活性物质发现与适药化研究北京市重点实验室-九游官网下载

科研队伍

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年进入中国医学科学院药物研究所工作,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。

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。

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.

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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