姓名：张嘉杰

职称：研究员，博士生导师

联系邮箱：zhangjj@smu.edu.cn

联系电话：020-61648548

主要招生方向：药物化学、工业药学

学习经历：

1986.09-1990.07湖南师范大学，化学，学士

1993.09-1996.07华南师范大学，高分子化学与物理，硕士

2001.09-2004.07第一军医大学，药理学，博士

工作经历：

1996.07-1997.09第一军医大学药物研究所，实习研究员

1997.09-2004.08第一军医大学药物研究所，助理研究员

2004.08-2009.12南方医科大学药学院，副研究员

2009.12-南方医科大学药学院，研究员

2005.08-南方医科大学药学院，实验中心主任

2010.01-南方医科大学药学院，药物设计与合成学科主任

研究方向：

1.基于靶标结构的药物分子设计

2.创新药物合成及活性评价研究

主要科研课题：

1.国家自然科学基金项目，抗激酶区突变耐药的ROS1选择性抑制剂的设计、合成及活性研究，81573263，2016.01-2019.12，负责人

2.广东省科技计划项目，高活性间变性淋巴瘤激酶抑制剂SMU-B的成药性研究，2014A020210012，2015.06-2018.06，负责人

3.广东省自然科学基金项目，抗ALK/ROS1及其激酶区突变耐药的双重抑制剂的设计、合成与活性研究，2015A030313285，2015.08-2018.08，负责人

4.国家自然科学基金项目，新型VEGFR酪氨酸激酶抑制剂IPC-032对Wnt/β-catenin信号异常活化的结肠癌细胞合成致死效应的分子机理81173097，2012.01-2012.12，负责人

5.广东省科技厅国际合作项目，基于HIV gp41融合多肽的新型抗艾滋病药物研究2011B050200006，2010.01-2012.12年，负责人。

6.广州市重大科技计划重大项目子课题，以受体酪氨酸激酶为靶点的新型抗肿瘤药物咪唑并吡啶类化合物的研究 2010U1-E00531-3，2010.09-2012.12，负责人

7.国家科技重大专项项目，新型抗肿瘤药物多靶点酪氨酸受体激酶抑制剂IPC-032的研究，2009ZX09103-010，2009.01-2010.12，主要成员（第二）

8.广州市重大科技计划重大项目子课题，以受体酪氨酸激酶为靶点的新型抗肿瘤药物咪唑并吡啶类化合物的研究 2009A1-E011-8，2009.01-2010.08，负责人

9.广东省科技计划项目，相应于HIVgp41的多肽类HIV融合抑制剂C34的研究2005A10904002，2005.01-2006.12，负责人

主要学术任职：

1.中国药理学会抗炎免疫药理学专业委员会 委员

2.广东省高性能计算学会专业委员会 常务理事

3.广东省药学会药物化学专业委员会 委员

主要论著：

1.YTian^#, TZhang^#, LLong,ZLi,SWan,GWang,YYu,JHou,XWu*,JZhang*,Design, synthesis, biological evaluation and molecular modeling of novel.2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors,Eur J Med Chem,2018,143:182-199.

2.Zhang T^#, Tian Y^#, Li Z, Liu S, Hu X, Yang Z, Ling X, Liu S*,Zhang J*,Molecular Dynamics Study to Investigate the Dimeric Structure of the Full-Length α-Synuclein in Aqueous Solution.J Chem Inf Model,2017,57(9):2281-2293.

3.Tian Y^#, Yu Y^#, Shen Y, Wan H, Chang S, Zhang T, Wan S,Zhang J*,Molecular Simulation Studies on the Binding Selectivity of Type-I Inhibitors in the Complexes with ROS1 versus ALK,J Chem Inf Model,2017, 57:977−987.

4.XY Wu^#*,Y Fu,YY Wang,SH Wan,JJ Zhang*,Computational investigation on inhibition mechanism of BRAFV600E by Vemurafenib (PLX4032) and its analogue PLX4720,Med Chem Res,2017,26:390–396.

5.Xiaoyun Wu^#*, Yuanyuan Wang, Shanhe Wan，Jiajie Zhang*, Investigation on the binding mechanism of loratinib with the c-ros oncogene 1 (ROS1) receptor tyrosine kinase via molecular dynamics simulation and binding free energy calculations,J BIOMOL STRUCT DYN, 2017,2017:e1538.

6.Fu Y, Wang Y, Wan S, Li Z, Wang G,Zhang J*, Wu X*,Bisarylureas Based on 1H-Pyrazolo[3,4-d]pyrimidine Scaffold as Novel Pan-RAF Inhibitors with Potent Anti-Proliferative Activities: Structure-Based Design, Synthesis, Biological Evaluation and Molecular Modelling Studies,Molecules,2017, 22:542.

7.Wu X^#*, Fu Y, Wang Y, Wan S,Zhang J*,Gaining insight into crizotinib resistance mechanisms caused by L2026M and G2032R mutations in ROS1 via molecular dynamics simulations and free-energy calculations,J Mol Model,2017,23:141.

8.Yu PJ, Wan LM, Wan SH, Chen WY, Xie H, Meng DM,Zhang JJ*, Xiao XL*,Standardized myrtol attenuates lipopolysaccharide induced acute lung injury in mice,Pharm Biol, 2016,54(12):3211-3216.

9.Hou J^#, Wan S^#, Wang G, Zhang T, Li Z, Tian Y, Yu Y, Wu X*,Zhang J*,Design, synthesis, anti-tumor activity, and molecular modeling ofquinazoline andpyrido[2,3-d]pyrimidine derivatives targetingepidermal growth factor receptor,Eur J Med Chem,2016,118:276-289.

