苏桂发 教授

发布者: 张战运 发布时间: 2018-11-23 浏览次数: 1515


---个人基本信息---

姓名:

苏桂发

出生年月:

1963.7

籍贯:

广西桂林

学历:

理学博士

职称:

教授

专业:

有机化学、药物化学


------教育和主要工作经历------

苏桂发理学博士二级教授,1982-7参加工作,1987-7广西师大工作。1996年开始独立指导研究生1998年晋升为教授,2001年获广西科技进步二等奖(排名第1)2003年获广西第七届青年科技奖,2003年入选广西高校百名中青年学科带头人资助计划,2005年入选广西“新世纪十百千人才工程”资助计划。2011年被遴选为有机化学专业博士研究生导师。获广西高校优秀教学成果二等奖一项(2012排名第1)、一等奖两项(排名第220122017)2014年获广西高等学校教学名师奖。

主持20多项厅级以上科研课题的研究,在国内外公开发表学术论文160多篇,获授权中国发明专利8项。作为主编、副主编、参编公开出版教材及学习指导书9(国家规划教材4)


------讲授的课程------

高等有机化学(研究生),物理有机化学(研究生),有机化学(本科生)、有机合成(本科生) 精细有机合成化学与工艺(本科生)


------研究领域------

主要研究和感兴趣的领域:杂环化合物的合成及生物活性研究、高效有机合成反应研究。

---近年研究项目---

目前主持的主要科研项目:

 1.利用分子内去芳构化环化策略合成螺环吡咯[2,1-b]喹唑酮化合物的反应研究(国家自然科学基金课题,直接经费40万,项目批准号: 219610052020.1–2023.12,主持)

 2.基于靶标药效团模型的AromathecinsLuotonin A的结构改造和构效关系研究(广西自然科学基金重点项目,项目编号2017GXNSFDA198045, 40, 2017.9–2021.9,主持)

 3. 3-苯并噻吩喹啉-4-酮类化合物的合成及其诱导的肿瘤细胞旁凋亡研究(省部共建国重室科研课题,项目编号CMEMR2018-A1, 30, 2018.5–2021.4,主持)


科研获奖

广西科技进步二等奖(排名第一, 2001),第七届广西青年科技奖(2003)


------近年代表性科研成果------


 1. Hong-Ping Zhao, Gui-Chao Liang, Shu-Min Nie, Xiuqiang Lu, Cheng-Xue Pan, Xin-Xian Zhong,* Gui-Fa Su,* and Dong-Liang Mo*. Metal-Free Graphene Oxide-Catalyzed Aza-Semi- -pinacol Rearrangement to Prepare 2-(Indol-2-yl)phenols and Benzofuro[3,2-b]indolines Containing Quaternary Carbon Centers, Green Chem.2020, 22, 404–410.

 2.Xin-Wei Wei, Jing-Mei Yuan, Wan-Yun Huang, Nan-Ying Chen, Xiao-Juan Li, Cheng-Xue Pan*, Dong-Liang Mo*, Gui-Fa Su*. 2-Styryl-4-aminoquinazoline derivatives as potent DNA-cleavage, p53-activation and in vivo effective anticancer agents,Eur.J. Med. Chem.2020, 186, 111851.

 3. Zengbo Wang, ChengTian, Qingqing Liu, Wei Zhang, Chengxue Pan*, Gui-Fa Su*. Study on the Synthesis of Benzophenanthridine Analogues via the Cyclization Reaction of Aryl-enamine Ester and Their Cytotoxicity, Chin. J. Org. Chem. 2019, 39, 1962–1969 (in Chinese).

 4.Zhengmin Yang, Wenxiu Li, Hua Chen, Qingyuan Mo, Jun Li,* Shulin Zhao, Cheng Hou, Jiangke Qin*, and Gui-Fa Su. Inhibitor structure-guided design and synthesis of near-infrared fluorescent probes for monoamine oxidase A (MAO-A) and its application in living cells and in vivo, Chem. Commun. 2019, 55, 24772480.

 5.Jun-Yi Liao,   Qing-Yan Wu,Xiuqiang Lu,Ning Zou,Cheng-Xue Pan,Cui Liang,   Gui-Fa SU*and Dong-LiangMo*.  Copper-Catalyzed Diastereoselective O-Transfer Reaction of N-Vinyl-α,β- -Unsaturated Nitrones with Ketenes into γ-Lactones through [5+2] Cycloaddition and N-O Bond Cleavage, Green Chem.2019, 21,6567–6573.

