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研究员

刘站柱

职 称:研究员

所属科室:合成药物化学研究室

导师类别:博士生导师

联系方式:liuzhanzhu@www.myhortonhome.com
010-63165253

所属重点实验室:天然药物活性物质与功能国家重点实验室
活性物质发现与适药化研究北京市重点实验室

个人简介

刘站柱 博士,研究员,博士生导师,北京协和医学院优秀教师。本科、硕士毕业于北京大学化学系,博士毕业于北京协和医学院。1990年在河北省药物所工作,后赴美国Georgia Institute of Technology化学与生物学院进修,2002年进入bobapp官方下载 工作,先后任副研究员、研究员,课题组长,2005年聘任为博士生导师。兼任所学术委员会委员,《化学快报》编委。主要从事创新药物的研发、天然产物全合成、有机合成方法学等方面的工作。主持多项国家自然科学基金、国家新药创制重大专项、北京市科研基金、中国医学科学院医学与健康科技创新工程。历年来发表研究论文70余篇,申请发明专利10余项,获得专利授权3项。培养研究生20余名。

研究方向

1. 创新药物的研究与开发 以具有强生物活性的天然产物为结构先导物,利用全合成手段,设计、合成具有生物活性的结构类似物,以期能够发现具有自主知识产权的创新药物。针对抗肿瘤、抗代谢性疾病、抗菌等疾病领域开展创新药物研究工作,已有1个降糖药物完成临床前研究。 2. 生物活性天然产物全合成 致力于建立高效的天然产物全合成方法,解决天然产物来源,为后续结构改造奠定基础。已完成多个复杂活性天然产物全合成,包括具有强抗肿瘤活性的(-)-renieramycin G、(-)-saframycin A、(-)-jorumycin、ceratamine A、(±)-parthenolide以及具有强抗菌活性的griseofamines等。 3. 有机合成方法学研究 开发高效的有机化学合成新方法,包括基于苯炔化学构建药物化学常见骨架、使用有机小分子实现常见有机反应的不对称催化等。

