2000.09 – 2004.07 复旦大学(原上海医科大学)药学院,药物化学系,理学博士
(导师:林国强院士、胡昌奇教授)
1994.09 - 1997.07 上海医科大学药学院,药物化学系,理学硕士(导师:夏鹏教授)
1983.09 – 1987.06 南昌大学,化学系,理学学士
学术经历:2010.01-现在复旦大学药学院天然药物化学教研室 教授、博士生导师
2009.01-2010.01复旦大学药学院天然药物化学教研室 教授、硕士生导师
2001.01-2010.01 复旦大学药学院天然药物化学教研室 副教授、硕士生导师
1997.07-2001.01复旦大学药学院有机化学教研室 副教授
行政经历:
2017.06-2019.09 复旦大学上海医学院副院长、复旦大学科研院副院长
复旦大学上海医学院规划与科研办主任
2012.12-2017.06 复旦大学药学院科研副院长
2014.12-2015.10 复旦大学药学院代院长
2009.01-2012.12 复旦大学药学院行政副院长
活性天然先导化合物的结构优化设计与发现及其功能靶标作用机制的研究
潜在临床靶标的药靶验证和抗肿瘤、抗炎症免疫以及抗耐药菌等新药研发与创制
天然产物优势骨架结构的多样性合成方法学和全合成研究
主持项目
1、科技部新药创制重大专项3项:新型抗革兰氏阳性多重耐药菌万古霉素类候选药物的研究与开发(2012ZX09J12108-05C);新型糖肽类战场上抗感染外用喷雾剂的研究与开发(2009ZXJ09004-090);多烯紫杉醇氟代衍生物的临床前研究(2009ZX09301011-015)。
2、国家自然科学基金面上项目7项:基于全新靶标膜联蛋白A3介导三阴性乳腺癌增殖转移的小分子探针抑制剂的发现与分子机制研究 (82073688,2021/01-2024/12);基于TNF-α靶点的抗溃疡性结肠炎天然优势骨架小分子抑制剂的设计与药物发现 (81673297);SGLT2抑制剂潜在毒性代谢产物的研究及其结构优化与合成(81402787);四氟多烯紫杉醇新型抗肝癌靶向前药的设计合成及成药性研究(81373276);新型铱手性配合物的合成及其抗卵巢癌作用机制的研究(81172920);天然产物白藜芦醇二聚体的全合成及其新型选择性雌激素受体调节剂作用的研究(30973612);不对称氨羟化反应新方法的研究及其在紫杉醇新类似物合成中的应用(20772017)。
3、教育部博士点基金课题1项:四氟多烯紫杉醇新型抗肝癌靶向前药的设计合成及成药性研究(20130071110070)。
4、上海市科委基金课题10项:
优秀学术带头人1项:抗肝癌靶向前药的设计及成药性研究(14XD1400300);
基础研究重点项目3项,包括新型抗结肠癌四氟多烯紫杉醇靶向前药的设计合成及成
药性研究(13JC1401200)、天然产物白藜芦醇二聚体的全合成及其新型选择性雌激素受体调节剂作用的研究(08JC1401600)、面向药物筛选的微流控仿生器官芯片技术研究(17JC1400200,子课题负责人);
生物医药领域科技支撑项目3项,包括治疗溃疡性结肠炎TNFα小分子抑制剂(R)-STU104的临床前研究(21S11907300,2021.8-2024.7)、抗骨质疏松天然Isopaucifloral F-pp磷酸酯一类新药临床前研(17431902500)、新型抗VRE及VRSA感染的万古霉素类二聚体候选药物的合成及成药性研究(13431900101);
生物医药重点科技攻关项目2项,包括新型抗卵巢癌铱配合物的合成及其诱导肿瘤细胞凋亡机制的研究(10431903100)、新型多烯紫杉醇类抗肿瘤化合物的临床前研究(07DZ19713);
上海市中央引导地方科技发展资金项目1项:濒危药材蟾酥中独特疗效物质的高效绿色制造(YDZX20223100001004,2022.9-2025.8,子课题负责人)。
5、上海市卫生局科技发展基金1项:植物雌激素白藜芦醇二聚体类化合物的合成和生物活性研究(054086);
6、上海市经济与信息化委员会2019年度上海市人工智能创新发展项目1项:结直肠癌手术机器人智能导航系统的研发与应用(ZJ6005065,2020.1-2022.12,子课题负责人)。
上海市优秀学术带头人(2014年)
上海市药学会科技奖二等奖(第一完成人,2012年)
荣获复旦大学三八红旗手
复旦大学药学院院长奖
复旦大学药学院“我心目中的好老师”等荣誉
从事药物化学研究近25年,带领科研团队围绕抗肿瘤、抗炎免疫以及抗感染耐药等适应症已发展7个候选药物进入临床前研究。科研成果在国际专业期刊JMC,Chem. Eur. J,OL,EJMC,JOC,OBC等上发表SCI研究论文64余篇,申请发明专利60余项,其中美国PCT专利2项,授权专利29项。作为博士后指导老师,指导博士后5名,期间获国家自然基金青年项目、中国博士后科学基金基金、上海市卫健委临床专项等资助总共7项。近几年以第一通讯作者发表代表性论文如下:
[1] Mei-Lin Tang, Haidong Li, Jin-Feng Ning, Xiaoyan Shen*, and Xun Sun*,Discovery of First-in-Class TAK1–MKK3 Protein–Protein Interaction (PPI) Inhibitor (R)-STU104 for the Treatment of Ulcerative Colitis through Modulating TNF-α Production. J. Med. Chem. 2022, 65, 6690−6709. (IF: 7.446)
[2] Zhipeng Huo, Kunlin Liu, Xi Zhang, Yongxi Liang*, Xun Sun*. Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity. Eur J Med Chem. 2022, 235, 114271. (IF: 6.514)
