中國藥科大學(xué)藥學(xué)院研究生導(dǎo)師介紹：徐云根

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徐云根，男，1964年7月生，藥物化學(xué)專業(yè)博士，教授，博士生導(dǎo)師�，F(xiàn)任藥物化學(xué)教研室主任，江蘇省藥物設(shè)計與成藥性優(yōu)化重點實驗室副主任，江蘇省高校“青藍(lán)工程”中青年學(xué)術(shù)帶頭人，江蘇省第六屆十大杰出專利發(fā)明人，江蘇省高校優(yōu)秀科技創(chuàng)新團(tuán)隊帶頭人。

近年來，專注于心腦血管、神經(jīng)系統(tǒng)和抗腫瘤藥物的設(shè)計與合成研究，先后獲得候選藥物2個。主持承擔(dān)國家自然科學(xué)基金（No.30672512,No.81072520,NO.21272277,No.21472242）、國家重大新藥創(chuàng)制科技重大專項（2009ZX09103-096、2015ZX09102001）等課題15余項。申請發(fā)明專利60余個，已獲得授權(quán)專利30個，包括美國（US7820692、US7541355）、加拿大（CA2657355）、澳大利亞（AU2007276557）等外國專利6個；其中多個專利產(chǎn)品或技術(shù)已實施轉(zhuǎn)讓或產(chǎn)業(yè)化。先后主持開發(fā)并獲得國家新藥證書9本。在國內(nèi)外核心刊物上發(fā)表論文90余篇，其中SCI論文50余篇。

研究方向：（1）新藥分子設(shè)計與合成研究；（2）藥物合成新技術(shù)與新工藝研究（碩士專業(yè)學(xué)位）。

聯(lián)系方式：025-83271244；Email：xyg64@126.com

近三年發(fā)表的部分論文：

1.Qihua Zhu, Dezhong Ji, Tingting Liang, Xueyan Wang, Yungen Xu*. Efficient Palladium-Catalyzed C−H Fluorination of C(sp3)−H Bonds: Synthesis of β‑Fluorinated Carboxylic Acids. Org Lett, 17, 3798−3801, 2015.

2.Zong-jie Gan, Yu-hua Wang, Yungen Xu*, Ting Guo, Jun Wang, Qiao Song, Xue-jun Xu, Shi-yuan Hu, Yu-jun Wang, De-chuan Wang, De-zhu Sun, Di Zhang, Tao Xi, Hao-dong Li, Hai-bo Zhang, Taijun Hang, Hong-guo Lu, Jing-gen Liu*. Discovery, Stereospecific Characterization and Peripheral Modification of 1-(Pyrrolidin-1-ylmethyl)-2-[(6-chloro-3- oxo-indan)-formyl]- 1,2,3,4-tetrahydroisoquinolines As Novel Selective k Opioid Receptor Agonists. Org Biomol Chem, 20(13), 5656-5673, 2015.

3.Shaochi Wang, Peng Dai, Yungen Xu*, Qiufang Chen, Qihua Zhu, Guoqing Gong*. Design, Synthesis, and Biological Evaluation of Dabigatran Etexilate Mimics, a Novel Class of Thrombin Inhibitors. Arch Pharm Chem. Life Sci, 348, 595–605, 2015.

4.Chen Zhou, Fangxia Zou, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of New Non-steroidal TGR5 Agonists Using Virtual Screening with Combined Pharmacophore Models. Med Chem Res, 24(6):2561-2572,2015.

5.Chen Zhou, Di Kang, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of Novel Selective LSD1 Inhibitors Using a Pharmacophore Based Virtual Screening Combined with Multiple Docking. Chem Biol Drug Design, 6：659-671, 2015.

6.Dong-Xing Chen, Jie Huang, Meng Liu, Yun-Gen Xu*, Cheng Jiang*. Design, Synthesis, and Evaluation of Non-ATP-Competitive Small-Molecule Polo-Like Kinase 1 (Plk1) Inhibitors. Arch Pharm Chem. Life Sci, 348(1):2–9, 2015.

7.Qiao Song,Dongmei Zhang, Qihua Zhu*, Yungen Xu*. p-Toluenesulfonohydrazide as Highly Efficient Initiator for Direct C−H Arylation of Unactivated Arenes. Org Lett, 16(20): 5272-5274, 2014.

8.Xiaobo Bao, Wei Yao, Qihua Zhu*, Yungen Xu*. Synthesis of 6-substituted phenanthridine derivatives by Palladium-Catalyzed Domino Suzuki-Miyaura/ Aza-Michael Reactions. Eur J Org Chem, (33):7443-7450, 2014.

9. Lei Shi*, Ting-Ting Wu, Zhi Wang, Jia-Yu Xue, Yun-Gen Xu*. Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. Eur J Med Chem, 84:698-707, 2014.

10.Yun Yang, Xinhui Wang, Qihua Zhu, Guoqing Gong*, Danmeng Luo, Aidou Jiang, Liyan Yang, Yungen Xu*. Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility. Bioorg Med Chem Lett, 24(7):1851-1855, 2014.

11.Jinyin Li, Jing Fang, Fanyi Zhong, Wenxue Li, Yuanjun Tang, Yungen Xu, Shilong Mao*, Guorong Fan*. Development and validation of a liquid chromatography/tandem mass spectrometry assay for the simultaneous determination of dabigatran etexilate, intermediate metabolite and dabigatran in 50 μL rat plasma and its application to pharmacokinetic study. Journal of Chromatography B. 973, 110–119, 2014.

