Yan Niu Ph.D.
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, 38 Xueyuan Road, Haidian Disctrict, Beijing, P.R. China, 100191
Tel: ＋86-10-82805281 (Office)
Email: yanniu@bjmu.edu.cn
RESEARCH INTERESTS
1) Design and synthesis of anti-Alzheimer’s disease agents.
2) Design and synthesis of the mitogen-activated protein kinases (MAPK) MEK1 inhibitors as antitumor and antivirus agents.
3) Computer-aided drug design (QSAR, Pharmacophore modeling, molecular docking and de novo design)
4) Fragment-based ligand discovery and drug design
EDUCATIONAL EXPERIENCES
1) 2002 - 2007: Ph.D candidate in Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center
2) 1998 - 2002: B.S. in Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center
RESEARCH EXPERIENCES
1) Aug. 2013 - present: Associate Professor, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, China
2) Jan. 2011 - Apr. 2011: Postdoc., Institute of Pharmacy, University of Innsbruck, Austria
3) Aug. 2007 - Jul. 2013: Lecturer, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, China
RESEARCH PROJECTS
1) Structure based de novo design and synthesis of non-peptidomimetic β-secretase inhibitors as anti-Alzheimer’s disease agnets. Three series of novel fragments, including hexahydropyrimidin-5-ol, benzamidine and 2-aminobenzimidazole, and two novel scaffolds were identified and optimized as novel inhibitors using both ligand and fragment-based docking and virtual screening.
2) Design and synthesis of allosteric inhibitors of the mitogen-activated protein kinases (MAPK) MEK1 as antitumor and antiviral agents.
3) Design, synthesis and biological evaluations of furan-based peptidic proteasome inhibitors as anti-tumor agents.
TEACHING EXPERIENCES
Computer-Aided Drug Design for graduate students;
Medicinal Chemistry for undergraduate students;
Experiments in Medicinal Chemistry for undergraduate, in which phenytoin sodium is synthesized in four steps.
PUBLICATIONS
Peng Liu, Yan Niu,* Chao Wang, Qi Sun, Yaya Zhai, Jiapei Yu,Jing Sun, Fengrong Xu, Gang Yan, Wenjie Huang, Lei Liang, Ping Xu*, 4-Oxo-1,4-dihydroquinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies, European Journal of Medicinal Chemistry. 2014, 79: 413- 421. Chao Wang, Hao Zhang, Fengrong Xu, Yan Niu*, Yun Wu, Xin Wang, Yihong Peng,Jing Sun, Lei Liang and Ping Xu* , Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents, Molecules 2013, 18, 6057-6091
Chao Wang, Fengrong Xu*, Yan Niu*, Yun Wu, Jing Sun, Yihong Peng, Lei Liang, Ping Xu*, Synthesis and Biological Evaluations of 3-Benzothiazol-2-yl Coumarin Derivatives as MEK1 Inhibitors, Letters in Drug Design & Discovery,2013, 10(8): 727-732
Lei Liang; Guanyu Yang; Fengrong Xu; Yan Niu; Qi Sun; Ping Xu*, Copper-Catalyzed Aerobic Dehydrogenation of C-C to C=C Bonds in the Synthesis of Pyridazinones. European Journal of Organic Chemistry, 2013(27), 6130-6136
Liang, L.; Yang, G.; Wang, W.; Xu, F.; Niu, Y.; Sun, Q.; Xu, P*, A Copper-Catalyzed Aerobic Cascade Dehydrogenative– Dehalogenative Reaction, Advanced Synthesis & Catalysis, 2013, 355 (7): 1284-1290
Lei Liang; Wei Wang; Jun Wu; Fengrong Xu; Yan Niu; Bo Xu*; Ping Xu* . Rational Design, Green Synthesis, and Initial Evaluation of a Series of Full-Color Tunable Fluorescent Dyes Enabled by the Copper-Catalyzed N-Arylation of 6-Phenyl Pyridazinones and Their Application in Cell Imaging. Chemistry-A European Journal, 2013, 19(41), 13774-13782
Yan Niu, Haifei Gao, Fengrong Xu, Lei Liang, Peng Liu, Chao Wang, Guanyu Yang, Qi Sun, Ping Xu*, Design, synthesis and in vitro biological evaluation of 3-styrylbenzimidamides as potential BACE1 inhibitors; Letters in Drug Design & Discovery, 2013, 10 (4):297-302
Lei Liang, Wei Wang, Fengrong Xu, Yan Niu, Qi Sun and Ping Xu*, Relay Catalysis by a Multifunctional Cu Catalyst in a Tandem Dehydro-/Dehalogenation Sequence along with N-Arylation; Org. Lett. 2013, 15 (11), 2770–2773
Yan Niu, Haifei Gao, Fengrong Xu, Chao Wang, Peng Liu, Guanyu Yang, Qi Sun, Ping Xu*, Synthesis, in vitro biological evaluation and molecular docking studies of benzimidamides as potential BACE1 inhibitors; Chem Biol Drug Des, 2012, 80: 775–780
Yan Niu, Chao Ma, Hongwei Jin, Fengrong Xu, Haifei Gao, Peng Liu, Yongjian Li, Chao Wang, Guanyu Yang and Ping Xu*, The Discovery of Novel b-Secretase Inhibitors: Pharmacophore Modeling, Virtual Screening, and Docking Studies, Chem Biol Drug Des, 2012, 79:972-80
Hai-Fei Gao, Yan Niu*, Feng-Rong Xu, Lei Liang, Bo Zhou, Yong-Jian Li, Chao Wang, Peng Liu, Ping Xu*, Design and synthesis of benzimidamides as potential BACE1 inhibitors, Journal of Chinese Pharmaceutical Sciences, 2012, 21 (2): 124-131.
