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汪小涧

时间:2020/7/17 来源: 阅读:12921次


汪小涧

汪小涧,男,博士,副研究员,硕士生导师。2005年毕业于中国药科大学药学理科基地班,获学士学位;2010年毕业于中国药科大学药物化学专业,获博士学位。2010年进入中国医学科学院药物研究所合成药物化学研究室开展研究工作。主要从事药物化学、新药研发、有机合成方法学等方面的研究工作。在药物所工作期间先后任助理研究员、副研究员。现为活性物质发现与适药化研究北京市重点实验室青年骨干成员。2011-2012期间赴美国伊利诺伊州立大学芝加哥分校开展联合研究工作。2011年获得了第14届中国药学会施维雅青年药物化学奖。20142016年度获得药物所 梁周黄于刘青年科技二等奖。2015年度获得江苏省科学技术一等奖(排名第6)。2016年度获得协和新星称号。主持承担了国家自然科学基金面上基金项目,青年基金项目,北京协和医学院青年教师项目,并作为主要研究人员参与了科技部863计划项目、国家十一五十二五重大新药创制专项课题、国家自然科学基金项目等。2010年至今共发表SCI论文30余篇,申请专利6项,已授权3项。是国际著名学术期刊: Green Chemistry; J. Med. Chem.; J. Org. Chem.; Org. Chem. Front.的审稿人。

 

联系方式:wangxiaojian@imm.ac.cn  010-63165248.

教育背景:2001.9 - 2005.6 中国药科大学理科基地班学士

          2005.9 – 2010.6 中国药科大学药物化学专业博士

工作经历:2010.11-2013.6 中国医学科学院药物研究所合成药物化学研究室

助理研究员

          2013.7-至今   中国医学科学院药物研究所合成药物化学研究室

副研究员

专业研究领域:基于人工智能(AI)的药物分子设计,合成与生物活性研究;

              结构多样性芳杂环的有机方法学研究;

              新药开发及合成工艺研究。

代表性论文:

1.    Xi, Q.; Wang, M.; Jia, W.; Yang, M.; Hu, J.; Jin, J.*; Chen, X.*; Yin, D.; Wang, X.*, Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists. J. Med. Chem. 2020, 63, 260-282. (IF=6.2)

2. Liu, T.; Jin, J.; Chen, Y.; Xi, Q.; Hu, J.; Jia, W.; Chen, X.; Li, Y.; Wang, X.*; Yin, D., Identification and Structure–Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P1). Bioorg. Chem.  2019, 82, 41-57. (IF=4.8)

3. Jia, W.; Xi, Q.; Liu, T.; Yang, M.; Chen, Y.; Yin, D.; Wang, X.*, One-Pot Synthesis of O-Heterocycles or Aryl Ketones Using an InCl3/Et3SiH System by Switching the Solvent. J.Org. Chem. 2019, 84, 5141-5149. (IF=4.3)

4. Yang, M.; Tao, B.; Chen, C.; Jia, W.; Sun, S.; Zhang, T.; Wang, X.*, Machine Learning Models Based on Molecular Fingerprints and an Extreme Gradient Boosting Method Lead to the Discovery of JAK2 Inhibitors. J. Chem. Inf. Model. 2019, 59, 5002-5012. (IF=4.5)

5. Chen, Y.; Liu, T.; Xi, Q.; Jia, W.; Yin, D.; Wang, X.*, A Computational Approach to the Study of the Binding Mode of S1P1R Agonists Based on the Active-Like Receptor Model. J. Chem. Inf. Model. 2019, 59 , 1624-1633. (IF=4.5)

6. Yang, M.; Xi, Q.; Jia, W.; Wang, X.*, Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. Bioorg. Med. Chem. Lett. 2019, 29,126758. (IF=2.6)

7.    Liu, T.; Jia, W.; Xi, Q.; Chen, Y.; Wang, X.*; Yin, D., Diversity-Oriented Synthesis of Heterocycles: Al(OTf)3-Promoted Cascade Cyclization and Ionic Hydrogenation. J.Org. Chem. 2018, 83, 1387-1393. (IF=4.8)

8.    Xiao, Q.; Jin, J.; Wang, X. J.; Hu, J. P.; Xi, M. Y.; Tian, Y. L.; Yin, D. L.*, Synthesis, identification, and biological activity of metabolites of two novel selective S1P1 agonists. Bioorg. Med. Chem. 2016, 24, 2273-2279. (IF=2.9)

9.    Xi, M. Y.; Wang, X. J.*; Ge, J.; Yin, D. L.*, N'-[(3-[benzyloxy]benzylidene]-3,4,5-

trihydroxy-benzohydrazide (1) protects mice against colitis induced by dextran sulfate sodium through inhibiting NFkappaB/IL-6/STAT3 pathway. Biochem. Biophys. Res. Commun. 2016, 477, 290-296. (IF=2.6)

10.  Xi, M. Y.; Ge, J.; Wang, X. J.*; Sun, C. B.; Liu, T. Q.; Fang, L.; Xiao, Q.; Yin, D. L.*, Development of hydroxy-based sphingosine kinase inhibitors and anti-inflammation in dextran sodium sulfate induced colitis in mice. Bioorg. Med. Chem. 2016, 24, 3218-3230. (IF=2.9)

