李 剑
发布人: 发布时间: 2008-12-05 作者: 访问次数: 20283

李 剑  副院长 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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本科(化学制药,2000.9)和硕士(药物化学,2003.9)均毕业于沈阳药科大学;博士(药物设计,2006.6)毕业于中科院上海药物研究所;2006.7-至今在华东理工大学药学院任教,历任讲师、副教授、教授。其间,2009.6-2009.8赴美国新墨西哥大学访问研究。2011.3起任药物科学系主任,2015.9起任药学院副院长;兼任中国高等教育学会药学教育研究会理事(2012.09-至今)、上海市青年联合会第十一届委员会委员(2013.11-至今)、第五届中国青年科技工作者协会会员(2014.8-至今)。 
 

先后荣获全国药学青年工作者最新成果一等奖(2006);中国药学会-施维雅青年药物化学奖(2007);上海市青年五四奖章集体(负责人,2011);上海市青年五四奖章(个人,2012);第八届“挑战杯”中国大学生创业计划竞赛铜奖和第七届上海市大学生创业计划大赛金奖(指导教师,2012);上海市研究生优秀成果(学位论文)(指导教师,2012和2013);首届华东理工大学青年英才校长奖(2014)。先后入选上海市科技启明星(2007);国家优秀青年科学基金(2012);教育部新世纪优秀人才(2012);上海市教委曙光学者(2014);华东理工大学首批青年英才(2012)等人才计划。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。迄今已在国内外重要刊物发表论文80余篇,一些研究成果发表在Nature Communications等国际有影响学术刊物上。申请中国发明专利30项(授权11项)。

 

主要研究方向
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1) 抗肿瘤创新药物开发
2) 抗耐药菌创新药物开发
3) 神经精神性疾病创新药物开发
4) 老药新用途开发研究

 

获奖成果
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1)   国家优秀青年科学基金获得者,2012年
2)   教育部新世纪优秀人才,2012年
3)  上海市曙光学者,2014年
4)  上海市徐汇区学科带头人,2014年
5)  上海市青年五四奖章(个人奖),2013年
6)  上海市青年五四奖章集体(负责人),2012年
7)  上海市研究生优秀成果(博士学位论文),指导教师,2013年
8)  上海市研究生优秀成果(硕士学位论文),指导教师,2012年
9)  华东理工大学首批“青年英才校长奖”,2014年
10) 第八届“挑战杯”中国大学生创业计划竞赛铜奖,指导教师,2012年
11) 第七届上海市大学生创业计划大赛金奖,指导教师,2012年

 

 

发表文章列表 (*为通讯作者)
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组建课题组后

 

2012年

 

43. Maosheng Lv, Ting Shi, Xiaona Mao, Xi Li, Yingyi Chen, Jin Zhu, Shuaishuai Ni, Xu Shen, Hualiang Jiang, Jian Li, Jian Zhang, Jin Huang.

1-(2,6-Dibenzyloxybenzoyl)-3-(9H-fluoren-9-yl)-urea: A novel cyclophilin A allosteric activator. Biochem. Biophys. Res. Commun. 2012, 425, 938-943.

 

42. Huang Huang, Ying Yu, Zhenting Gao, Yong Zhang, Chenjing Li, Xing Xu, Hui Jin, Wenzhong Yan, Ruoqun Ma, Jin Zhu, Xu Shen, Hualiang Jiang, Lili Chen*, Jian Li*.

Discovery and Optimization of 1,3,4-Trisubstituted-pyrazolone Derivatives as Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonists. J. Med. Chem. 2012, 55, 7037−7053.

 

41. Yan Zhang, Jing Deng, Sheng Ma, Lin Xue, Jin Zhu, Weiliang Zhu, Hualiang Jiang, Jian Li*, Liyan Miao*.

The Effect of First-in-Class Small Molecule RhoA Inhibitor, HL07, on the Phenylephrine-induced Artery Contraction. Curr. Pharm. Design 2012, 18, 4258–4264.

 

40. Jing Deng, Ning Li, Hongchuan Liu, Zhili Zuo, Oi Wah Liew, Weijun Xu, Gang Chen, Xiankun Tong, Wei Tang*, Jin Zhu, Jianping Zuo, Hualiang Jiang, Cai-Guang Yang*, Jian Li*, Weiliang Zhu*.

Discovery of Novel Small Molecule Inhibitors of Dengue Viral NS2B-NS3 Protease Using Virtual Screening and Scaffold Hopping. J. Med. Chem. 2012, 55, 6278–6293.

 

39. Lu Liu, Deyan Wu, Xiangmin Li, Sinan Wang, Hao Li, Jian Li*, Wei Wang*.

Organocatalytic enantioselective conjugate addition of ketones to isatylidine malononitriles. Chem. Commun. 2012, 48, 1692–1694.

