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周啟璠
研究助理教授
研究助理教授
zhouqf@sustech.edu.cn

周啟璠,浙江臺州人,現任南方科技大學格拉布斯研究院研究助理教授(副研究員),生物技術副高級工程師。2019年于沈陽藥科大學獲得藥物化學專業博士學位,師從陳國良教授,并榮獲國家獎學金。主要從事腫瘤、病毒和炎癥相關疾病的小分子創新藥物研究與開發。于2020年加入南方科技大學張緒穆教授課題組,作為項目骨干完成新型口服抗新冠藥物SHEN26的臨床前研究工作,目前已完成III期臨床試驗進入上市申請階段。以一作(含共一)或通訊在STM, STTT, EJMC, JOC等期刊發表SCI文章20余篇,申請發明專利20余項,其中作為主要發明人獲得中國專利授權10項。


研究領域:

1. 基于病毒共性靶標的小分子藥物開發;

2. 發展基于新機制、新靶點的抗腫瘤、抗炎和抗病毒小分子抑制劑


學術成果:

  1. Yongzhi Chen1, Kunyu Lu1, Binhao Rong1, Yuanmei Wen, Guanguan Li, Shuo Li, Deyin Guo, Qifan Zhou*, Shuwen Liu*, Xumu Zhang*. Discovery of Novel Thiophene-Based Baloxavir Derivatives as Potent Cap-Dependent Endonuclease Inhibitors for Influenza Treatment. Journal of Medicinal Chemistry, 2024, https://doi.org/10.1021/acs.jmedchem.4c01979.

  2. Fan Pan1, Qifan Zhou*,1, Ming Yan1, Sidi Yang1, Ruiyu Hu, Yongzhi Chen, Yuanmei Wen, Yang Chao, Cailing Xie, Weixin Ou, Yingjun Li, Hongmin Zhang*, Deyin Guo*, Xumu Zhang*. Development of pyrimidone derivatives as nonpeptidic and noncovalent 3-chymotrypsin-like protease (3CLpro) inhibitors with anti-coronavirus activities. Bioorganic Chemistry, 2024, 154, 107988.

  3. Yongzhi Chen1, Qifan Zhou**,1, Fan Pan, Binhao Rong, Renwei Xiao, Yuanmei Wen, Jingyuan Song, Zhengchao Tu, Shuwen Liu****, Yingjun Li***, Xumu Zhang*. Synthesis and anti-influenza virus activity of substituted dibenzoxepine-based baloxavir derivatives. European Journal of Medicinal Chemistry, 2024, 280, 116922.

  4. Qishu Chen1, Qifan Zhou1,*, Sidi Yang1, Fan Pan, Hongqi Tao, Yuanmei Wen, Yang Chao, Cailing Xie, Weixin Ou, Deyin Guo*, Yingjun Li*, Xumu Zhang*. Identification of adenosine analogues as nsp14 N7?methyltransferase inhibitors for treating coronaviruses infection. Bioorganic Chemistry, 2024, 153, 107894.

  5. Qishu Chen1, Qifan Zhou1, Guanguan Li, Shuo Li, Yingjun Li* and Xumu Zhang*. Optimized kilogram-scale synthesis and impurity identification of SHEN26 (ATV014) for treating COVID-19. Organic Process Research & Development. 2024, 28, 2188-2195.

  6. Qifan Zhou1, Sidi Yang1, Liu Cao1, Yang Yang1, Tiefeng Xu, Qishu Chen, Hongzhou Lu, Yingjun Li*, Deyin Guo*, Xumu Zhang*. Preclinical characterization of SHEN26, an oral cyclohexanecarboxylate prodrug of 1′-CN-4-aza-7,9-dideazaadenosine C-nucleoside for the treatment of SARS-CoV-2. Signal Transduction and Targeted Therapy, 2023, 8, 27. 

  7. Qifan Zhou1, Yinzhu Luo1, Yujun Zhu1, Qishu Chen, Jingfei Qiu, Feng Cong*, Yingjun Li*, Xumu Zhang*. Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses. European Journal of Medicinal Chemistry, 2023, 249.

  8. Liu Cao1, Yingjun Li1, Sidi Yang1, Guanguan Li1, Qifan Zhou1, Jing Sun1, et al. The adenosine analogue prodrug ATV006 is orally bioavailable and has potent preclinical efficacy against SARS-CoV-2 and its variants. Science Translational Medicine, 2022, 14, eabm7621. 

  9. Qifan Zhou, Lina Jia, Fangyu Du, Xiaoyu Dong, Wanyu Sun, Lihui Wang, Guoliang Chen*. Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents. New Journal of Chemistry, 2020, 44, 2247-2255. 

  10. Fangyu Du1, Qifan Zhou1, Wenjiao Sun, Cheng Yang, Chunfu Wu, Lihui Wang* and Guoliang Chen*. 5-Hydroxyindole-based EZH2 inhibitors assembled via TCCA-catalyzed condensation and Nenitzescu reactions. Molecules, 2020, 25, 2059–2083.