[3] Jianwu Lu, Xiao Li, Shun Yuan, Yinquan Wang, Han Sun, Weizhao Weng, Yinfei Shi, Xiaoxu Wang, Kongcheng Huang, Xun Sun*, and Taizhi Wu*. Identification, Synthesis, and Comprehension of an Imidazole N-3 Regioisomeric Impurity of Olmesartan Medoxomil Key Intermediate. Org. Process Res. Dev. 2022, 26, 4, 1247–1257.(IF: 3.317)
[4] Wang Xianlian, Xu Yongmei, Zong Zaiwei, Cai Jinna, Chen Chunlin, Zhang Qingwei, Sun Xun*, Li Jianqi*. Design, synthesis and biological evaluation of novel 5-methyl-2,4,5,6-tetrahydropyrrolo [3,4-c] pyrazole derivatives as potent potassium-competitive acid blockers. Bioorganic & Medicinal Chemistry. 2022, 64, 116765.(IF: 3.641)
[5] Zheng-Nan Ren, Jun Yang, Meng-Ya Zhang, Yi-Wen Huang, Dong-Xiao Song, Xun Sun*, Li-Long Pan, Jia Sun. A novel resveratrol analog upregulates sirtuin 1 and inhibits inflammatory cell infiltration in acute pancreatitis. Acta. Pharmacol. Sin., 2022. 43,1624. (IF: 6.15)
[6] Baohui Yuan, He Liu, Xiaoliang Dong, Xiaohua Pan, Xun Sun*, Jia Sun*, Li-Long Pan*. A Novel Resveratrol Analog Upregulates SIRT1 Expression and Ameliorates Neointima Formation. Frontiers in Cardiovascular Medicine 2021, 8, 756098.(IF:6.050)
[7] Jiaxin Huang, Hongyi Wang, Zenong Wu, Xun Sun, Fuli Zhang. Improved synthesis of cenobamate, Chin. J. Med. Chem., 2021, 31, 419-421, 425. (IF: 0.31)
[8] Yi Zhao, Long An, Shupan Guo, Xiaoxing Huang, Huajie Tian, Li Liu, Tao Chen, Xun Sun*, Qibing Mei, Rutao Wang. LMR-101, a novel derivative of propofol, exhibits potent anticonvulsant effects and possibly interacts with a novel target on γ-aminobutyric acid type A receptors. Epilepsia, 2021, 62, 238-249. (IF: 5.864)
[9] Chen-Chen Zhang, Zhi-Peng Huo, Mei-Lin Tang, Yong-Xi Liang*, Xun Sun*. TMSOTf-mediated approach to 1,3-oxazin-2-one skeleton through one-pot successive reduction-[4 + 2] cyclization process of imides with ynamides. Tetrahedron Lett., 2021, https://doi.org/10.1016/j.tetlet.2021.152946
[10] Renwu Lia, Lingling Yan, Xun Sun⁎, Weiping Zheng⁎. A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring Nε-thioacetyl-lysine. Bio. Med. Chem. Lett., 2020, 28, 115356.
[11] Ji-lai Han; Mei-Lin Tang; Xun Sun*. Study on the Total Synthesis of Resveratrol Dimers Quadrangularin A and Pallidol. Chinese J. Org. Chem., 2020, 40(6): 1571-1577.
[12] Yongxi Liang; Mei-Lin Tang; Zhipeng Huo; Chenchen Zhang; Xun Sun*. A Concise Approach to N-substituted Rhodanines through a Base-assisted One-pot Coupling and Cyclization Process. Molecules. 2020, 5, 1138.
