今天是:2017年11月24日 星期五 农历十月初七
海俐 副教授(硕士生导师)
作者:佚名  来源:  发布时间:2017年07月08日  点击/评论:11481/0

海俐 副教授(硕士生导师)

联系方式

E-mail: smile@scu.edu.cn

成都市人民南路三段17# 四川大学华西药学院,610041


教育背景

1997-2001年 四川大学华西药学院药物化学专业本科

2001-2006年 四川大学华西药学院硕博连读

2008-2010年 美国宾西法尼亚州匹兹堡大学药学院事博士后


研究方向

本小组致力于主动靶向药物设计、合成与靶向性研究,利用配体与靶器官、细胞的特异性结合,赋予药物分子或载体靶向性。最近,我们针对血脑屏障上的营养物质转运体及锁定系统开展了一系列探索性的研究,设计了多种前药及配体,初步展示了这些化合物作为靶向分子潜在的应用价值。

                      

主要科研和教学情况

1. 国家自然科学基金青年基金:“具有‘锁定’功能的GLUT1高亲和力脑靶向药物载体的设计、合成及应用”2012-2014(负责人)

2. 四川大学青年科学研究基金:“新型脑靶向脂质体配体的设计、合成及在反义靶向治疗脑胶质瘤中的应用”2008-2009(负责人)

3. 教育部留学回国人员科研启动基金:“以AMPK为靶标的新型结构类型的化合物设计、合成及活性研究”(负责人)

4. 国家自然科学基金面上项目:“具有ASGR高亲和力脂质体配体的设计、合成及在反义核苷酸靶向治疗肝癌中的应用” 2007-2009(主研)

5. 教育部博士点基金,教育部优先资助领域项目:“具有“锁定”功能的GLUT1高亲和力脑靶向药物载体的设计、合成及应用”2012-2014(主研)

6. 教育部博士点基金项目:“肝靶向125I-ASON胰岛素受体介导的肝癌治疗药物研制” 2006-2008(主研)

7. 十二五国家“重大新药创制”科技重大专项“药物大品种技术改造”:抗肿瘤药物卡培他滨及其关键中间体的开发和产业化.2011-2015(参研)

8. “863”项目:“药物与治疗基因纳米粒的研究与开发”(参研)

9. 2012年度四川大学优秀青年骨干教师奖励


发表论文

1. Xiaojun Ma, Guanghui Lv, Xu Cheng, Weijian Li, Rui Sang, Yong Zhang, Qiantao Wang, Li Hai,* and Yong Wu*. Novel cyclodextrin-modified h-BN@Pd(II) nanomaterial: An efficient and recoverable catalyst for ligand-free C-C crosscoupling reactions in water. Applied Organometallic Chemistry, 2017, 0:e3854.

2. Ren-Jun Li, Yan Zhou, Yang Zheng, Li Hai *, Yong Wu*. The synthesis and biological evaluation of unsymmetrical 2,2-di(1H-indol-3-yl)-N-phenylacetamide derivatives. Tetrahedron Letters, 2016, 57(26): 2829-2832.

3. Yang Zheng, Ren-Jun Li, Zhen Zhan, Yan Zhou, Li Hai*, Yong Wu*. Fe-catalyzed regioselective Friedel–Crafts hydroxyalkylation of N-substituted glyoxylamide with indoles. Chinese Chemical Letters, 2016, 27(1): 41-46.

4. Yaoling Wang, Xu Cheng, Zhen Zhan, Xiaojun Ma, Ruifang Nie, Li Hai*, Yong Wu*. IBX-promoted domino reaction of a-hydroxy amides: A facile one-pot synthesis of isatins. RSC Advances, 2016, 6, 2870 – 2874.

5. Zhan Zhen, Zhang Guoyao, Cheng Xu, Lü Guanghui, Zheng Yang, Hai Li*, Wu Yong*. CuCl2-Promoted Friedel-Crafts Hydroxyalkylations of Indoles. Chinese Journal of Organic Chemistry, 2015, 35(12): 2559-2567.

6. Zhen Zhan, Xu Cheng, Yang Zheng, Xiaojun Ma, Xiaoyu Wang, Li Hai*, Yong Wu*. PhI(OAc)2-promoted metal-free oxidation of 2-oxoaldehydes: A facile one-pot synthesis of cyanoformamides. RSC Advances, 2015, 5, 82800 – 82803.

7. Jue Li, Yang Zheng, Xinling Yu, Songyang Lv, Qiantao Wang, Li Hai*, Yong Wu*.Synthesis of isatins by the palladium-catalyzed intramolecular acylation of unactivated aryl C(sp2)-H bond. RSC Advances, 2015, 5, 103280 – 103283.

8. Zhen Zhan, Xu Cheng, Xiaojun Ma, Jie Li, Li Hai* and Yong Wu*. Hydrogen peroxide-promoted metal free oxidative amidation of 2-oxoaldehydes: A facile access to unsymmetrical oxamides. Tetrahedron, 2015, 71(38): 6928-6934.

9. Yi Zhao, Xiaolong Li, Hong Liu, Yongguo Yu, Li Hai, Li Guo*, Yong Wu*. First synthesis and characterization for the stereoisomers of Ulipristal acetate. Steroids, 2015, 95: 7-16.

