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芦逵,男,博士,教授,博士生导师。天津科技大学食品营养与安全和药物化学国际科技合作基地副主任。入选天津市“131”创新人才培养工程第二层次。2002年本科毕业于中国农业大学应用化学系,2007年博士毕业于北京大学化学与分子工程学院。同年赴美国加利福尼亚大学洛杉矶分校化学与生物化学系从事博士后研究。2008年回国,就职于国际知名医药外包公司(PPD)旗下的保诺科技(北京)有限公司。期间担任药物化学课题组长,带领十几人的研究团队从事抗肿瘤,抗丙肝和抗艾滋病的新药开发。2011年加入yh1187银河网站。

 

主讲课程

本科生课程:药物合成反应,药物合成反应实验

研究生课程:药物合成与设计,近代有机合成基础

 

主要教学研究及成果情况

参与了一门天津市专业学位优秀课程和一门校一流课程的建设;

指导完成一项国家级和一项校级大创项目;

指导研究生获得天津科技大学优秀硕士论文2

2016年天津科技大学“一帮一”先进个人;

指导的研究生多次获得国家奖学金和一等研究生学业奖学金

 

科研领域及方向

[1]药物合成化学:治疗糖尿病、流感、肿瘤等疾病的小分子药物的设计、化学合成、结构修饰和构效关系研究。具有生物活性的天然产物的合成和结构修饰

[2]有机合成化学:合成含氟和含硫有机化合物的新方法研究

[3]化学生物学:利用正向化学遗传学的方法来寻找具有生物活性的天然产物的作用靶点

 

科研情况

[1] 国家自然科学基金面上项目:正向化学遗传学方法寻找天然产物Plicamine的抗肿瘤作用靶点研究 (主持人) 2021-2024

[2] 国家自然科学基金青年项目:1,4-加成类型的Ugi反应及其在多样性导向合成中的应用研究 (主持人) 2013-2015

[3] 科技部国际交流项目:中法杰出青年交流项目 (主持人)2017

[4] 天津市高等学校科技发展基金项目新型苯二氮卓类化合物的多样性导向合成研究 (主持人) 2013-2015

[5] 横向项目:若干含硫鬼臼毒素衍生物的合成 (主持人)2021-2022

[6] 横向项目:若干含氟奥司他韦衍生物的合成和工艺开发 (主持人)2020-2022

 

主要学术成果

发表SCI论文40余篇,其中以第一作者或通讯作者发表论文30余篇,其中一区8篇,二区13篇,总影响因子超过100

代表性论文如下:

[1] Metal-Free Difluoromethylselenolation of Arylamines Under Visible-light Photocatalysis. Kui Lu,* Quan Li,  Xiaolan Xi, Ting Zhou, and Xia Zhao*, J. Org. Chem., 2020, 85, 1224.

[2] Synthesis of a-Trifluoromethyl Ethanone Oximes via the Three-component Reaction of Aryl-substituted Ethylenes, tert-Butyl Nitrite, and the Langlois Reagent. Kui Lu,* Xianfu Wei, Quan Li, Yuxuan Li, Liangshuo Ji, Erbing Hua,* Yujie Dai and Xia Zhao*, Org. Chem. Front, 2019, 6, 3766.

[3] Total Synthesis of Wikstrol A and Wikstrol B. Kui Lu,* Ming Li, Yuna Huang, Yuanyuan Sun, Zhi Gong, Qijun Wei, Xia Zhao, Yongmin Zhang* and Peng Yu*, Org. Biomol. Chem. 2019, 17, 8206.

[4] Synthesis & α-glucosidase inhibitory & glucose consumption-promoting activities of flavonoid-coumarin hybrids. Hua Sun, Xiaotong Song, Yunchang Tao, Ming Li, KeYang, Hang Zheng, Zongxin Jin, Robert H Dodd, Guojun Pan, Kui Lu* and Peng Yu*, Future Med. Chem. 2018, 10, 1055.