 

38. Lu Liu, Deyan Wu, Shu Zheng, Tengfei Li, Xiangmin Li, Sinan Wang, Jian Li, Hao Li*, Wei Wang*.

Synthesis of Highly Functionalized Chiral 3,3’-Disubstituted Oxindoles via an Organocatalytic Enantioselective Michael Addition of Nitroalkanes to Indolylidenecyanoacetates. Org. Lett. 2012, 14, 134–137.

 

37. Deyan Wu, Fangfang Jin, Weiqiang Lu, Jin Zhu, Cui Li, Wei Wang, Yun Tang, Hualiang Jiang, Jin Huang*, Guixia Liu*, Jian Li*.

 Synthesis, Structure–Activity Relationship, and Pharmacophore Modeling Studies of Pyrazole-3-Carbohydrazone Derivatives as Dipeptidyl Peptidase IV Inhibitors. Chem. Biol. Drug Des. 2012, 79, 897–906.

 

36. Jing Deng, Fei Wang, Wenzhong Yan, Jin Zhu, Hualiang Jiang, Wei Wang*, Jian Li*.

 Synthesis of 3-substitued 1,5-aldehyde esters via an organocatalytic highly enantioselective conjugate addition of new carbonylmethyl 2-pyridinylsulfone to enals. Chem. Commun. 2012, 48,148–150.

 

35. Jin Zhu, Shunting Yu, Wenchao Lu, Jing Deng, Jian Li, Wei Wang.

 Direct oxidative conversion of 3-aryl propionaldehydes to 3-aryl acroleins promoted by SOMO catalysis. Tetrahedron Lett. 2012, 53, 1207–1209.

 

2011年

34. Jiangping Lou, Zhen Liu, Yan Li, Mi Zhou, Zhengxi Zhang, Shu Zheng, Renxiao Wang*, Jian Li*.

Synthesis and anti-tumor activities of N’-benzylidene-2- (4-oxothieno[2,3-d]pyrimidin- 3(4H)-yl)acetohydrazone derivatives. Bioorg. Med. Chem. Lett.2011, 21, 6662–6666.

 

33. Shilei Zhang, Hexin Xie, Aiguo Song, Deyan Wu, Jin Zhu, Sihan Zhao, Jian Li*, Xinhong Yu*, Wei Wang*.

Efficient preparation of trans-α,β-unsaturated aldehydes from saturated aldehydes by oxidative enamine catalysis. Sci. China Ser B: Chem. 2011, 54, 1932–1936.

 

32. Jing Deng, Enguang Feng, Sheng Ma, Yan Zhang, Xiaofeng Liu, Honglin Li*, Huang Huang, Jin Zhu, Weiliang Zhu, Xu Shen, Liyan Miao*, Hong Liu, Hualiang Jiang, Jian Li*.

Design and Synthesis of Small Molecule RhoA Inhibitors: A New Promising Therapy for Cardiovascular Diseases? 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. Weiqiang Lu, Peng Che, Yanyan Zhang, Honglin Li, Shien Zou, Jin Zhu, Jing Deng, Xu Shen, Hualiang Jiang, Jian Li,* Jin Huang*.

HL005—A new selective PPARγ antagonist specifically inhibits the proliferation of MCF-7. J. Steroid Biochem. Mol. Biol. 2011, 124,112–120.

 

30. Shilei Zhang, Hexin Xie, Jin Zhu, Hao Li, Xinshuai Zhang, Jian Li,* Wei Wang,*

Organocatalytic enantioselective β-functionalization of aldehydes by oxidation of enamines and their application in cascade reactions. Nat. Commun. 2011, 2, 211 (本论文分别被美国Chemical & Engineering News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. Ruoqun Ma, Jin Zhu, Jie Liu, Lili Chen*, Xu Shen, Hualiang Jiang, Jian Li,*

Microwave-Assisted One-Pot Synthesis of Pyrazolone Derivatives under Solvent-Free Conditions. Molecules 2010, 15, 3593-3601.

 

28.Jing Deng, Shilei Zhang, Peng Ding, Hualiang Jiang, Wei Wang*, Jian Li*.

Facile creation of 3-indolyl-3-hydroxy-2-oxindoles by an organocatalytic enantioselective Friedel-Crafts reaction of indoles with isatins. Adv. Synth. Catal. 2010, 352, 833-838.

 

27.Shilei Zhang, Jian Li*, Shihang Zhao, Wei Wang*.

1,3-Benzodithiole-1,1,3,3-tetraoxide (BDT) as a versatile methylation reagent in catalytic enantioselective Michael addition reaction with enals. Tetrahedron Lett. 2010, 51, 1766-1769.

