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Biography

Xiaowei Wu is a Principal Investigator at Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Zhongshan Institute for Drug Discovery, SIMM, CAS. He obtained his PhD degree in 2017 from Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences (CAS), China. From 2017 to 2021, He worked as a post-doc at H. Lee Moffitt Cancer Center & Research Institute and Baylor College of Medicine, respectively. Dr. Wu’s primary interest is the development of novel small-molecule therapeutics for the treatment of cancer and other diseases. Meanwhile, he’s also interested in developing green and practical reaction for heterocycles synthesis.

Research Directions

2017.8-2018.6  Postdoctoral fellow, Department of Drug Discovery, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, USA

2018.6-2021.02  Postdoctoral fellow, Department of Pharmacology and Chemical Biology, Baylor College of Medicine, Houston, Texas, USA

2021.03-To date  Principal Investigator, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China

Achievements

Medicinal chemistry, the development of transition-metal-catalyzed reactions and their application in the medicinal chemistry

(1) Several potent FGFR covalent inhibitors were obtained with the assistance of ligand-based virtual screening, which showed good activities in vitro and in vivo assays. These pyrazolo[3,4-d]pyridazinone derivatives may serve as lead compounds for further drug development.

(2) An efficient Ru(II)-catalyzed redonx-neutral [4 + 1] annulation of benzamides and propargyl alcohols by C?H bond activation for accessing potentially bioactive N-substituted quaternary isoindolinones was developed, in which propargyl alcohols serve as rare one-carbon components. Because of our pioneering work, many impressive progresses with propargyl alcohols have been made (From Zhou et al, ChemPlusChem 2020, 85, 405) and this work has been cited over 90 times.

(3) A ruthenium(II)-catalyzed C?H allylation at the C-2 position of N-ethoxycarbamoyl indoles with allyl alcohols via β-hydroxide elimination was developed. Further, this method does not require high temperature, external oxidants, and expensive additives. This work was highlighted by Synfacts and ChemistryViews.

Publications

1. Haifang Meng, Huiying Xu, Zhi Zhou, Zhenhao Tang, Yidi Li, Yu Zhou,* Wei Yi,* Xiaowei Wu*. Recyclable rhodium-catalyzed C-H activation/[4+2] annulation with unconventional regioselectivity at ambient temperature: experimental development and mechanistic insight. Green Chemistry, 2022, accepted. DOI: 10.1039/D2GC02347D

2. Xiaowei Wu, Bao Wang, Shengbin Zhou, Yu Zhou, Hong Liu. Ruthenium-Catalyzed Redox-Neutral [4+1] Annulation of Benzamides and Propargyl alcohols via C-H Bond Activation. ACS Catalysis, 2017, 7, 2494-2499.

3. Fei Zhao*, Zhi Zhou, Yangbin Lu, Jin Qiao, Xiaoning Zhang, Xin Gong, Siyu Liu, Shuang Lin, Xiaowei Wu*, Wei Yi*. Chemo-, Regio-, and Stereoselective Assembly of Polysubstituted Furan-2(5H)-ones Enabled by Rh(III)-Catalyzed Domino C-H Alkenylation/Directing Group Migration/Lactonization: A Combined Experimental and Computational Study. ACS Catalysis, 2021, 11, 13921-13934.

4. Xiaowei Wu, Bao Wang, Yu Zhou, Hong Liu. Propargyl alcohols as one-carbon synthons: redox-neutral Rh (III)-catalyzed C-H bond activation for the synthesis of isoindolinones bearing a quaternary carbon. Organic Letters, 2017, 19, 1294-1297.

5. Xiaowei Wu, Haitao Ji. Ruthenium(II)-Catalyzed Regio- and Stereoselective C?H Allylation of Indoles with Allyl Alcohols. Organic Letters, 2018, 20, 2224-2227. Highlighted by Synfacts and ChemistryViews.

6. Xiaowei Wu, Yangbin Lu, Jin Qiao, Wenhao Dai, Xiuwen Jia, Hangcheng Ni, Xiaoning Zhang, Hong Liu, and Fei Zhao. Rhodium(III)-Catalyzed C–H Alkenylation/Directing Group Migration for the Regio- and Stereoselective Synthesis of Tetrasubstituted Alkenes. Organic Letters, 2020, 22, 9163-9168.

7. Xiaowei Wu, Dengyou Zhang, Shengbin Zhou, Feng Gao, Hong Liu. Site-specific indolation of proline-based peptides via copper(II)-catalyzed oxidative coupling of tertiary amine N-oxides. Chemical Communications, 2015, 51, 12571-12573.

8. Xiaowei Wu, Mengdi Dai, Jihui Zhao, Yulan Wang, Chunpu Li, Xia Peng, Rongrong Cui, Bao Wang, Yang Dai, Dan Feng, Hualiang Jiang, Meiyu Geng, Jing Ai, Mingyue Zheng, Hong Liu. Design, Synthesis and pharmacological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors. Acta Pharmaceutica Sinica B. 2021, 11, 781-794.

9. Yulan Wang,# Yang Dai,# Xiaowei Wu,# Fei Li, Bo Liu, Chunpu Li, Qiufeng Liu, Yuanyang Zhou, Bao Wang, Mingrui Zhu, Rongrong Cui, Xiaoqin Tan, Zhaoping Xiong, Jia Liu, Minjia Tan, Yechun Xu, Mei-Yu Geng, Hualiang Jiang, Hong Liu, Jing Ai, Mingyue Zheng. The Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as Novel Covalent FGFR Inhibitors by Rational Drug Design. J. Med. Chem. 2019, 62, 7473-7488.

10. Fei Zhao,* Xin Gong, Yangbin Lu, Jin Qiao, Xiuwen Jia, Hangcheng Ni, Xiaowei Wu,* Xiaoning Zhang*. Additive-Controlled Divergent Synthesis of Tetrasubstituted 1,3-Enynes and Alkynylated 3H-pyrrolo[1,2-a]indol-3-ones via Rhodium Catalysis. Organic Letters, 2021, 23, 727-733.