[5] Synthesis and cytotoxic studies of novel 5-phenylisatin derivatives and their anti-migration and anti-angiogenic evaluation. Qian Zhang, Yuou Teng, Yuan Yuan, Tingting Ruan, Qi Wang, Xing Gao, Yao Zhou, Kailin Han, Yonmin Zhang, Peng Yu*and Kui Lu* Eur. J. Med. Chem. 2018, 156, 800.

[6] Copper-catalyzed Direct Trifluoromethylthiolation of Indoles by tert-Butyl 2-((trifluoromethyl)sulfonyl)hydrazine-1-carboxylate. Kui Lu,* Quan Li, Xiaolan Xi, Yuna Huang, Zhi Gong, Peng Yu and Xia Zhao*, Org. Chem. Front, 2018, 5, 3088.

[7] One-pot Synthesis of β-lactams by Ugi and Michael addition Cascade Reaction. Xing Gao, Chunhui Shan, Zhihao Chen, Yan Liu, Xia Zhao, Ao Zhang, Peng Yu,a Hervé Galons,* Yu Lan* and Kui Lu*, Org. Biomol. Chem. 2018, 16, 6096.

[8] Transition-Metal-Free Direct Trifluoromethylthiolation and Trifluoromethylsulfoxidation of Electron-rich Aromatics with CF3SO2Na in the presence of PCl3. Xia Zhao*, Aoqi Wei, Bo Yang, Tianjiao Li, Quan Li, Di Qiu and Kui Lu*, J. Org. Chem., 2017, 82, 9175.

[9] Synthesis and anti-oxidant activity evaluation of (±)-Anastatins A, B and their analogs. Guojun Pan, Xuehui Li, Long Zhao, Meng Wu, Chao Su, Xuzhe Li, Yongmin Zhang, Peng Yu, Yuou Teng* and Kui Lu *, Eur. J. Med. Chem. 2017, 138, 577.

[10] Synthesis of 6-hydroxyaurone analogues and evaluation of their α-glucosidase inhibitory and glucose consumption-promoting activity: Development of highly active 5, 6-disubstituted derivatives. Hua Sun, Weina Ding, Xiaotong Song, Dong Wang, Mingzhu Chen, Kaili Wang, Yazhou Zhang, Peng Yuan, Ying Ma, Runling Wang, Robert H. Dodd, Yongmin Zhang, Kui Lu* and Peng Yu*, Bioorg. Med. Lett. 2017, 27, 3226

[11] Total Synthesis of I3,II8-Biapigenin and Ridiculuflavone A. Kui Lu,* Ke Yang, Xiaoliang Jia, Xing Gao, Xia Zhao, Guojun Pan, Yantao Ma, Qiyao Huang and Peng Yu*, Org. Chem. Front, 2017, 4, 578

[12] Transition-Metal Free Direct Difluoromethylthiolation of Electron-Rich Aromatics with Difluoromethanesulfonyl Chloride. Xia Zhao,* Aoqi Wei, Tianjiao Li, Zhiyang Su, Jun Chen, and Kui Lu*, Org. Chem. Front, 2017, 4, 232.

[13] Transition Metal-Free Direct Trifluoromethylthiolation of Indoles using Trifluoromethanesulfonyl Chloride in the Presence of Triphenylphosphine. Kui Lu,* Zhijie Deng, Ming Li, Tianjiao Li and Xia Zhao*, Org. Biomol. Chem. 2017, 15, 1254.

[14] Synthesis and antioxidant evaluation of desmethylxanthohumol analogs and their dimers. Yuou Teng, Xuzhe Li, Ke Yang, Xuehui Li, Zijun Zhang, Luyao Wang, Zhijie Deng, Binbin Song, Zhihong Yan, Yongmin Zhang, Kui Lu,* and Peng Yu*, Eur. J. Med. Chem. 2017, 125, 335

[15] 1,4-Addition Ugi Reaction Using Cyclic α,β-Unsaturated Ketone as Substrate. Kui Lu,* Yantao Ma, Meile Gao, Yan Liu, Ming Li, Chuanming Xu, Xia Zhao,* and Peng Yu*, Org. Lett. 2016, 18, 5038.

