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  李锐

【个人简历】

李锐,男,博士生导师,研究员,毕业于中科院成都生物研究所。

 

【研究方向】

药物化学

主要研究方向:主要从事计算机辅助靶向小分子抗肿瘤及 HIV 病毒药物的设计、合成及活性评价。

 

【授权专利】

  1. 李锐、魏于全. 4-1,2,3-三氮唑-香豆素衍生物及其制备方法和用途. 专利申请号:CN201110108662
  2. 李锐、魏于全. N-苯基-2-巯基苯甲酰胺衍生物及其制备方法和用途. 专利申请号:CN102603585A

 

【申请项目】

2008

3

校青年基金

雷公藤内酯酮叶酸靶向药物的合成及其主要作用靶点蛋白的质谱鉴定与基于受体的药物修饰

负责人

已完成

2009

10

国家自然科学基金项目编号(30901743

PI3K α mTOR 双靶点抑制剂的设计合成及活性筛选

负责人

已完成

2011

1

重大新药创制

靶向HIV-1/VIF小分子抗艾滋病一类药物的研发

负责人

进行中

2015

1

国家自然科学基金面上项目,81472780BET小分子抑制剂的设计合成及联合siRNA干扰的单载体双靶向复合物的抗白血病作用研究

负责人

进行中

 

