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Your search keyword '"Ding-Qiang Fu"' showing total 4 results
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4 results on '"Ding-Qiang Fu"'

1. The aptamer-based RNA-PROTAC

Author

Yan Xu, Yi Yuan, Ding-Qiang Fu, Yi Fu, Shan Zhou, Wan-Ting Yang, Xu-Yang Wang, Guang-Xun Li, Juan Dong, Feng Du, Xin Huang, Qi-Wei Wang, and Zhuo Tang

Subjects
Organic Chemistry, Clinical Biochemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Molecular Biology, Biochemistry
Published
2023
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2. Catalytic asymmetric synthesis of N-substituted tetrahydroquinoxalines via regioselective Heyns rearrangement and stereoselective transfer hydrogenation in one pot

Author

Zhuo Tang, Guangxun Li, Xin Cui, Gao-feng Yang, Jinzhong Zhao, Xiao-kang Nie, Ding-qiang Fu, and Jin Huang

Subjects
Reaction mechanism, Chemistry, Yield (chemistry), Enantioselective synthesis, Regioselectivity, Substrate (chemistry), Stereoselectivity, General Chemistry, Transfer hydrogenation, Medicinal chemistry, Catalysis
Abstract

N-Substituted tetrahydroquinoxalines (37 examples) were step-economically obtained in good yield (

Published
2021
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3. Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs

Author

Guangxun Li, Zhuo Tang, Xin Cui, Ding-qiang Fu, Yun Deng, Fengming Qin, Yan Xu, Shaohua Yao, and Yi Yuan

Subjects
Pharmacology, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Monophenol Monooxygenase, Tyrosinase, Organic Chemistry, General Medicine, Cell biology, Melanin synthesis, Structure-Activity Relationship, Design synthesis, Pyrones, Drug Design, Drug Discovery, Proteolysis, Humans, Mushroom tyrosinase, Enzyme Inhibitors, Skin damage, Biological evaluation
Abstract

The human tyrosinase is the most prominent therapeutic target for pigmentary skin disorders. However, the overwhelming majority efforts have been devoted to search mushroom tyrosinase inhibitors, which show poor inhibitory activity on human tyrosinase and certain side effects that cause skin damage in practical application. Herein, a series of degraders that directly targeted human tyrosinase was firstly designed and synthesized based on newly developed PROTAC technology. The best PROTAC TD9 induced human tyrosinase degradation obviously in dose and time-dependent manner, and its mechanism of inducing tyrosinase degradation has also been clearly demonstrated. Besides, encouraging results that low-toxicity PROTAC TD9 was applied to reduce zebrafish melanin synthesis have been obtained, highlighting the potential to treatment of tyrosinase-related disorders. Moreover, this work has innovatively expanded the application scope of PROTAC technology and laid a solid foundation for further development of novel drugs treating pigmentary skin disorders.

Published
2021

4. Regioselective, Diastereoselective, and Enantioselective One-Pot Tandem Reaction Based on an in Situ Formed Reductant: Preparation of 2,3-Disubstituted 1,5-Benzodiazepine

Author

Zhuo Tang, Guangxun Li, Gao-feng Yang, Xin Cui, Jinzhong Zhao, Jin Huang, Xiao-kang Nie, and Ding-qiang Fu

Subjects
In situ, Tandem, 010405 organic chemistry, Chemistry, Organic Chemistry, Enantioselective synthesis, Regioselectivity, Stereoisomerism, 010402 general chemistry, Transfer hydrogenation, 01 natural sciences, Combinatorial chemistry, Catalysis, 0104 chemical sciences, Benzodiazepines, Cascade reaction, Cyclization, Reducing Agents
Abstract

The 1,5-benzodiazepines are important skeletons frequently contained in medicinal chemistry. Herein, we described an unexpected tandem cyclization/transfer hydrogenation reaction for obtaining chiral 2,3-disubstituted 1,5-benzodiazepines. The enolizable aryl aldehydes were chosen as substrates to react with symmetric and unsymmetric

Published
2021

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