10. Yi He, Xiaolong Li, Jue Li, Xiaocen Li, Li Guo, Li Hai*, Yong Wu*. A novel and convenient route for the construction of 5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indoles and its application in the synthesis of Rizatriptan. ?Yi He and Xiaolong Li are co-first authors. Tetrahedron Letters, 2014, 55(29): 3938-3941.

11. Yi Zhao, Boyi Qu, Xueying Wu, Xiaocen Li, Qingqing Liu, Xiuxiu Jin, Li Guo, Li Hai*, Yong Wu*. Design, synthesis and biological evaluation of brain targeting l-ascorbic acid prodrugs of ibuprofen with “lock-in” function. European Journal of Medicinal Chemistry, 2014, 82: 314-323.

12. Xu Cheng, Xiaocen Li, Yanjun Duan, Yongguo Yu, Li Hai*, Yong Wu*. A new and efficient method for the synthesis of Ulipristal acetate. Steroids, 2014, 84:78-83.

13. Xiaocen Li, Boyi Qu, Xiuxiu Jin, Li Hai*, Yong Wu*. Design, synthesis and biological evaluation for docetaxel loaded brain targeting liposome with “lock-in” function. Journal of drug targeting, 2014, 22(3): 251-261.

14. Yun Ren, RenJun Li, Yong Deng, Mei Guan, Yong Wu*, Li Hai*. First synthesis and characterization of SRR/RSS-Ezetimibe. Tetrahedron Letters, 2013, 54(48): 6443–6446. Nov 27.

15. Yun He, Erxiao Sun, Yi Zhao, Li Hai*, Yong Wu*. The one-pot synthesis of 4-Aryl-1H-1,2,3-triazoles without azides and metal catalization. Tetrahedron Letters, 2014, 55(1): 111-115.

16. Xue-Ying Wu, Xiao-Cen Li, Jie Mi, Jing You, Li Hai*. Design, synthesis and preliminary biological evaluation of brain targeting L-ascorbic acid prodrugs of ibuprofen. Chinese Chemical Letters. 2013, 24(2): 117–119.

17. Jianbo Wu, Xueying Wu, Fan Lei, Huajie Yuan, Li Hai, Yong Wu*. Design, synthesis and antibacterial activities of a series of new 2-oxaisocephems. Bioorg. Med. Chem. Lett., 2012, 22(16), 5293–5296.

18. Fulan Xie, Nian Yao, Yao Qin, Qianyu Zhang, Huali Chen, Mingqing Yuan, Jie Tang, Xiankun Li, Wei Fan, Qiang Zhang, Yong Wu, Li Hai*, Qin He*. Investigation of glucose-modified liposomes using polyethylene glycols with different chain lengths as the linkers for brain targeting. Int J Nanomedicine, 2012; 7: 163–175.

19. Wei Fan, Yong Wu, Xian-Kun Li, Nian Yao, Xun Li, Yong-Guo Yu, Li Hai*. Design, synthesis and biological evaluation of brain-specific glucosyl thiamine disulfide prodrugs of naproxen, European Journal of Medicinal Chemistry, 2011, 46(9): 3651-3661.

20. Barbara Bonamassa, Li Hai, Dexi Liu*. Hydrodynamic Gene Delivery and Its Applications in Pharmaceutical Research. Pharm Res, 2011, 28:694–701.

21. Li Hai, Zhi-Rong Zhang, Shan Wang, Xiang Xiao, Yong Wu*. Synthesis of Multivalent Galactosides as Targeting Ligand for Gene Delivery. Synthetic Communications, 2010, 40(12): 1802-1811.

22. Pei Chen, Yu Luo, Li Hai, Shan Qian and Yong Wu*. Design, synthesis, and pharmacological evaluation of the aqueous prodrugs of desmethyl anethole trithione with hepatoprotective activity. European Journal of Medicinal Chemistry, 2010, 45(7): 3005-3010.

23. Li Hai, Jiao Lu, Zhi-Rong Zhang, Shou-Zhu Liao, Jin-Cheng Yang, Yong Wu*. Synthesis of multivalent galactosides with high affinity for the hepatic asialoglycoprotein receptor. Lett. Org. Chem., 2007, 4: 559-562.

24. Lei Tang, Yong Wu, Jiao Lu, Zhi Rong ZHANG, Jin Cheng YANG,Li Hai*. Synthesis of a Novel Tri-antennary Galactoside with High hepatocyte targeting. Chin. Chem. Lett., 2007, 18(5):513-515.

25. Li Hai, Jiang Fan, Zhirong Zhang, Guoyao Zhang, Yong Wu*. Synthesis of Cholesterylated Thiogalactosides for Gene Delivery. Synthetic Communications, 2006, 36(18): 2633 – 2648.

26. Li Hai, Xun SUN, Zhi Rong ZHANG, Yu LUO, Yong WU?.Synthesis of Amphiphilic Hepatocyte Targeting Cholesterylated Thiogalactosides. Chin Chem Lett, 2005, 16(8):1021-1023.




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