6. Jing-Mei Yuan, Kai Wei, Guo-Hai Zhang, Nan-Ying Chen, Xin-Wei Wei, Cheng-Xue Pan*, Dong-Liang Mo*, Gui-Fa Su*. Cryptolepine and Aromathecin based Mimics as Potent DNA-cleavage and Anticancer Agents: Design, Synthesis and DNA Targeting-Induced Apoptosis, Eur.J. Med. Chem.2019, 169, 144158.

 7. Si-Yi Wu, Wei-Li Chen, Xiao-Pan Ma, Cui Liang, Gui-Fa Su,* and Dong-Liang Mo*. Copper-Catalyzed [3+2] Cycloaddition and Interrupted Fischer Indolization to Prepare Polycyclic Furo[2,3-b]indolines from N-Aryl Isatin Nitrones and Methylenecyclopropanes, Adv. Synth. & Catal.2019,361(5), 965 970.

 8. Qing-Qing Liu, Ke Lu, Hai-Miao Zhu, Shi-Lin Kong, Jing-Mei Yuan, Guo-Hai Zhang, Nan-Ying Chen, Chen-Xi Gu, Cheng-Xue Pan*, Dong-Liang Mo*, Gui-Fa Su*. Identification of 3-(benzazol-2-yl)quinoxaline derivatives as potent anticancer compounds: Privileged structure-based design, synthesis, and bioactive evaluation in vitro and in vivo, Eur. J. Med. Chem. 2019, 165, 293−308.

 9. Ning Zou, Ji-Wen Jiao, Yu Feng, Cheng-Xue Pan, Cui Liang, Gui-Fa Su,* and Dong-Liang Mo*. Iron(III)/Copper(II)-Cocatalyzed Cycloaddition/[3,3]-Rearrangement/N−O Bond Cleavage To Prepare Polysubstituted Pyrrolizines from N Vinyl-α,β-Unsaturated Nitrones and Activated Alkynes, Org. Lett.2019, 21, 481−485.

 10. Yan-Xiao Jiao, Lin-Su Wei, Chun-Yang Zhao, Kai Wei, Dong-Liang Mo,* Cheng-Xue Pan,* and Gui-Fa Su*. Isobutyl Nitrite-Mediated Synthesis of Quinoxalines through Double C−H Bonds Amination of N-Aryl Enamines,Adv. Synth. Catal.2018, 360(22), 4446–4451.

 11. Chun-Hua Chen, Qing-Yan Wu, Cui Wei, Cui Liang, Gui-Fa Su* and Dong-Liang Mo*. Iron(III)-catalyzed selective N–O bond cleavage to prepare tetrasubstituted pyridines and 3,5-disubstituted isoxazolines from N-vinyl-α,β-unsaturated ketonitrones, Green Chem.,2018, 20, 2722−2729.  (Inside Front Cover Paper)

 12. Lin-Su Wei, Guo-Xue He, Xiang-Fei Kong, Cheng-Xue Pan,* Dong-Liang Mo,* and Gui-Fa Su*. Gold(III)-Catalyzed Selective Cyclization of Alkynyl Quinazolinone-Tethered Pyrroles: Synthesis of Fused Quinazolinone Scaffolds, J. Org. Chem. 2018, 83, 6719−6727.

 13. Chun-Yang Zhao, Kun Li, Yu Pang, Jia-Qing Li, Cui Liang, Gui-Fa Su*, and Dong-Liang Mo*. Iodine(III) Reagent-Mediated Intramolecular Amination of 2-Alkenylanilines to Prepare Indoles,  Adv. Synth. Catal. 2018,360, 1919–1925.

 14.Hong-Yan Bi, Feng-Ping Liu, Cui Liang, Gui-Fa Su*, and Dong-Liang Mo*. A Tunable Route to Prepare ɑ,β-Unsaturated Esters and ɑ,β-Unsaturated-γ-Keto Esters through Copper-Catalyzed Coupling of Alkenyl Boronic Acids with Phosphorus Ylides, Adv. Synth. Catal. 2018, 360, 1510– 1516.

 15. Xiang-Fei Kong,Feng Zhan, Guo-Xue He, Cheng-Xue Pan, Chen-Xi Gu, Ke Lu, Dong-Liang Mo,* and Gui-Fa Su*. Gold-Catalyzed Selective 6-exo-dig and 7-endo-dig Cyclizations of  Alkyn-Tethered Indoles To Prepare Rutaecarpine Derivatives, J. Org. Chem. 2018,83(4), 2006– 2017.     