发表论文

1. Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors, Junmin Dong, Xuan Pan, Ying Yang, Guangyan Zhang, Zhiyan Xiao, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2021, 223, 113631-113645.
2. An improved total synthesis of griseofamine A, Xuan Pan‡, Rui Yu‡, Zhanzhu Liu*,Tetrahedron Letters, 2021, 67, 152894-152895.
3. Synthesis and cytotoxicity of (−)-homorenieramycin G and its derivatives, Yantao Ma, Xuan Pan*, Baohe Guan, Guangyan Zhang, Zhanzhu Liu*, Organic & Biomolecular Chemistry, 2020, 18, 9883-9894.
4. Design, synthesis and cytotoxicity of novel hexacyclic saframycin–ecteinascidin analogs, Xiangran Lu, Xuan Pan, Baohe Guan, Zhanzhu Liu*, Organic & Biomolecular Chemistry, 2020, 18, 237-249.
5. Regioselective bromination of 6-hydroxytetrahydroisoquinolines, Ke Wang, Xuan Pan, Kun Peng, Zhanzhu Liu*, Journal of Heterocyclic Chemistry, 2020, 1-4.
6. Total synthesis and antibacterial activity evaluation of griseofamine A and 16-epi-griseofamine A, Xuan Pan, Zhanzhu Liu*, Organic Letters, 2019, 21(7), 2393-2396.
7. A novel specific peroxisome proliferator-activated receptor γ (PPARγ) modulator YR4-42 ameliorates hyperglycaemia and dyslipidaemia and hepatic steatosis in diet-induced obese mice, Yi Huan‡, Xuan Pan‡, Jun Peng, Chunming Jia, Sujuan Sun, Guoliang Bai, Xing Wang, Tian Zhou, Rongcui Li, Shuainan Liu, Caina Li, Quan Liu, Zhanzhu Liu*, Zhufang Shen*, Diabetes Obesity & Metabolism, 2019, 2553-2563.
8. A concise synthesis of (E)-3-aryl-2,3,4,5-tetrahydro-1H-3-benzazonines by aryne induced [2,3] Stevens rearrangement of 1,2,3,4-tetrahydroisoquinolines, Xuan Pan‡, Yantao Ma‡, Zhanzhu Liu*, Organic & Biomolecular Chemistry, 2018, 16(40), 7393-7399.
9. Synthesis of 3-aryl-3-benzazepines via aryne [1,2] Stevens rearrangement of 1,2,3,4-tetrahydroisoquinolines, Xuan Pan, Zhanzhu Liu*, Organic Chemistry Frontiers, 2018, 5(11), 1798-1810.
10. Synthesis and cytotoxicity of novel imidazo[4,5-d]azepine compounds derived from marine natural product ceratamine A, Xuan Pan‡, Lulu Tao‡, Ming Ji, Xiaoguang Chen, Zhanzhu Liu*, Bioorganic & Medicinal Chemistry Letters, 2018, 28(5), 866-868.
11. Asymmetric synthesis of highly functionalized tyrosine derivatives for the construction of bistetrahydroisoquinoline alkaloids, Enming Du, Xuan Pan, Baohe Guan, Zhanzhu Liu*, Tetrahedron Letters, 2018, 59(31), 3029-3032.
12. Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings, Zhaozhu Sun, Tian Zhou, Xuan Pan, Ying Yang, Yi Huan, Zhiyan Xiao, Zhufang Shen*, Zhanzhu Liu*, Bioorganic & Medicinal Chemistry Letters, 2018, 28(18), 3050-3056.
13. Synthesis and cytotoxicity of a novel series of saframycin-ecteinascidin analogs containing tetrahydro-β-carbboline moieties, Xiangran Lu, Xuan Pan, Ying Yang, Ming Ji, Xiaoguang Chen, Zhiyan Xiao, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2017, 135(28), 260-269.
14. Effective synthesis and cytotoxicity of novel microtubule-stabilizing agent ceratamine A analogues, Lulu Tao, Xuan Pan**, Ming Ji, Xiaoguang Chen, Zhanzhu Liu*, Tetrahedron, 2017, 73(15), 2159-2171.
15. Stereoselective total synthesis of (±)-parthenolide and (±)-7-epiparthenolide, Liang Li, Xuan Pan, Baohe Guan, Zhanzhu Liu*, Tetrahedron, 2016, 72, 4346-4354.
16. Synthesis and biological evaluation of novel tetrahydroisoquinoline-C-aryl glucosides as SGLT2 inhibitors for the treatment of type 2 diabetes, Xuan Pan, Yi Huan, Zhufang Shen, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2016, 114, 89-100.
17. Synthesis of indolo[2,3-a]pyrrolo[3,4-c]carbazoles via the oxidative cyclization of bisindolylmaleimides with Pd(TFA)2/Cu(OAc)2, Xuan Pan, Ke Wang, Baohe Guan, Zhanzhu Liu*, Journal of Heterocyclic Chemistry, 2015, 52, 911-913.
18. Asymmetric total synthesis of three stereoisomers of (-)-renieramycin G and their cytotoxic activities, Enming Du, Wenfang Dong, Baohe Guan, Xuan Pan, Zheng Yan, Li Li, Nan Wang, Zhanzhu Liu*, Tetrahedron, 2015, 71, 4296-4303.
19. The preparation of novel chiral auxiliaries SAMIQ/RAMIQ and their application in the asymmetric Michael addition, Xuan Pan, Zhanzhu Liu*, Tetrahedron, 2014, 70, 4602-4610.
20. Synthesis and cytotoxic activities of a series of novel N-methyl-bisindolylmaleimide amide derivatives, Ke Wang, Zhanzhu Liu*, Journal of Asian Natural Products Research, 2014, 3, 296-303.
21. Total synthesis of microtubule-stabilizing agent Ceratamine A, Qiguo Feng, Lulu Tao, Zhanzhu Liu*, The Journal of Organic Chemistry, 2013, 78, 12814-12818.
22. Synthesis and cytotoxicity of dinuclear platinum (II) complexes of (1S,3S)-1,2,3,4-tetrahydroisoquinolines, Geng Xu, Ju Guo, Zheng Yan, Nan Wang, Zhanzhu Liu*, Chinese Chemical Letters, 2013, 24, 186-188.
23. Synthesis and cytotoxicity of 3-aryl acrylic amide derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa, Ju Guo, Wenfang Dong, Wei Liu, Zheng Yan, Nan Wang, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2013, 62, 670-676.
24. Synthesis and cytotoxic activities of a series of novel N-methyl-bisindolylmaleimide amino acid ester conjugates, Ke Wang, Zheng Yan, Nan Wang, Zhanzhu Liu*, Chinese Chemical Letters, 2012, 23, 462-465.
25. Total synthesis and cytotoxicity of (-)-jorumycin and its analogues, Wei Liu, Xiangwei Liao, Wenfang Dong, Zheng Yan, Nan Wang, Zhanzhu Liu*, Tetrahedron, 2012, 68, 2759-2764.
26. Asymmetric synthesis and cytotoxicity of (-)-saframycin A analogues, Wenfang Dong, Wei Liu, Zheng Yan, Xiangwei Liao, Baohe Guan, Nan Wang, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2012, 49, 239-244.
27. Asymmetric total synthesis of (-)-saframycin A from L-tyrosine, Wenfang Dong, Wei Liu, Xiangwei Liao, Baohe Guan, Shizhi Chen, Zhanzhu Liu*, The Journal of Organic Chemistry, 2011, 76, 5363–5368.
28. Synthesis and cytotoxicity of (-)-renieramycin G analogues, Wei Liu, Wenfang Dong, Xiangwei Liao, Zheng Yan, Baohe Guan, Nan Wang, Zhanzhu Liu*, Bioorganic & Medicinal Chemistry Letters, 2011, 21, 1419-1421.
29. Synthesis of an Isomer of the Renieramycin Skeleton from L-Tyrosine, Wei Liu, Wen Fang Dong, Xiang Wei Liao, Bao He Guan, Zhan Zhu Liu*, Journal of Heterocyclic Chemistry, 2011, 48, 414-418.
30. Synthesis and cytotoxicity of cis-dichloroplatinum (II) complexes of (1S,3S)-1,2,3,4-tetrahydroisoquinolines, Geng Xu, Zheng Yan, Nan Wang, Zhanzhu Liu*, European Journal of Medicinal Chemistry, 2011, 46, 356-363.