【代表性论著】

  1. Feng X, Zhou Z, Ma C, Yin X, Li R*, Dong L, Chen YC* Trienamines derived from interrupted cyclic 2,5-dienones:remote δ, ε-C=C bond activation for asymmetric Inverse-Electron-Demand Aza-Diels-Alder reaction. Angew. Chem. Int. Ed. 2013, 52: 14173 –14176
  2. Zhou M, Luo H, Li R*, Ding ZY Exploring the binding mode of HIV-1 Vif inhibitors by blind docking, molecular dynamics and MM/GBSA. RSC Adv. 2013, 3: 22532
  3. Zhang WJ, Li Z, Zhou M, Wu F, Hou XY, Luo H, Liu H, Han X, Yan GY, Ding ZY, Li R* Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents. Bioorg. Med. Chem. Lett. 2014, 24: 799–807
  4. Ma C, Gu J, Teng B, Zhou QQ, Li R*, Chen YC* 1?Azadienes as Regio- and Chemoselective Dienophiles in Aminocatalytic Asymmetric Diels Alder Reaction Org. Lett. 2013, 24:6206–6209
  5. Wu F, Hou XY, Luo H, Zhou M, Zhang WJ, Ding ZY, Li R*. Exploring the selectivity of PI3Ka and mTOR inhibitors by 3D-QSAR, molecular dynamics simulations and MM/GBSA binding free energy decomposition. MedChemComm. 2013,4: 1482
  6. Han B, Liu QP, Li R*Tian X, Xiong XF, Deng JG, Chen YC*. Discovery of Bifunctional Thiourea/Secondary-Amine Organocatalysts for the Highly Stereoselective Nitro-Mannich Reaction of a-Substituted Nitroacetates.Chem. Eur. J. 2008, 14, 8094 – 8097
  7. Li Z, Zhou M, Wu F, Li R*, Ding ZY Self-organizing molecular field analysis on human beta-secretase  onopeptide inhibitors:5,5-disubstituted aminohydantoins Eur. J. Med.  Chem.,2011,46:58-64
  8. Shi JY, Xu GB, Zhu W, Ye HY, Yang SY,  Luo YF, Han J,  Yang JC, Li R*, Chen LJ*, Wei YQ Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors. Bioo. Med. Chem. Lett.  2010, 20: 4273-4278.
  9. Feng X, Zhou Z, Yin X, Li R*, Chen YC*. Enantioselective Direct Bisvinylogous 1,6-Additions of β-Allyl-2-cyclohexenone to α,α-Dicyanodienes through Trienamine Catalysis. Eur. J. Org. Chem. 2014, 5906–5909 
  10. Luo H, Shi JY, Lu LF, Wu F, Zhou M, Hou XY, Li R*  Molecular dynamics-based self-organizing molecular field analysis on 3-amino-6-arylpyrazines as the ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase inhibitors, Med. Chem. Res., 2014, 23: 747-758.
  11. Hou XY, Luo H, Zhong H, Wu F, Zhou M, Zhang WJ, Han X, Yan GY, Zhang MQ, Lu LF, Ding ZY, He G*, Li R*. Analysis of furo[3,2-c]tetrahydroquinoline and pyrano[3,2-c]-tetrahydroquinoline derivatives as antitumor agents and their metabolites by liquid chromatography/electrospray ionization tandem mass spectrometry Rapid Commun. Mass Spectrom. 2013, 27, 1222–1230
  12. He G, Qiu MH, Li R*, Song XR, Zheng X, Shi JY, Xu GB, Han J, Yu LT, Yang SY, Chen LJ, Wei YQ  Molecular docking-based 3D-QSAR studies of pyrrolo [3, 4-c] pyrazole derivatives as Aurora-A inhibitors Mol. Simulat. 2011,37: 31- 42
  13. Peng AH#, Li R#, Hu J, Chen LJ*, Zhao X, Luo HD, Ye HY, Yuan Y, Wei YQ, Flow rate gradient high-speed counter-current chromatography separation of five diterpenoids from Triperygium wilfordii and scale-up. J. Chromatography A, 1200, 2: 129-135.
  14. Li R*, Peng A H, He CM,  Wang XH, Shi JY, Chen  LJ, Wei YQ Analysis of triptophenolide and its related compounds from tripterygium wilfordii Hook.f by electrospray ionization tandem mass spectrometry. Int. J. Mass Spectrom. , 278,1: 38-49
  15. Li R; Chen W; Shi JY; Chen LJ; Chen YC; Ding LS; Wei YQ. Design and synthesis a new bi(thiourea) Pd pincer guided by ESI-MS/MS Int. J. Mass Spectrom. 2008,43:542-546.
  16. Zhou, M; Luo, H; Li, Z; Wu, F; Huang, CH; Ding, ZY; Li, R*. Recent Advances in Screening of Natural Products for Antimicrobial Agents. Comb. Chem High Throu. Scr. 2012, 15: 306-315.
  17. He ZQ, Han B, Li R*, Wu L, Chen YC* Enantioselective construction of lactone[2,3-b]piperdine skletons via organocatalytic tandem reactions Org. Biomol. Chem., 2010, 8: 755-757.
  18. Lei J, Cui HL, Li R*, Wu L, Ding ZY, Chen YC* Tribuyltin hydride-mediated radical cyclisation reactions:efficient construction of multiply substituted cyclopentanes Org. Biomol. Chem., 2010, 8: 2840-2844.
  19. Zhang SJ, Cui HL, Jiang K, Li R*, Ding ZY, Chen YC* Enantioselective allylic amination of morita-baylis-hillman carbonates catalysed by modified cinchona alkaloids. Eur. J. Org.  Chem. , 2009, 33:5804-5809
  20. Li R, Wu ZJ, Zhang F, Ding LS*, Differentiation of three pairs of aconitum alkaloid isomers from Aconitum nagarum by electrospray ionization tandem mass spectrometryRapid Commun. Mass Spectrom. 2006; 20: 157-170
