ChumMokPuah,XuShen,HualiangJiang.
BindingInteractionofQuercetin-3-β-galactosideandItsSyntheticDerivativeswithSARS3CL^pro:Structure–activityRelationshipStudiesRevealsSalientPharmacophoreFeatures.Bioorg.Med.Chem.2006,14,8295-8306.

6.YuZhou,JianLi,HongLiu,LinxiangZhao,HualiangJiang.
AnUnusualDe-nitroReductionof2-Substituted-4-nitroquinolines.TetrahedronLett.2006,47,8511-8514.
5.WeiHuang,JianLi,JingTang,HongLiu,JianhuaShen,HualiangJiang.
Microwave-assistedSynthesisof2-Amino-thiophene-3-carboxylicDerivativesunderSolvent-FreeCondition.Synth.Commun.2005,35,1351-1357.
4.XiaoningGuo,LiZhong,JinzhiTan,JianLi,XiaominLuo,HualiangJiang,FajunNan,LipingLin,XiongwenZhang,JianDing.
InVitroPharmacologicalCharacterizationofTKI-28,aBroad-SpectrumTyrosineKinaseInhibitorwithAnti-TumorandAnti-AngiogenicEffects.CancerBiol.Ther.2005,4,1125-1132.
3.HongruiSong,FeiWang,JianLi,ShoufangZhang.
SynthesesofTetrahydropyrrolizino[2,1-c]quinolineDerivatives.Chem.Res.ChineseU.2005,21,460-462.
2.GuangSun,JianLi,ShoufangZhang.
Synthesesof5-Phenylsulfenyl-2,3-dihydro-1-pyrrolizinoneandItsIsomer.ChineseJ.Med.Chem.2003,13,156-158.(inChinese)
1.HongYu,FeiWang,YangLuan,JianLi,ShoufangZhang.
SynthesisandAnti-inflammatoryandAnalgesicActivitiesof5-Aryl-1,2-dihydro-1-pyrrolizinones.ChineseJ.Med.Chem.2003,13,335-338.(inChinese)