专著

专利

1. 一类抗肿瘤天然产物ecteinascidins结构类似物的制备和医药用途,刘站柱,陈晓光,鲁向冉,潘璇,季鸣,贯宝和,专利号:ZL201810298367.4,授权公告日:2021年04月13日。
2. 一类IDO1抑制剂的制备和用途,刘站柱,潘璇,董俊敏,张广艳,贯宝和,申请号:202110313379.1,申请日:2021年03年24日。
3. 一类四氢异喹啉化合物及其盐的制备和医药用途,刘站柱,申竹芳,于然,贯宝和,彭军,潘璇,刘泉,刘率男,孙素娟,李彩娜,孙兆柱,贾春明,姜茜,王悦,周艳丽,专利号:ZL201611207052.1,授权公告日:2021年04月13日。
4. 一类含中环四氢咔啉-四氢异喹啉化合物的制备和用途,刘站柱,马艳涛,潘璇,贯宝和,张广艳,于瑞,申请号:202010258549.6,申请日:2020年04年03日。
5. 一类含中环的Renieramycin G衍生物的制备和用途,刘站柱,马艳涛,潘璇,贯宝和,张广艳,于瑞,申请号:202010229704.1,申请日:2020年03年27日。
6. 钠糖共转运体2抑制剂、其制法和其药物组合物与用途,刘站柱,申竹芳,潘璇,环奕,刘泉,王悦,专利号:ZL201410218852.8,授权公告日:2019年07月02日。
7. 一类四氢咔啉-四氢异喹啉化合物的制备和医药用途,刘站柱,陈晓光,鲁向冉,潘璇,季鸣,贯宝和,申请号:201811266399.2,申请日:2019年05月07日。
8. GPR40受体激动剂、其制法和其药物组合物与用途,刘站柱,申竹芳,孙兆柱,潘璇,周甜,环奕,贯宝和,申请号:201810234530.0,申请日:2018年03月21日。
9. 一类抗肿瘤海洋天然产物ecteinascidins的结构类似物,刘站柱,陈晓光,董文芳,刘伟,廖祥伟,王晔,贯宝和,申请号:PCT/CN2011/075920,申请日:2012年12月27日。
10. 一类抗肿瘤海洋天然产物ecteinascidins的结构类似物,刘站柱,陈晓光,董文芳,刘伟,廖祥伟,王晔,贯宝和,申请号:2010101261284,申请日:2010年03月15日。

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