  21. Li R, Zhou Y, Ding LS*, ESI-QqTOF-MS/MS and APCI-MSn Analysis of Steriod  saponins from the Rhizomes of Dioscorea panthaica, J. Mass Spectrom. 2006; 41: 1-22
  22. Li R, Wang XL, Zhou Y, Cai M, Ding LS*, Analysis of sodium adduct paeoniflorin, albiflorin and their derivatives by (+)ESI-MSn, DFT calculations and  computer-aided mass spectrometry analysis program. J. Mass Spectrom. 2007; 42: 335-345.
  23. 侯雪艳, 武锋, 周孟, 罗浩, 张文娟, 韩璇, 闫国毅,师建友,李锐*. 吡咯并 [3, 4-c] 吡唑衍生的 Aurora 激酶抑制剂在电喷雾质谱中的裂解规律研究. 高等学校化学学报, 2013:71: 1161-1166.
  24. 李锐,周燕, 杨永成, 吴志军, 丁立生*. 无患子皂苷成分的串联质谱分析. 高等学校化学学报, 2006; 27: 52-54.
  25. Han B, He ZQ, Li JL, Li R, Jiang K, Liu TY, Chen YC. Organocatalytic Regio- and Stereoselective Inverse-Electron-Demand Aza-Diels-Alder Reaction of alpha,beta-Unsaturated Aldehydes and N-Tosyl-1-aza-1,3-butadienes. Angew. Chem. Int. Ed. 2009, 48: 5474-5477.
  26. Li JL, Kang TR, Zhou SL, Li R, Wu L, Chen YC* Organocatalytic Asymmetric Inverse-Electron-Demand Diels-Alder Reaction of Electron-Deficient Dienes and Crotonaldehyde. Angew. Chem. Int. Ed. 2010, 49:6418-6420.
  27. Xie JW, Chen W, Li R, Zeng M, Du W, Yue L, Chen YC*, Wu Y, Zhu J, Deng JG* Highly asymmetric Michael addition to alpha,beta-unsaturated ketones catalyzed by 9-amino-9-deoxyepiquinine. Angew. Chem. Int. Ed. 2007, 46: 389-392.
  28. Liu YK, Li R, Yue L, Li BJ, Chen YC*, Wu Y, Ding LS. Unexpected ring-opening reactions of aziridines with aldehydes catalyzed by nucleophilic carbenes under aerobic conditions. Org. Lett. 2006, 8: 1521-1524.
  29. Luo YF, Ma L, Zheng H, Chen LJ*, Li R, He CM. Discovery of (Z)-5-(4-Methoxybenzylidene)thiazolidine-2,4-dione, a Readily Available and Orally Active Glitazone for the Treatment of Concanavalin A-Induced Acute Liver Injury of BALB/c Mice. J. Med. Chem. 2010, 53: 273-2781.
  30. Luo YF, Xu YB, Chen LJ *, Hu J, Peng C, Xie DC, Shi JY, Huang WC, Xu GB, Peng M, Han J, Li R, Yang SY, Wei YQ. Semi-synthesis and anti-proliferative activity evaluation of novel analogues of Honokiol. Bioorg Med. Chem. Lett. 2009; 19: 4702-4705.
  31. He G, Qiu MH, Li R, Ouyang L, Wu FB, Song XR* Multicomplex-Based Pharmacophore-Guided 3D-QSAR Studies of N-Substituted 2'-(Aminoaryl)Benzothiazoles as Aurora-A Inhibitors. Chem. Bio. Drug Design. 2012, 79: 960-971.
  32. Wang XH,  Chen X,  Chen LJ*,  Wang BQ,  Peng C,  He CM,  Tang MH,  Zhang F, Hu J, Li R, Zhao X, Wei YQ. Optimizing high-performance liquid chromatography method for quantification of glucosamine using 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate derivatization in rat plasma: application to a pharmacokinetic study.Biomed. Chrom. 2008, 22: 1265-1271.
  33. Zhang F, Tang MH, Chen LJ*, Li R, Wang XH, Duan JG, Zhao X, Wei YQ. Simultaneous quantitation of aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine and benzoylhypaconine in human plasma by liquid chromatography-tandem mass spectrometry and pharmacokinetics evaluation of "SHEN-FU" injectable powder. J. Chrom. B. 2008, 873: 173-179.
  34. Chen W, Du W, Yue L, Li R, Wu Y, Ding LS, Chen YC* Organocatalytic enantioselective indole alkylations of alpha, beta-unsaturated ketones. Org. Biomol. Chem. 2007, 5 :816-821.
  35. Liu TY, Li R, Chai Q, Long J, Li BJ, Wu Y, Ding LS, Chen, YC* Enantioselective Michael addition of alpha-substituted cyanoacetates to vinyl ketones catalyzed by bifunctional organocatalysts. Chemistry. 2007, 13: 319-327.
  36. Chen W, Li R, Wu Y, Ding LS, Chen YC* Self-supported thiourea-palladium complexes: Highly air-stable and recyclable catalysts for the Suzuki reaction in neat water. Synthesis. 2006, 18: 3058-3062.
  37. Chen WY, Xiang H, Li R, Du W, Wu Y, Ding LS, Chen YC* Organocatalytic and stereoselective [3+2] cycloadditions of azomethine imines with alpha,beta-unsaturated aldehydes. Adv. Syn. Catalyst. 2006, 348: 1818-1822.
  38. Chen W, Li R , Han B, Li BJ, Chen YC*, Wu Y, Ding LS, Yang D The design and synthesis of bis(thiourea) ligands and their application in Pd-catalyzed Heck and Suzuki reactions under aerobic conditions. Eur J. Org. Chem. 2006, 5: 1177-1184.
  39. Liu TY, Long J, Li BJ, Jiang L, Li R, Wu Y, Ding LS, Chen YC* Enantioselective construction of quaternary carbon centre catalysed by bifunctional organocatalyst. Org Biomol Chem. 2006, 4: 2097-2099.

 

【联系方式】

电子信箱:lirui@scu.edu.cn

通讯地址:成都市人民南路三段17号四川大学生物治疗国家重点实验室

邮编:610041

 

生物治疗国家重点实验室 管理入口
地址:中国四川成都高朋大道科园四路一号 邮编:610041