[16] Iodine-catalysed regioselective thiolation of flavonoids using sulfonyl hydrazides as sulfenylation reagents. Xia Zhao*, Zhijie Deng, Aoqi Wei, Boyang Li and Kui Lu*, Org. Biomol. Chem. 2016, 14, 7304.

[17] Synthesis of Substituted Pyrroles via Copper-catalyzed Cyclization of Ethyl Allenoates with Activated Isocyanides. Kui Lu*, Fang Ding, Long Qin, Xiaoliang Jia, Chuanming Xu, Xia Zhao, Qingwei Yao and Peng Yu*, Chem-Asian. J. 2016, 11, 2121.

[18] Total synthesis of 8-(6-umbelliferyl)-apigenin and its analogs as anti-diabetic reagents. Guojun Pan, Lianbo Zhao, Na Xiao, Ke Yang, Yantao Ma, Xia Zhao, Zhenchuan Fan, Yongmin Zhang, Qingwei Yao, Kui Lu* and Peng Yu*, Eur. J. Med. Chem. 2016, 122, 674.

[19] Iodine-catalyzed thiolation of electron-rich aromatics using sulfonyl hydrazides as sulfenylation reagents Xia Zhao*, Tianjiao Li, Lipeng Zhang, and Kui Lu*, Org. Biomol. Chem. 2016, 14, 1131.

[20] Mitochondrial Ca2+ uptake by the voltage-dependent anion channel 2 regulates cardiac rhythmicity. Hirohito Shimizu, Johann Schredelseker, Jie Huang, Kui Lu, Shamim Naghdi, Fei Lu, Sarah Franklin, Hannah DG Fiji, Kevin Wang, Huanqi Zhu, Cheng Tian, Billy Lin, Haruko Nakano, Amy Ehrlich, Junichi Nakai, Adam Z Stieg, James K Gimzewski, Atsushi Nakano, Joshua I Goldhaber, Thomas M Vondriska, György Hajnóczky, Ohyun Kwon, Jau-Nian Chen* elife 2015, 4 (Co-fisrt author)

[21] Synthesis of 2-Aryl and 3-Aryl Benzo[b]furan Thioethers Using Aryl Sulfonyl Hydrazides as Sulfenylation Reagents. Xia Zhao*, Lipeng Zhang, Xiaoyu Lu, Tianjiao Li and Kui Lu*, J. Org. Chem., 2015, 80, 2918-2924.

[22] p-Toluenesulphonic acid-promoted, I2-catalysed sulphenylation of pyrazolones with aryl sulphonyl hydrazides. Xia Zhao*, Lipeng Zhang, Tianjiao Li, Guiyan Liu, Haomeng Wang and Kui Lu*, Chem. Commun., 2014, 50, 13121-13123.

[23] Development of a Concise and Diversity-Oriented Approach for the Synthesis of Plecomacrolides via the Diene-Ene RCM. Kui Lu, Mengwei Huang, Zheng Xiang, Yongxiang Liu, Jiahua Chen* and Zhen Yang*, Org. Lett., 2006, 8, 1193-1196.

[24] A Concise and Diversity-Oriented Strategy for the Synthesis of Benzofurans and Indoles via Ugi and Diels-Alder Reactions. Kui Lu, Tuoping Luo, Zheng Xiang, Reza Fathi*, Jiahua Chen* and Zhen Yang*, J. Comb. Chem., 2005, 7, 958-967.

 

 

授权发明专利:

1) 天然黄酮Anastatin B的衍生物及制备和应用

2) 一种合成25-二羰基哌嗪类化合物的方法

3) 一类2,3,4-三取代吡咯类化合物及其合成方法

4)  由a-酮戊二酸到戊二酸合成的方法

5) 256-三取代-32H-苯并呋喃酮类衍生物及应用

6) 一种香豆素取代黄酮类化合物的制备及其在制备抗糖尿病药物中的应用

7) 应用交叉偶联反应合成硫代苯并呋喃类化合物的新方法

获奖情况

葛兰素史克公司合成金奖 2009年2010年

联系方式

办公地点:天津经济技术开发区第十三大街29号yh1187银河网站(300457)

办公电话:022-60912562; 实验室电话:022-60912590

Email: lukui@tust.edu.cn

 

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