 

26.Jie Liu, Jin Zhu, Hualiang Jiang, Wei Wang*, Jian Li*.

Pd-catalyzed cascade Heck-Saegusa: direct synthesis of enals from aryl iodides and allyl alcohol. Chem. Comm. 2010, 46, 415-417.

 

25.Hao Li, Yafei Ji, Jian Li, Shilei Zhang, Chenguang Yu, Wei Wang*.

Organocatalytic enantiodelective Michael addition reactions of fluoronalonates with a, b-unsaturated aldehydes. Sci. China Ser B: Chem., 2010, 53, 135-139.

 

 

2009年

24. Shuaishuai Ni, Yaxia Yuan, Jin Huang, Xiaona Mao, Maosheng Lv, Jin Zhu, Xu Shen, Jianfeng Pei*, Luhua Lai, Hualiang Jiang, Jian Li*.

Discovering Potent Small Molecule Inhibitors of Cyclophilin A Using de Novo Drug Design Approach. J. Med. Chem. 2009, 52, 5295-5298. 

 

23. Jie Liu, Jin Zhu, Hualiang Jiang, Wei Wang,* Jian Li*.

Direct Oxidation of b-Aryl Substituted Aldehydes to a, b-Unsaturated Aldehydes Promoted by a o-Anisidine-Pd(OAc)2 Co-catalyst. Chemistry- An Asian Journal. 2009, 4, 1712-1716.

 

22. Honglin Li, Jin Huang, Lili Chen, Xiaofeng Liu, Tong Chen, Jin Zhu, Weiqiang Lu, Xu Shen, Jian Li*, Rolf Hilgenfeld*, Hualiang Jiang*.

Identification of Novel Falcipain-2 Inhibitors as Potential Antimalarial Agents through Structure-Based Virtual Screening. J. Med. Chem. 2009, 52, 4936-4940. 

 

21. Jin Zhu, Jie Liu, Ruoqun Ma, Hexin Xie, Jian Li*, Hualiang Jiang, Wei Wang*.

A Direct Amine-Pd(OAc)2 Co-catalyzed Saegusa Oxidation Reaction of Unmodified Aldehydes to α, β-Unsaturated Aldehydes. Adv. Synth. Catal. 2009, 351, 1229-1232.

 

20. Feng Fan, Jin Zhu, Shuaishuai Ni, Jiagao Cheng*, Yun Tang, Congmin Kang, Jian Li*, Hualiang Jiang
Pharmacophore Refinement and 3D-QSAR Studies of Inhibitors of Cyclophilin A Containing Amide Linker. QSAR & Comb. Sci. 2009, 28, 183-193.

 

19. Jin Zhu, Tong Chen, Lili Chen, Weiqiang Lu, Peng Che, Jin Huang*, Honglin Li*, Jian Li*, Hualiang Jiang.

2-Amido-3-(1H-Indol-3-yl)-N-Substitued-Propanamides as a New Class of Falcipain-2 Inhibitors. 1. Design, Synthesis, Biological Evaluation and Binding Model Studies. Molecules 2009, 14, 494-508.

  
18. Jin Zhu, Tong Chen, Jie Liu, Ruoqun Ma, Weiqiang Lu, Jin Huang*, Honglin Li*, Jian Li*, Hualiang Jiang.
2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin -2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation. Molecules 2009, 14, 785-797.

  

2008年
17. Yanqing Liu, Enkun Zhou, Kunqian Yu, Jin Zhu, Yu Zhang, Xin Xie*, Jian Li *, Hualiang Jiang
Discovery of A Novel Lead Compound of the CCR5 Antagonist Through Fragment Assembly. Molecules 2008, 2426-2441.

 

16. Yu Zhou, Jian Li, Jian Li, Linxiang Zhao, Hualiang Jiang.

Improved Synthesis of Zanamivir. Chinese J. Med. Chem.2008, 18, 429-433. (in Chinese)

 

15. Xishan Xiong, Hong Liu, Lili Fu, Lin Li, Jian Li, Xiaomin Luo, Changlin Mei.

Antitumor Activity of a New N-Substituted Thiourea Derivative, an EGFR Signaling-Targeted Inhibitor against a Panel of Human Lung Cancer Cell Lines. Chemotherapy 2008, 54, 463-474.

 

2007年

14. Qi Jia, Jian Li, Lili Chen, Xiaofeng Liu, Hongsheng Tan, Weiliang Zhu.

Synthesis and SAR studies on hyperin and its analogues as 3CL protease inhibitors of human coronavirus 229E. Chinese J. Med. Chem. 2007, 17, 288-294. (in Chinese)



参加工作之前(2006年7月)

13. Jian Li, Jing Chen, Chunshan Gui, Li Zhang, Yu Qin, Qiang Xu, Jian Zhang, Hong Liu, Xu Shen, Hualiang Jiang.

Discovering Novel Chemical Inhibitors of Human Cyclophilin A: Virtual Screening, Synthesis and Bioassay. Bioorg. Med. Chem. 2006, 14, 2209-2224.