 16. Xiao-Pan Ma, Kun Li, Si-Yi Wu, Cui Liang, Gui-Fa Su* and Dong-Liang Mo*. Construction of 2,3-quaternary fused indolines from alkynyl tethered oximes and diaryliodonium salts through a cascade strategy of N-arylation/ cycloaddition/[3,3]- rearrangement, Green Chem.2017, 19(24), 5761–5766.2017 Green Chemistry Hot Articles. (Inside Front Cover Paper)

 17. Ning Zou, Ji-Wen Jiao, Yu Feng,a Chun-Hua Chen, Cui Liang, Gui-Fa Su,* and Dong-Liang Mo.*Diastereoselective Synthesis of Nine-Membered Heterocycles via the Cycloaddition and Sequential Rearrangement of N-Vinyl Nitrones with Isocyanates, Adv. Synth. Catal.2017, 359, 3545–3350.

18. Wei-Min Shi, Feng-Ping Liu, Zhi-Xin Wang, Hong-Yan Bi, Cui Liang, Li-Ping Xu,* Gui-Fa Su,*and Dong-Liang Mo.* Synthesis of 1-Vinyl/Aryl Benzotriazole 3-Oxides through Copper-Catalyzed C-N Bond Coupling Reaction, Adv. Synth. Catal., 2017, 359(16), 2741-2746.

 19. Guo-Hai Zhang, Jing-Mei Yuan, Gang Qian, Chen-Xi Gu, Kai Wei, Dong-Liang Mo, Jiang-Ke Qin, Yan Peng, Zu-Ping Zhou, Cheng-Xue Pan*, and Gui-Fa Su*. Phthalazino[1,2-b]- -quinazolinones as p53 Activators: Cell Cycle Arrest, Apoptotic Response and Bak–Bcl-xl Complex Reorganization in Bladder Cancer Cells, J. Med. Chem.2017, 60(16), 6853− 6866.

 20. Chun-Hua Chen,Qing-Qing Liu,Xiao-Pan Ma, Yu Feng, Cui Liang, Cheng-Xue Pan, Gui-Fa Su,* and Dong-Liang Mo*. Copper-Catalyzed Selective N Vinylation of 3 (Hydroxyimino)- -indolin-2-ones with Alkenyl Boronic Acids: Synthesis of N Vinyl Nitrones and Spirooxindoles, J. Org. Chem. 2017,82, 6417−6425.

 21. Yan-Xiao Jiao, Ling-Ling Wu, Hai-Miao Zhu, Jiang-Ke Qin, Cheng-Xue Pan,* Dong-Liang Mo,* and Gui-Fa Su*. Tandem C–N Bonds Formation through Condensation and Metal-Free N-Arylation: Protocol for Synthesizing Diverse Functionalized Quinoxalines, J. Org. Chem.2017, 82(8), 4407−14.

22. Guo-Xue He, Jing-Mei Yuan, Hai-Miao Zhu, Kai Wei, Ling-Yun Wang, Shi-Lin Kong, Dong-Liang Mo, Cheng-Xue Pan* and Gui-Fa Su*. Synthesis and antitumor evaluation of 2,3-diarylbenzofuran derivatives on HeLa cells, Bioorg. Med. Chem. Lett. 2017, 27, 1660–1664.

23. Yan-Xiao Jiao, Xiao-Pan Ma, Gui-Fa Su* and Dong-Liang Mo*. Recent Advances in Arylation and Alkenylation of N–O bonds, Synthesis, 2017,49, 933-959.

 24. Xiao-Pan Ma, Jie-Feng Zhu, Si-Yi Wu, Chun-Hua Chen, Ning Zou, Cui Liang, Gui-Fa Su,*and Dong-Liang Mo*. Cycloaddition of Fluorenone N Aryl Nitrones with Methylenecyclopropanes and Sequential 1,3-Rearrangement: An Entry to Synthesis of Spirofluorenylpiperidin-4-ones, J. Org. Chem.2017, 82, 502−511.

 25. Zhi-Xin Wang, Wei-Min Shi, Hong-Yan Bi, Xiao-Hua Li, Gui-Fa Su* and Dong-Liang Mo*. Synthesis of N-(2-Hydroxyaryl)benzotriazoles via Metal-Free O-Arylation and N−O Bond Cleavage, J. Org. Chem. 2016, 81, 8014-8021.