11.  Ge, J.; Wang, X. J.*; Liu, T. Q.; Shi, Z. Y.; Xiao, Q.; Yin, D. L.*, Assembly of substituted phenanthridines via a cascade palladium-catalyzed coupling reaction, deprotection and intramolecular cyclization. RSC Adv. 2016, 6, 19571-19575. (IF=2.9)

12.  Fang, L.; Wang, X. J.*; Xi, M. Y.; Liu, T. Q.; Yin, D. L.*, Assessing the ligand selectivity of sphingosine kinases using molecular dynamics and MM-PBSA binding free energy calculations. Mol. BioSys. 2016, 12, 1174-1182. (IF=2.8)

13.  Wang, X. J.*; Sun, C. B.; Fang, L.; Yin, D. L.*, Discovery of novel sphingosine kinase 1 inhibitors via structure-based hierarchical virtual screening. MedChemcom 2015, 6, 413-417.(IF=2.3)

14.  Liu, T. Q.; Wang, X. J.*; Yin, D. L.*, Recent progress towards ionic hydrogenation:Lewis acid catalyzed hydrogenation using organosilanes as donors of hydride ions. RSC Adv. 2015, 5, 75794-75805. (IF=3.3)

15.  Tian, Y. L.; Wang, X. J.*; Xiao, Q.; Sun, C. B.; Yin, D. l.*, Synthesis of Dihydrobenzoheterocycles through Al(OTf)3-Mediated Cascade Cyclization and Ionic Hydrogenation. J.Org. Chem. 2014, 79, 9678-9685. (IF=4.8)

16.  Tian, Y. L.; Jin, J.; Wang, X. J.*; Hu, J. P.; Xiao, Q.; Zhou, W. Q.; Chen, X. G.; Yin, D. l.*, Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design. Eur. J. Med. Chem. 2014, 85, 1-15. (IF=3.9)

17.  Qi, J. G.; Sun, C. B.; Tian, Y. L.; Wang, X. J.*; Li, G.; Xiao, Q.; Yin, D. L.*, Highly Efficient and Versatile Synthesis of Lactams and N-Heterocycles via Al(OTf)3-Catalyzed Cascade Cyclization and Ionic Hydrogenation Reactions. Org. Lett. 2014, 16, 190-192. (IF=6.7)

18.  Zhang, X. J.; Li, X.; Sun, H. P.; Wang, X. J.; Zhao, L.; Gao, Y.; Liu, X. R.; Zhang, S. L.; Wang, Y. Y.; Yang, Y. R.; Zeng, S.; Guo, Q. L.; You, Q. D., Garcinia xanthones as orally active antitumor agents. J.Med.Chem. 2013, 56, 276-292. (IF=6.3)

19.  Tian, Y. L.; Qi, J. G.; Sun, C. B.; Yin, D. l.; Wang, X. J.*; Xiao, Q., One-pot synthesis of 4-methylisoquinolines via a sequential Pd-catalyzed Heck reaction and intramolecular cyclization. Org. Biomol. Chem. 2013, 11, 7262-7266.(IF=3.5)

20.  Wang, X. J.; Lu, N.; Yang, Q.; Gong, D. D.; Lin, C. J.; Zhang, S. L.; Xi, M. Y.; Gao, Y.; Wei, L. B.; Guo, Q. L.; You, Q. D., Studies on chemical modification and biology of a natural product, gambogic acid (III): determination of the essential pharmacophore for biological activity. Eur. J. Med. Chem. 2011, 46, 1280-1290. (IF=3.9)

21.  Li, G.; Xiao, Q.; Li, C.; Wang, X. J.*; Yin, D. L., A facile preparation of tetralins from arene-1,4-diones using titanium(IV) chloride and triethylsilane. Tetrahedron Lett. 2011, 52, 6827-6830. (IF=2.1)

 

著:

《世界上市新药2 副主编   化学工业出版社 

 

利:

1.   尤启冬、汪小涧、杨倩、卢娜、林昌军、郭青龙。 藤黄属衍生物,其制备方法和医药用途。 专利号:ZL201010139385。美国专利号 US 8501803.

2.   杨倩、汪小涧、尤启冬、汤依群、陈春林、郭小可、金英华。芳甲胺类化合物及其制备方法和用途。专利号:ZL200910030031

3.   汪小涧、尤启冬、孙丽、席眉扬、黄婧婕、付继华、尹大力。苯并杂环类化合物、其制备方法及其医药用途。专利号:ZL201210101703

4.   尤启冬、张晓进、李想、刘晓蓉、孙昊鹏、汪小涧、郭青龙。一类藤黄属衍生物、其制 备方法和医药用途。专利号:ZL201110347886

5.   韩伟娟、张海婧、汪小涧、金晶、李刚、张翼、肖琼、周琬琪、陈晓光、尹大力。胺基丙二醇类衍生物、其制备方法和药物组合物与用途。专利申请号:201110188255

6.   田育林、汪小涧、金晶、齐建国、周琬琪、陈晓光、尹大力。含五元芳杂环的氨基丙二醇类化合物、其制备方法及其医药用途。专利申请号:201410053130.1

7.   齐建国、汪小涧、金晶、田育林、周琬琪、陈晓光、尹大力。胺基丙二醇类衍生物、其制备方法和其药物组合物与用途。专利申请号:201410053128

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