INHIBITORS

作品数:1279被引量:2687H指数:18
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相关领域:医药卫生更多>>
相关作者:张志丽刘俊义徐萍田超邹晓民更多>>
相关机构:北京大学中国医学科学院北京协和医学院北京化工大学中国科学院更多>>
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相关基金:国家自然科学基金国家重点基础研究发展计划中国博士后科学基金国家教育部博士点基金更多>>
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Discovery of Novel Long-Chain Alkenyl Diacid Derivatives as ACLY Inhibitors
《Chinese Journal of Chemistry》2022年第22期2663-2670,共8页Gao-Lei Song Lei Cao Mei Zhang Yu-Rou Yang Jie Ma Zhi-Fu Xie Jing-Ya Li Fa-Jun Nan 
supported by grants fromthe"Personalized Medicines-Molecular Signature-based Drug Discovery and Development"Strategic Priority Research Program of the Chinese Academy of Sciences(XDA12040328);the Medical Guidance Project of Shanghai ScienceandTechnology Commission(20S11903400);the Natural Science Foundation of Shanghai's 2021"Science and Technology InnovationAction Plan"(21ZR1475300);the National Natural Science Foundation of China(No.82170872).
ATP citrate lyase(ACLY)synthesizes cytosolic acetyl coenzyme A(acetyl-CoA),an essential biosynthetic precursor for lipid synthesis and the acetyl donor required for protein acetylation.The aberrant expression and acti...
关键词:Alkenyl diacid derivatives Cancer ACLY inhibitors ACETYL-COA Structure-activity relationships 
Discovery of CECR2 Bromodomain Inhibitors with High Selectivities over BPTF Bromodomain
《Chinese Journal of Chemistry》2022年第17期2072-2080,共9页Haibo Lu Shijia Zu Zhe Duan Yueyao Feng Jie Wang Jingyi Ma Qi Li Dongying Chen Bo Li Kaixian Chen Cheng Luo Jin Lin Tian Lu Hua Lin 
the Science and Technology Commission of Shanghai Municipality(Y811298033 to Q.L.,and 19XD1404700 to C.L.);the scientific research innovation program“Xiyuanjiang River Scholarship”of the College of Life Sciences,Fujian Normal University;the State Key Laboratory of Drug Research(SIMM2105KF-07toH.L.);Fujian Provincial Natural Science Foundation(2021J01203 to H.L.);the Natural Science Foundation of Fujian Province(2019J05073 to J.L.);the Joint Funds forthe Innovation of Science and Technology of Fujian Province(2018Y9071 to J.L.).
Cat's eye syndrome chromosome candidate 2 bromodomain(CECR2 BRD)and Bromodomain PHD transcription factor bromodomain(BPTF BRD)are the same subfamily proteins,both of which are highly conserved in sequence and binding ...
关键词:CECR2 bromodomain BPTF bromodomain INHIBITORS Structure-activity relationships chemical probe 
Discovery of Tryptophan-tetrahydroisoquinoline Derivatives as Multifunctional Agents for Treatment of Alzheimer's Disease被引量:1
《Chinese Journal of Chemistry》2022年第15期1821-1830,共10页Xin Lu Yijun Liu Nan Qin Chenxi Du Yanyu Hu Yao Chen Haopeng Sun 
We gratefully thank the support from the grants of the National Natural Science Foundation of China(Nos.81872728 and 82173652);the Natural Science Foundation of Jiangsu Province(No.BK20191411).
Comprehensive Summary The cholinesterases are essential targets implicated in the pathogenesis of Alzheimer's disease(AD).We have identified tryptophan-tetrahydroisoquinoline derivatives as selective micro-nanomolar b...
关键词:Alzheimer's disease BUTYRYLCHOLINESTERASE INHIBITORS Molecular modeling Biological activity 
A Practical and High-Affinity Fluorescent Probe for Butyrylcholinesterase:A Good Strategy for Binding Affinity Characterization
《Chinese Journal of Chemistry》2022年第11期1285-1292,I0002,共9页Lei Wang Chenxi Du Hui Liu Weimin Qiu Xin Lu Yanyu Hu Yueqing Li Tianyu Sun Yao Chen Haopeng Sun 
We gratefully thank the support from the grants of the National Natural Science Foundation of China(Nos.81872728 and 82173652);the Natural Science Foundation of Jiangsu Province(No.BK20191411)。
Butyrylcholinesterase(BChE)is regarded as a promising target for the treatment of Alzheimer's disease(AD),as its level significantly increases along with the progress of this disease.Therefore,the development of poten...
关键词:BUTYRYLCHOLINESTERASE Alzheimer's disease Fluorescent probes INHIBITORS High-throughput screening 
Discovery of a Potent Botulinum Neurotoxin A Inhibitor ZM299 with Effective Protections in Botulism Mice被引量:2
《Chinese Journal of Chemistry》2022年第3期357-364,共8页Jianxin Wang Yuelin Wu Deyan Luo Chunlin Zhuang Nianzhi Ning Yanming Zhang Zhili He Jie Gao Zhanying Hong Xiguo Xv Wannian Zhang Tao Li Zhenyuan Miao Hui Wang 
the National Natural Science Foundation of China(Nos.82173743 and U20A20136).
Botulinum neurotoxins serotype A(BoNT/A)is the deadliest toxins known to humans and the"Category A"agent for bioterrorism.Over the past 20 years,significant efforts have been put forth to develop effective inhibitors ...