  11. Qifan Zhou, Fangyu Du, Yuanguang Chen, Yang Fu, Wenjiao Sun, Ying Wu, Guoliang Chen*. L-(-)-Quebrachitol as a ligand for selective copper (0)-catalyzed N?arylation of nitrogen-containing heterocycles. Journal of Organic Chemistry, 2019, 84, 8160–8167. 

  12. Qifan Zhou, Fangyu Du, Yuanguang Chen, Yang Fu, Guoliang Chen*. “On Water” promoted N-arylation reactions using Cu (0)/myo-inositol catalytic system. Tetrahedron Letters, 2019, 60, 1938–1941. 

  13. Chunling Yuan1, Xiaoli Guo1, Qifan Zhou1, Fangyu Du, Xiaoyu Zhou, Peng Liu, Tianyan Chi, Xuefei Ji, Jinheng Gao, Chengwen Chen, Hongli Lang, Jia Xu, Danyang Liu, Yang Yang, Shimeng Qiu, Guoliang Chen* and Libo Zou*. OAB-14, a novel small molecule, improves Alzheimer’s disease-related pathologies and cognitive impairments by increasing -amyloid clearance in APP/PS1 mice. BBA-Molecular Basis of Disease, 2019, 1865, 161–180. 

  14. Yajie Shi1, Qifan Zhou1, Fangyu Du, Yang Fu, Yang Du, Ting Fang and Guoliang Chen*. Iridium-catalyzed intramolecular C-N and C-O/S cross-coupling reactions: Preparation of benzoazole derivatives. Tetrahedron Letters, 2019, 60, 151082–151090. 

  15. Fangyu Du1, Qifan Zhou1, Yang Fu, Yuanguang Chen, Ying Wu* and Guoliang Chen*. Copper(II)-catalyzed C–N coupling of aryl halides and N-nucleophiles promoted by quebrachitol or diethylene glycol. Synlett, 2019, 30, 2161–2168. 

  16. Fangyu Du1, Qifan Zhou1, Yang Fu, Hanqi Zhao, Yuanguang Chen and Guoliang Chen*. tert-Butyl(3-cyano-4,6-dimethylpyridin-2-yl)carbonate as a green and chemoselective N–tert-butoxycarbonylation reagent. New Journal of Chemistry, 2019, 43, 6549–6554. 

  17. Fangyu Du, Qifan Zhou, Xiaoxiao Fu, Yajie Shi, Yuanguang Chen, Wuhong Fang, Jingyu Yang* and Guoliang Chen*. Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents. RSC Advances, 2019, 9, 2498–2508. 

  18. Fangyu Du, Qifan Zhou, Wenjiao Sun and Guoliang Chen*. Targeting cancer stem cells in drug discovery: Current state and future perspectives. World Journal of Stem Cells, 2019, 11, 398–420. 

  19. Fangyu Du, Qifan Zhou, Yajie Shi, Miao Yu, Wenjiao Sun and Guoliang Chen*. Synthesis of regorafenib through novel preparation of the intermediate 4-amino-3-fluorophenol via fries and Beckman rearrangements. Synthetic Communications, 2019, 49, 576–586. 

  20. Caijiao Wu1, Qifan Zhou1, Dake Song, Hui Li, Changshun Bao, Xuelong Liu, Xuefei Bao and Guoliang Chen*. An improved process for the preparation of pimavanserin tartrate. Journal of Chemical Research, 2019, 43, 480-485. 

  21. Qifan Zhou, Chen Peng, Fangyu Du, Linbo Zhou, Yajie Shi, Yang Du, Dongdong Liu, Wenjiao Sun, Meixia Zhang*, Guoliang Chen*. Design, synthesis and activity of BBI608 derivatives targeting on stem cells. European Journal of Medicinal Chemistry, 2018, 151, 39-50. 

  22. Qifan Zhou, Fangyu Du, Xinjie Liang, Wenqiang Liu, Ting Fang and Guoliang Chen*. Zinc (II)-mediated selective O-benzylation of 2-oxo-1,2-dihydropyridines systems. Molecules, 2018, 23, 1784-1798. 

  23. Qifan Zhou, Fangyu Du, Yajie Shi, Wenqiang Liu, Dongdong Liu and Guoliang Chen*. An efficient protocol for the production of pymetrozine via a new synthetic strategy. Journal of Chemical Research, 2018, 42, 395-446. 

  24. Qifan Zhou, Fangyu Du, Yajie Shi, Ting Fang, Guoliang Chen*. The synthesis and analysis of 1-methyl-4-phenyl-1H-imidazol-2-amine and by-products. Journal of Chemical Research, 2018, 42, 608–610. 

  25. Fangyu Du, Qifan Zhou, Dongdong Liu, Ting Fang, Yajie Shi, Yang Du, Guoliang Chen*. Dimerization of aromatic compounds using palladium-carbon catalyzed Suzuki–Miyaura cross-coupling by one-pot synthesis. Synlett, 2018, 29, 779-784.

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