12.Kun Liu, Shuowei Yao,Yinghan Lou, Yungen Xu*. Synthesis and anti-angiogenetic activity evaluation of N-(3-aryl acryloyl)aminosaccharide derivatives. Carbohyd Res, 381:83-92,2013.

13.Yan Tang, Zhewei Tu, Jing Sun, Xiong Zhu*, Kun Liu, Shuying He, Yungen Xu*. Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4. Lett Drug Des Discov,10(10): 935-941,2013.

14.QihuaZhu, XuyangWang, Zhaoxing Chu, Guangwei He*, Guangping Dong, YungenXu*. Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors. Bioorg Med Chem Lett, 23(7):1993-6,2013.

15.Yun-Zhan Li, Guo-Qing Gong*, Wen-Hui Yang, Xin-Hui Wang, Mei-Ling Jiang, Yi Zhou, Xiao-Zhi Yang, Yun-Gen Xu*, Guang-Wei He. Antithrombotic activity of HY023016, a novel Dabigatran prodrug evaluated in animal thrombosis models. Thrombosis Research, 131(5), 425-435,2013.

16.Haiping Zhou, Huiting Su, Zongjie Gan, Dechuan Wang, Yungen Xu*. An efficient procedure for synthesis of 2, 3-dihydro-1Hindene-1-methanamines. Res Chem Intermed, 39:4091-4098, 2013.

17.Zhi Wang, Yi-Qiao Fan, Lei Shi*, Yun-Gen Xu*. Synthesis, crystal structure, and biological activities of a Zn(II) complex with a Se substituted Schiff base. J Coord Chem, 66(11): 2032-2038, 2013.

18.Xiao-Zhi Yang, Xiao-Juan Diao, Wen-Hui Yang, Feng Li, Guang-Wei He, Guo-Qing Gong, Yun-Gen Xu*. Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate. Bioorg Med Chem Lett, 23: 2089-2092,2013.

19.Xu Zhang, Ting Peng, Xun Ji, Jian Li, Linjiang Tong, Zeng Li, Wei Yang, Yungen Xu, Mengyuan Li, Jian Ding, Hualiang Jiang, Hua Xie, Hong Liu*. Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. Bioorg Med Chem, 21(24):7988-7998, 2013.

20.Bin Hu, Qiao Song, Yungen Xu*. Scale-up Synthesis of Antidepressant Drug Vilazodone. Org Process Res Dev, 16(9):1552-1557,2012.

21.Xiao-Zhi Yang, Wen-Hui Yang, Yun-Gen Xu*, Xiao-Juan Diao, Guang-Wei He, Guo-Qing Gong*. Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity. Eur J Med Chem, 57: 21-28, 2012.

22.Yi Zhou, Guoqing Gong*, Wenhui Yang , Yin Wang, Jing Xu, Yungen Xu. The cardioprotective effect of TG-6, a newly synthesized compound, on ischemia-reperfusion injury in rats. Eur J Pharmacol, 683(1-3):190-196,2012.

23.靳璐, 姜向敏, 何廣衛(wèi)*, 徐文婷, 龔國清, 徐云根*. 4(6)-{2-[4-(2,3,4-三甲氧基芐基)哌嗪-1-基]-2-氧代乙氧基}芳甲酰胍類化合物的合成及其Na＋/H＋交換器-1抑制活性, 有機化學(xué). 32(2): 326-332,2012.

24.Jin Ning, Yang Yun, Xu Wenting, Yang Xiaozhi, Gong Guoqing, Xu Yungen*. Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na+/H+ Exchanger Inhibitors. Chin J Chem, 30(2):333-340,2012.

25.Zongjie Gan, Bin Hu, Qiao Song, Yungen Xu*. Convenient Chlorination of Some Special Aromatic Compounds using N-Chlorosuccinimide. Synthesis-Stuttgart, 44(7):1074-1078,2012.

26.Qihua Zhu, Xuyan Wang, Yungen Xu*. Palladium-Catalyzed Tandem Reactions of β-(2-Bromophenyl)-α,β-Unsaturated Carbonyl Compounds with 2-Hydroxyphenylboronic Acid: A New Route to Benzo[c]chromenes. Eur J Org Chem, 6: 1112-1114, 2012.

出版的主要論著或教材：

1.《Medicinal Chemistry》(Second Edition)，科學(xué)出版社，2012年9月第二版，編者。

2.《藥物化學(xué)》，中國醫(yī)藥科技出版社，2011年2月第二版，副主編。

3．國家執(zhí)業(yè)藥師資格考試應(yīng)試指南《藥學(xué)專業(yè)知識》（二），中國醫(yī)藥科技出版社，2011年1月第一版，編者。

4.《藥物化學(xué)》，人民衛(wèi)生出版社，2011年8月第七版，編者。

5.《藥物化學(xué)實驗方法學(xué)》，人民衛(wèi)生出版社，2010年6月出版，編者。

6.《藥物化學(xué)》，化學(xué)工業(yè)出版社，2015年8月出版，編者。

7.《藥物化學(xué)實驗與指導(dǎo)》（雙語），中國醫(yī)藥科技出版社，2008年8月出版，副主編。

8.《藥物設(shè)計學(xué)》，人民衛(wèi)生出版社，2007年8月第一版，編者。