12. Jian Li, Jian Zhang, Jing Chen, Xiaomin Luo, Weiliang Zhu, Jianhua Shen, Hong Liu, Xu Shen, Hualiang Jiang.
Strategy for Discovering Chemical Inhibitors of Human Cyclophilin A: Focused Library Design, Virtual Screening, Chemical Synthesis and Bioassay. J. Comb. Chem. 2006, 8, 326-337.

11. Jian Li, Jing Chen, Li Zhang, Feng Wang, Chunshan Gui, Li Zhang, Yu Qin, Hong Liu, Fajun Nan, Jingkang Shen, Donglu Bai, Kaixian Chen, Xu Shen, Hualiang Jiang.
One Novel Quinoxaline Derivative as a Potent Human Cyclophilin A Inhibitor Shows Highly Inhibitory Activity Against Mouse Spleen Cell Proliferation. Bioorg. Med. Chem. 2006, 14, 5527-5534.

10. Jian Li, Mingyue Zheng, Wei Tang, Peilan He, Weiliang Zhu, Tianxian Li, Jianping Zuo, Hong Liu, Hualiang Jiang.

Syntheses of Triazole-Modified Zanamivir Analogues via Click Chemistry and Anti-AIV Activities. Bioorg. Med. Chem. Lett. 2006, 16, 5009-5013. 

   

9. Jian Li, Ling Chen, Hong Liu, Xu Shen, Hualiang Jiang.

Progress in Cyclophilin A Inhibitors Research. J. China Pharmaceut. U. 2006, 37, 195-200. (in Chinese)

 

8. Jian Li, Jinzhi Tan, Lili Chen, Jian Zhang, Xu Shen, Changlin Mei, Lili Fu, Liping Lin, Jian Ding, Bin Xiong, Xishan Xiong, Hong Liu, Xiaomin Luo, Hualiang Jiang.

Design, Synthesis and Antitumor Evaluation of New Series of N-Substituted-thiourea Derivatives. Acta Pharmacol. Sin. 2006, 27, 1259-1271.

  
7. Lili Chen, Jian Li(co-first author),  Cheng Luo, Hong Liu, Weijun Xu, Gang Chen, Oi Wah Liew, Weiliang Zhu, Chum Mok Puah, Xu Shen, Hualiang Jiang.
Binding Interaction of Quercetin-3-β-galactoside and Its Synthetic Derivatives with SARS 3CLpro: Structure–activity Relationship Studies Reveals Salient Pharmacophore Features. Bioorg. Med. Chem.2006, 14, 8295-8306.
 

6. Yu Zhou, Jian Li, Hong Liu, Linxiang Zhao, Hualiang Jiang.

An Unusual De-nitro Reduction of 2-Substituted-4-nitroquinolines. Tetrahedron Lett. 2006, 47, 8511-8514.

 

5. Wei Huang, Jian Li, Jing Tang, Hong Liu, Jianhua Shen, Hualiang Jiang.

Microwave-assisted Synthesis of 2-Amino-thiophene-3-carboxylic Derivatives under Solvent-Free Condition. Synth. Commun. 2005, 35, 1351-1357.

 

4. Xiaoning Guo, Li Zhong, Jinzhi Tan, Jian Li, Xiaomin Luo, Hualiang Jiang, Fajun Nan, Liping Lin, Xiongwen Zhang, Jian Ding.

In Vitro Pharmacological Characterization of TKI-28, a Broad-Spectrum Tyrosine Kinase Inhibitor with Anti-Tumor and Anti-Angiogenic Effects. Cancer Biol. Ther. 2005, 4, 1125-1132.

 

3. Hongrui Song, Fei Wang, Jian Li, Shoufang Zhang.

Syntheses of Tetrahydropyrrolizino [2,1-c]quinoline Derivatives. Chem. Res. Chinese U. 2005, 21, 460-462.

 

2. Guang Sun, Jian Li, Shoufang Zhang.

Syntheses of 5-Phenylsulfenyl-2,3-dihydro-1-pyrrolizinone and Its Isomer. Chinese J. Med. Chem. 2003, 13, 156-158. (in Chinese)

 

1. Hong Yu, Fei Wang, Yang Luan, Jian Li, Shoufang Zhang.

Synthesis and Anti-inflammatory and Analgesic Activities of 5-Aryl-1,2-dihydro-1- pyrrolizinones. Chinese J. Med. Chem. 2003, 13, 335-338. (in Chinese)