关键词:Botulinum Neurotoxin A BOTULISM Virtual screening Drug design INHIBITORS 
Hybeanones A and B,Two Highly Modified Polycyclic Polyprenylated Acylphloroglucinols from Hypericum beanii
《Chinese Journal of Chemistry》2022年第1期53-58,共6页Beiye Yang Changxing Qi Zeyu Yao Shuang Lin Fengli Li Weiguang Sun Zhengxi Hu Yonghui Zhang 
financially supported by the National Natural Science Foundation for Distinguished Young Scholars(81725021);the National Science and Technology Project of China(2018ZX09201001-001-003);the Innovative Research Groups of the National Natural Science Foundation of China(81721005);the National Natural Science Foundation of China(82003633);the Academic Frontier Youth Team of HUST(2017QYTD19);the Fundamental Research Funds for the Central Universities(2020kfyXJJS083);the Integrated Innovative Team for Major Human Diseases Program of Tongji Medical College(HUST).
Hybeanones A and B(1 and 2),two highly oxygenated and rearranged polycyclic polyprenylated acylphloroglucinols(PPAPs),were isolated from the aerial parts of Hypericum beanii.Their structures comprising absolute config...
关键词:Hypericum beanii Natural products Structure elucidation INHIBITORS Molecular docking 
Commiphoroids G_(1)-G_(3), H and I, Five Terpenoid Dimers as Extracellular Matrix Inhibitors from Resina Commiphora被引量:2
《Chinese Journal of Chemistry》2021年第8期2172-2180,共9页Lu Dong Jian-Bing Jiang Yong-Ming Yan Shu-Mei Wang Yong-Xian Cheng 
This study was supported financially by the National Science Fund for Distinguished Young Scholars(No.81525026);the National Key R&D Program of China(No.2017YFA0503900);the She nzhe n Fundame ntal Research Program(No.JCYJ20200109114003921);the SZU Top Ranking Project(No.86000000210);the Natural Science Research Project of Shenzhen University(2019122);the SZU Medical Young Scientist Program.
Commiphoroids G_(1)-G_(3),H and I(1-5),five new terpenoid dimers were isolated from Resina Commiphora.Their structures and absolute configurations were determined by using spectroscopic,computational and crystallograp...
关键词:Resina Commiphora Natural products Terpenoid dimers Structural elucidation Anti-renal fibrosis 
Design, Synthesis and Biological Evaluation of Novel α-Acyloxycarboxamide-Based Derivatives as c-Met Inhibitors
《Chinese Journal of Chemistry》2021年第8期2241-2250,共10页Yu-juan Feng Yu-Lin Ren Li-Ming Zhao Guo-Qiang Xue Wen-Hao Yu Jia-Qi Yang Jun-Wei Liu 
This work was supported by the Fundamental Research Funds for the Central Universities(Nos.31920170193 and 31920200026).
Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractiv...
关键词:4-(2-Fluorophenoxy)quinoline derivatives c-Met inhibitors Passerini reaction a-Acyloxycarboxamide Biological evaluation 
Synthesis, Antimicrobial Activity, and Molecular Docking of Benzoic Hydrazide or Amide Derivatives Containing a 1,2,3-Triazole Group as Potential SDH Inhibitors
《Chinese Journal of Chemistry》2021年第5期1319-1330,共12页Yue Ding Ling Zhang Song Yang Zhong Li Pei-Yi Wang 
the National Natural Science Foundation of China(21662009,21702037,31860516,21877021);Guizhou Provincial S&T Program([2017]5788);Frontiers Science Center for Asymmetric Synthesis and Medicinal Molecules,Department of Education,Guizhou Province[Qianjiaohe KY number(2020)004];Key Technologies R&D Program(2014BAD23B01);Program of Introducing Talents of Discipline to Universities of China(111 Program,D20023).
The present study was carried out in an attempt to synthesize a new class of antimicrobial agents containing a 1,2,3-triazole motif formed by classical copper catalyzed click chemistry.Antifungal bioassay results show...
关键词:HYDRAZIDE AMIDE 1 2 3-TRIAZOLE Molecular docking SDH inhibitory activity 
Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors
《Chinese Journal of Chemistry》2021年第1期115-120,共6页Na Luo Xiaoyu Fang Mingbo Su Xinwen Zhang Dan Li Honglin Li Shiliang Li Zhenjiang Zhao 
This work was supported by the National Key Research and Development Program(No.2016YFA0502304 to H.L.);the National Natural Science Foundation of China(No.81825020 to H.L,No.81803437 to SL.);the National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program",China(No.2018ZX09711002);the Fundamental Research Funds for the Central Universities,Special Program for Applied Research on Super Computation of the NSFC-Guangdong Joint Fund(the second phase)under Grant No.U1501501;Shiliang Li is sponsored by Shanghai Sailing Program(No.18YF1405100);Honglin Li is also sponsored by the National Program for Special Supports of Emi nent Professionals and the National Program for Support of Top-notch Young Professionals.
Dipeptidyl peptidase 4(DPP-4)is a clinically validated target for the treatment of type 2 diabetes mellitus(T2DM).To discover novel and potent DPP-4 inhibitors,three series of compounds were designed and synthesized i...
关键词:TypeⅡdiabetes Dipeptidyl peptidaseⅣ INHIBITORS Molecular docking Structure-activity relationship 
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