[13] Zheng-Yu Liu, Mei-Lin Tang, Jin-Feng Ning, Yun-Peng Hao, Lu Zhou, Xun Sun*. Novel octapeptide-DTX prodrugs targeting MMP-7 as effective agents for the treatment of colorectal cancer with lower systemic toxicity. Eur. J. Med. Chem.2020, 193,112194. (IF:4.833)
[14] Xi-Xi Liu, Mei-Lin Tang, Chen Zhong, Yun Tang, Jian-Ming Yu, Xun Sun*. Design, synthesis and biological evaluation of novel indone derivatives as selective ERβ modulators. Med. Chem. Res.2019, 28, 1010–1026.
[15] Zhi Meng, Mei-Lin Tang, Liting Yu, Yongxi Liang, Jilai Han, ChenChen Zhang, Fupin Hu, Jian-Ming Yu, and Xun Sun*. Novel Mercapto Propionamide Derivatives with Potent New Delhi Metallo-β-Lactamase‑1 Inhibitory Activity and Low Toxicity. ACS Infect. Dis.2019, 5, 903−916.
[16] Liting Yu, Mei-Lin Tang, Chang-Mei Si, Zhi Meng, Yongxi Liang, Jilai Han, and Xun Sun*, Zinc-Mediated Decarboxylative Alkylation of Gem-difluoroalkenes. Org. Lett.2018, 20, 4579−4583.
[17] Yong-Wei Jiang, Liang Xu, Wei Fu, Hua Lin, Jian-Ming Yu, Xun Sun*. Design, synthesis and biological activity of novel demethylvancomycin dimers against vancomycin-resistant enterococcus faecalis. Tetrahedron2018, 74,3527-3533.
[18] Mingliang Wang, Yanjia Fang, Shoulai Gu, Fangfang Chen, Zhengjiang Zhu,Xun Sun*, Jidong Zhu, Discovery of novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors. Eur. J. Med. Chem.2017, 132, 157–172.
[19] Mingliang Wang, Yimin Hu*, Zhe Jiang, Hong C. Shen, Xun Sun*. Divergent copper-mediated dimerization and hydroxylation of benzamides involving C–H bond functionalization. Org. Biomol. Chem., 2016, 14, 4239−4246.
[20] Yun-peng Hao, Zheng-yu Liu, Cheng Xie, Lu Zhou, Xun Sun*. Novel Fluorinated Docetaxel Analogue for Anti-hepatoma:Molecular Docking and Biological Evaluation. Eur. J. Pharm. Sci.2016, 88, 274−281.
[21]Mei-Lin Tang, Chen Zhong, Zheng-Yu Liu, Peng Peng, Xin-Hua Liu*, Xun Sun*. Discovery of novel sesquistilbene indanone analogues as potent anti-inflammatory agents. Eur. J. Med. Chem. 2016, 113, 63–74.
[22] Mei-Lin Tang, Lu Zhou, Jun Chang, Zhuo-Han Hu, Yan Qin*, Xun Sun*. Differential metabolism of 3FDT and docetaxel in RLMs, rats, and HLMs. Eur. J. Med. Chem.2016, 113, 81–91.
[23] Jiao Song, Peng Peng, Jun Chang, Ming-Ming Liu, Jian-Ming Yu, Lu Zhou*, Xun Sun*. Selective non-zinc binding MMP-2 inhibitors: novel benzamide Ilomastat analogs with anti-tumor metastasis. Bioorgan. Med. Chem. Lett.2016, 26, 2174-2178.
[24] Qiang-Sheng Sun, Hua Lin*, Xun Sun, Xing-Wen Sun*, Highly efficient synthesis of enantioenriched fully-substituted spirocyclohexane oxindoles via a Michael-Michael-aldol cascade reaction. Tetrahedron Letters 2016, 57 , 5673–5676.
[25] Wei Tao, Wen Zhou, Zhu Zhou, Chang-Mei Si, Xun Sun, Bang-Guo Wei*, An enantioselective total synthesis of tubulysin V. Tetrahedron, 2016, 72, 5928–5933.
[26] Ge Xu, Baihua Xu, Yanli Song, Xun Sun*, An efficient method for synthesis of bexagliflozin and its carbon-13 labeled analogue, Tetrahedron Letters, 2016, 57, 4684–4687.
[27] Mei-Lin Tang, Peng Peng, Zheng-Yu Liu, Jian Zhang, Jian-Ming Yu and Xun Sun*,Sulfoxide-Based Enantioselective Nazarov Cyclization: Divergent Syntheses of (+)-Isopaucifloral F, (+)-Quadrangularin A, and(+)-Pallidol. Chem. Eur. J.2016, 22, 14535 – 14539.