 26. Chun-Yang Zhao, Liang-Gui Li, Qing-Rong Liu, Cheng-Xue Pan, Gui-Fa Su* and Dong-Liang Mo*. Synthesis of β-acetoxy alcohols by PhI(OAc)2-mediated metal-free diastereoselective β-acetoxylation of alcohols, Org. Biomol. Chem.,2016, 14, 6795–803.

 27. Wei-Min Shi, Xiao-Pan Ma, Gui-Fa Su*, Dong-Liang Mo*. New developments of ketonitrones in organic synthesis, Org. Chem. Front.2016, 3, 116–130.

28. Guo-Hai Zhang, Wen-Bin Xue, Yun-Feng An, Jing-Mei Yuan, Jiang-Ke Qin, Cheng-Xue Pan*, Gui-Fa Su*. Distinct novel quinazolinone exhibits selective inhibition in MGC-803 cancer cells by dictating mutant p53 function, Eur. J. Med. Chem.2015, 95, 377-387.

29. Wei-Min Shi, Xiao-Pan Ma, Cheng-Xue Pan, Gui-Fa Su,* and Dong-Liang Mo*. Tandem C―O and C―N Bonds Formation Through O-Arylation and [3,3]-Rearrangement by Diaryliodonium Salts: Synthesis of N-Aryl Benzo[1,2,3]triazin-4(1H)-one Derivatives, J. Org. Chem.2015, 80, 11175- 11183.

 30. Xiao-Pan Ma,Wei-Min Shi,Xue-Ling Mo,Xiao-Hua Li,Liang-Gui Li,Cheng-Xue Pan,Bo Chen,* Gui-Fa Su,* and Dong-Liang Mo*. Synthesis of α,β-Unsaturated N-Aryl Ketonitrones from Oximes and Diaryliodonium Salts: Observation of a Metal-Free N-Arylation Process,J. Org. Chem.2015, 80, 10098-10107.

 31. Qing-Rong Liu, Cheng-Xue Pan, Xiao-Pan Ma, Dong-Liang Mo,* and Gui-Fa Su*. (Diacetoxyiodo)benzene–Mediated Reaction of Ethynylcarbinols: Entry to α,α′-Diacetoxy Ketones and Glycerol Derivatives, J. Org. Chem.2015, 80, 6496−6501.

 32. Yan-Li Xu, Ying-Ming Pan,* Pei Liu, Heng-Shan Wang, Xiao-Yan Tian, and Gui-Fa Su*. Indium (III) chloride catalyzed conjugate addition reaction of alkynylsilanes to acrylate esters,J. Org. Chem.2012, 77, 3557−3562.

 33.潘成学,苏桂发,焦艳晓,魏凯,莫冬亮.一种喹喔啉衍生物的高效合成方法, 2018-6-5授权,中国发明专利号ZL 201510969658.8.

 34.潘成学,魏凯,苏桂发,袁静梅,莫冬亮.一种新的[1,2,b]茚并喹啉类衍生物及其制备方法和在抗肿瘤药物中的应用, 2018-7-11授权,中国发明专利号ZL 201510969658.8.

 35.潘成学,苏桂发,孔石林,戴求资,朱海妙,刘晴晴。萘并[1,2-h][1,6]萘啶-3(4H)-酮类化合物及其制备方法和应用,中国发明专利号ZL 201610554316.4

 36.苏桂发,潘成学,钱刚,袁静梅,张国海,何国学。酞嗪并[1,2,b]喹唑啉-8-酮化合物及其制备方法和抗肿瘤药物中的应用,中国发明专利号ZL 201510969739.8

 37. 潘成学,苏桂发,焦艳晓,吴玲玲,覃江克。2, 3-二取代喹喔啉衍生物的制备方法,中国发明专利号ZL201410323633.6

38. 苏桂发,焦艳晓,潘成学,韦罗山,孔石林,黄婉云。川芎嗪茋类衍生物及其制备方法与应用, 中国发明专利号ZL 201410075473.8

39. 苏桂发,郑志兵,农娟,李松,王莉莉,覃江克,潘成学,唐煌,邓业成。新的哌嗪和高哌嗪类衍生物及其制备方法和应用,中国发明专利号ZL 201110324535.0.

40. 苏桂发,潘成学,冯凯熙,戴支凯,覃江克,唐煌,刘华钢。2,3-二氧乙基-5-甲基-8,9-二甲氧基苯并菲啶衍生物及其制备方法和应用,中国发明专利号ZL 201210381432.2.