10.Wu X^#*, Wan S, Wang G, Jin H, Li Z, Tian Y, Zhu Z,Zhang J*, Molecular dynamics simulation and free energy calculation studies of kinase inhibitors binding to active and inactive conformations of VEGFR-2,J Mol Graph Model.,2015,56:103-112.

11. Tian Y, Shen Y, Zhang X, Ye L, Li Z, Liu Z,Zhang J*, Wu S,Design Some New Type-I c-met Inhibitors Based on Molecular Docking and Topomer CoMFA Research,Mol Inf,2014,33:536-543.

12.Xiaoyun Wu^#*,Shanhe Wan,Zhonghuang Li,Lin Yan,Jiajie Zhang*,Shuguang Wu,3D-QSAR study on 2,3-dihydroimidazo [4,5]-pyridin-2-one derivatives with a meta substitution pattern as V600E BRAF inhibitors,Med Chem Res,2014,23: 587-602.

13.Li JR^#, Wu N^#, Tian YX ,Zhang JJ*, Wu SG*,Aminopyridyl/Pyrazinyl Spiro[indoline-3,4′-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors,ACS MedChem Lett, 2013, 4 (8):1948-5875.

14. Ye, LB^#, Ou XM^#, Tian YX, Yu BW, Luo Y, Feng BH, Lin H ,Zhang JJ*, Wu SG*,Indazoles as potential c-met inhibitors: Design, synthesis and molecular docking studies,Eur J Med Chem,2013,65:112-8.

15. Wu XY^#*, Wan SH,Zhang JJ*,Three Dimensional Quantitative Structure-Activity Relationship of 5H-Pyrido[4,3-b] indol-4-carboxamide JAK2 Inhibitors,Int J Mol Sci.2013,14(6):12037-53.

16. Wu XY^#*, Chen WH^#, Wu SG, Tian YX,Zhang JJ*,Pyrrolo[3,2-d]pyrimidine Derivatives as Type II Kinase Insert Domain Receptor (KDR) Inhibitors: CoMFA and CoMSIA Studies,Int J Mol Sci,2012,13(2):2387-2404.

17.Ye LB^#, Tian YX^#, Li ZH, Jin H, Zhu ZG, Wan SH, Zhang JY, Yu PJ,Zhang JJ*, Wu SG*，Design, synthesis and molecular docking studies of some novel spiro[indoline-3,4’- piperidine]-2- ones as potential c-met inhibitors,Eur J Med Chem,2012, 50:370-375.

18.Tian YX, Xu J, Li ZH, Zhu ZG,Zhang JJ*, Wu SG,Combined 3D-QSAR and Docking Modeling Study on Indolocarbazole Series Compounds as Tie-2 Inhibitors,Int J Mol Sci,2011, 12(8):5080-5097.

19.Lianbao Ye, Yuanxin Tian, Zhonghuang Li,Jia-Jie Zhang*, Shuguang Wu*,Design and Synthesis of Some Novel 3,4,5-Tetrahydro-1H-pyrido [4,3-b] indoles as Potential c-Met Inhibitors,Helvetica Chimica Acta, 2012 (95):320-326.

20.Jun-Yan Zhang^#, Hong Jin^#, Guang-Fa Wang, Peng-Jiu Yu, Shao-Yu Wu, Zheng-Guang Zhu, Zhong-Huang Li, Yuan-Xin Tian, Wei Xu,Jia-Jie Zhang*, Shu-Guang Wu*,Methyl-1-hydroxy-

2-naphthoate, a novel naphthol derivative, inhibits lipopolysaccharide-induced inflammatory response in macrophages via suppression of NF-κB, JNK and p38 MAPK pathways,Inflamm Res,2011, 60:851-859.

21.Yuanxin Tian, Jian Xu, Zhonghuang Li, Zhengguang Zhu,Jia-Jie Zhang*, Shu-Guang Wu*,Combined 3D-QSAR and Docking Modeling Study on Indolocarbazole Series Compounds as Tie-2 Inhibitors,Int J Mol Sci,2011, 12(8):5080-5097.

22.Wu SY^#, Wang GF^#, Liu ZQ, Rao JJ, Lü L, Xu W, Wu SG*,Zhang JJ*,Effect of geniposide, a hypoglycemic glucoside, on hepatic regulating enzymes in diabetic mice induced by a high-fat diet and streptozotocin, Acta Pharmacol Sin,2009,30(2):202-8.

23.Wang GF^#, Wu SY^#, Rao JJ, Lü L, Xu W, PANG JX，Liu ZQ, Wu SG*,Zhang JJ*,Genipin inhibits endothelial exocytosis via nitric oxide in cultured human umbilical vein endothelial cells,Acta Pharmacol Sin,2009,30(5):589-596.

主要专利:

1.1-(2-氨基吡啶-4-基)-3-哌啶甲酰胺衍生物及其合成方法和应用。申请号:201710237252.X

2.3-(1-(氨基吡啶氧基乙基)苯甲酰胺衍生物及其合成方法和应用。申请号:201710059925.7

3.6-吡唑取代喹唑啉类化合物及其衍生物、合成方法及其应用。申请号:201610156123.3

4.2-氨基吡咯并[1,2-f][1,2,4]三嗪类化合物、合成方法及应用。申请号:201510259005.0，授权

5.一种螺三环类化合物及其制备方法、以含该类化合物的药物组合物及其应用。申请号:201110328838.X，授权

6.一种稠三环类化合物及其制备方法、以含该类化合物的药物组合物及其应用。申请号:201110327893.7，授权

7.一种螺环化合物及其制备方法和应用。申请号:201010205187.0，授权

8.一种四氢吡啶并吲哚类化合物及其制备方法和应用。申请号:201010205202.1，授权

9.一种咪唑并吡啶类化合物。申请号:200910128203.8，授权