Dong Wang, Liguo Yang, Jingjing Su, Yan Niu, Xiaoping Lei, Juan Xiong, Xiaohua Cao, Yinghe Hu, Bing Mei, Jin-Feng Hu, Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline, Biochemical and Biophysical Research Communications 410 (2011) 229–234
YongJian Li, FengRong Xu, Yan Niu, XiaoMin Zou, Yue Yuan, HaiFei Gao, Chao Wang, GuanYu Yang, Qi Sun, Ping Xu*. Efficient synthesis of terminal α,β-unsaturated ketones as the intermediates of the proteasome epoxyketone inhibitors via Weinreb amide. Journal of Chinese Pharmaceutical Sciences. 2011, 20: 564-71
Yan Niu, Yuehua Wang, Xiaomin Zou, Xiaoming Yang, Chao Ma, Yang Lü, Bo Zhou, Yue Yuan, Guanhua Du and Ping Xu*. Synthesis and preliminary evaluation of peptidomimetic inhibitors of human β-secretase. European Journal of Medicinal Chemistry. 2010, 45: 2089-2094.
Wen Si, Xuliang Zhang, Yan Niu, Huiting Yu, Xiaoping Lei, Huanxin Chen, Xiaohua Cao, A novel derivative of xanomeline improves fear cognition in aged mice, Neuroscience Letters, 473 (2010): 115–119
Yue Yuan, XiaoMin Zou, Yan Niu, FengRong Xu, Ke Mou, Bo Zhou, Chao Wang, YongJian Li, GuanYu Yang, Ping Xu *.Synthesis of acyclic analogs of Syringolin A as potential 20S proteasome inhibitors. Journal of Chinese Pharmaceutical Sciences: 19 (2010) 423–435
7. Bo Zhou, Yan Niu, Xiao-Min Zou, Feng-Rong Xu, Yue Yuan, Chao Wang, Hai-Fei Gao, Peng Liu, Ping Xu*, Structure-based design of hexahydropyrimidin-5-ols as novel non-peptidic β-secretase inhibitors, Journal of Chinese Pharmaceutical Sciences, 2010, 19 (5): 391-400
Wen Lv, Wei Lv, Niu Yan, Lei Xiao-Ping*, Homology modeling and molecular docking on muscarinic M1 Receptor, Acta Physico-Chimica Sinica. 2009, 25(7): 1259-1266
Yihui Cui, Dong Wang, Wen Si, Wen Lv, Yan Niu, Xiaoping Lei, Yinhe Hu, Xiaohua Cao*, Enhancement of memory function in aged mice by a novel derivative of xanomeline, Cell Research (2008) 18: 1151–1153
PATENTS
Ping Xu, Yan Niu, Peng Liu, Fengrong Xu, Lei Liang, Preparation and applications of β-secretase inhibitors. Chinese Patent, Application No. 2013013006.6
Ping Xu, Yihong Peng, Chao Wang, Yan Niu, Hao Zhang, Fengrong, Xu, Preparation an applications of MEK kinase inhibitors. Chinese Patent, Application No. 201210440137.X
LEI Xiao-Ping, LU Wen, NIU Yan, et al. Substituted pyridines as muscarinic M1 receptor agonists, preparation and application. Chinese Patent , CN1821243A
