贾文强，中国医学科学院药物研究所，合成室，助研

教育经历：

2011/09-2014/07，中国科学院化学研究所，博士，

2006/09-2009/07，兰州大学，化学化工学院，硕士

2002/09-2006/07，兰州大学，化学化工学院，学士

工作经历：

2014/08-至今，中国医学科学院药物研究所，合成室，助研

代表性论著

(1) Jia, W.-Q.# ; Xi, Q.-M.; Liu, T.-Q.; Yang, M.-J.; Chen, Y.-H.; Yin, D.-L.; Wang, X.-J.* 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.

(2) Jia, W.-Q. #; Zhang, H.-M. ǂ; Zhang C.-L.; Gao, Z.-H.; Ye, S. *, N-Heterocy-clic Carbene Catalyzed [4+2] annulation of a,b-Unsaturated acids: Enantioselective synthesis of dihydropyridinones and spirocyclic oxindolodihydropyridinones, Org. Chem. Front. 2016, 3, 77-81.

(3) Jia, W.-Q. #; Chen, X.-Y. Sun, L.-H. and Ye, S. *, Organocatalytic [4+2] cyclization of a,b-unsaturated acyl chlorides with aldimines: Highly enantioselective synthesis of dihydropyridinone and piperidine derivatives, Org. Biomol. Chem. 2014, 12, 2167-2171.

(4) Zhang, H.-M. #; Jia, W.-Q. #; Liang, Z.-Q. and Ye, S. *, N-Heterocyclic Carbene-Catalyzed [3+3] Cyclocondensation of Bromoenal and Ketimines: Highly Enantioselective Synthesis of Dihydropyridinones, Asian J. Org. Chem. 2014, 3. 462-465. (Zhang and Jia contributed equally to this work)

(5) 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.

1. 基于改善理化性质的选择性S1P1受体激动剂的研究  国家自然科学基金面上项目（No. 81473096）

2. 基于分子片段的选择性S1P1受体激动剂的设计，合成与生物活性研究 国家自然科学基金青年项目 （No. 81102322）

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

1. 基于改善理化性质的选择性S1P1受体激动剂的研究  国家自然科学基金面上项目（No. 81473096）

2. 基于分子片段的选择性S1P1受体激动剂的设计，合成与生物活性研究 国家自然科学基金青年项目 （No. 81102322）

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)

专 著：

《世界上市新药2》 副主编   化学工业出版社 

专 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