MACROCYCLIZATION

作品数:10被引量:3H指数:1
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相关领域:理学医药卫生更多>>
相关期刊:《Acta Biochimica et Biophysica Sinica》《Chinese Journal of Natural Medicines》《Chinese Journal of Chemistry》《Chinese Chemical Letters》更多>>
相关基金:国家自然科学基金河南省自然科学基金The Royal Society更多>>
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Modular,Scalable Total Synthesis of Neopetromin
《Chinese Journal of Chemistry》2024年第23期3023-3028,共6页Hiroshige Ogawa Yuuya Nagata Hugh Nakamura 
Financial support for this work was provided by a grant from the RGC of the Hong Kong SAR,China(ECS,HKUST 26302024);start-up funds from HKUST(Project No.R9820)to H.N;This work was partly supported by JSPS KAKENHI Grant Number JP23H03810,JST-ERATO(JPMJER1903);the Institute for Chemical Reaction Design and Discovery(ICReDD),which was established by the World Premier International Research Initiative(WPI),MEXT,Japan(Y.N.);The computation was partly performed using Research Center for Computational Science,Okazaki,Japan(Project:23-IMS-C119,Y.N.).
The first total synthesis of neopetromin,featuring the highly strained Tyr C-6-to-Trp N-1’linkage,is hereby reported.This modular synthetic strategy,employing C—H arylation and Larock macrocyclization,offers a novel...
关键词:Total synthesis Natural product Biaryl cyclic peptides RiPPs C-H activation Larock macrocyclization Scalable synthesis 
Asymmetric macrocyclization enabled by Rh(Ⅲ)-catalyzed C-H activation:Enantioenriched macrocyclic inhibitor of Zika virus infection
《Chinese Chemical Letters》2024年第11期378-383,共6页Chao Chen Wenwen Yu Guangen Huang Xuelian Ren Xiangli Chen Yixin Li Shenggui Liang Mengmeng Xu Mingyue Zheng Yaxi Yang He Huang Wei Tang Bing Zhou 
supported by National Natural Science Foundation of China(No.81973166);Science and Technology Commission of Shanghai Municipality(No.22XD1424600);Natural Science Foundation of Shanghai Municipality(No.22ZR1474100);Taishan Scholar Foundation of Shandong Province(No.tsqn202306322);National Key R&D Program of China(No.2021YFC2300700);Shandong Laboratory Program(No.SYS202205);Shandong Provincial Natural Science Foundation(Nos.ZR2023LSW003 and ZR2023JQ028)。
The development of enantioselective C-H macrocyclizations to efficiently access structurally diversified macrocycles is highly desirable,but remain a big challenge.Herein,we reported the first rhodium(Ⅲ)-catalyzed as...
关键词:C-H activation Carboamidation Enantioselective macrocyclization Anti-Zika virus activity 
Design and synthesis of antiviral pseudo-natural products through effective one-step acylmethylation macrocyclization
《Chinese Journal of Natural Medicines》2023年第10期721-722,共2页LI Shang WANG Xiaobing 
supported by the Natural Science Foundation of Jiangsu Province(No.BK20201332).
Influenza virus poses a significant threat to global public health,causing serious repercussions on human life and social well-being.Over the past decades,various antiviral drugs targeting either the virus itself or i...
关键词:Natural products C-H activation MACROCYCLIZATION H1N1 inhibitors 
Antimony salt-promoted cyclization facilitating on-DNA syntheses of dihydroquinazolinone derivatives and its applications被引量:1
《Chinese Chemical Letters》2023年第8期201-207,共7页Qigui Nie Jie Sun Xianfu Fang Xun He Feng Xiong Gong Zhang Yangfeng Li Yizhou Li 
supported by grants from the National Natural Science Foundation of China(Nos.22222702,22107016,22107017 and 21907011);the Fundamental Research Funds for the Central Universities(No.2022CDJQY-001);Beijing National Laboratory for Molecular Sciences(No.BNLMS202104);the Natural Science Foundation of Chongqing(Nos.cstc2020jcyj-jqX0009,cstc2021jcyjmsxmX0016 and cstc2021jcyj-cxttX0002);High-end Foreign Expert Introduction Program(No.G2022165020L);Shenzhen Innovation Center for Small Molecule Drug Discovery Co.(No.H20220687).
DNA-encoded chemical libraries technology has become a novel approach to finding hit compounds in early drug discovery.The chemical space in a DEL would be expanded to realize its full potential,especially when integr...
关键词:DNA-encoded chemical libraries ANTIMONY Dihydroquinazolinone MACROCYCLIZATION DNA-compatible chemistry 
Harnessing the cyclization strategy for new drug discovery被引量:2
《Acta Pharmaceutica Sinica B》2022年第12期4309-4326,共18页Kai Tang Shu Wang Wenshuo Gao Yihui Song Bin Yu 
This work is supported by the National Natural Science Foundation of China(Nos.22277110,81973177 and 31900875,China);the Natural Science Foundation of Henan Province(Nos.222300420069 and 222301420049,China);Program for Science&Technology Innovation Talents in Universities of Henan Province(No.21HASTIT045,China).
The design of new ligands with high affinity and specificity against the targets of interest has been a central focus in drug discovery.As one of the most commonly used methods in drug discovery,the cyclization repres...
关键词:Ring cyclization SPIROCYCLIZATION MACROCYCLIZATION Conformational constraint Lead generation New drug discovery 
Natural scaffolds-inspired synthesis of CF_(3)-substituted macrolides enabled by Rh-catalyzed C–H alkylation macrocyclization
《Chinese Chemical Letters》2022年第4期2015-2020,共6页Tongyu Bi Yi Xu Xin Xu Bixi Tang Qing Yang Yi Zang Zhenyang Lin Jia Li Weibo Yang 
the"100 Talent Program of Chinese Academy of Sciences";"1000-Youth Talents Plan";ShanghaiYouth Talent,National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program"China(No. 2018ZX09711002–006);Science and Technology Commission of Shanghai Municipality (No. 18431907100);ShanghaiTechnology Innovation Action Plan (No. 18JC1415300);the Research Grants Council of Hong Kong (No. HKUST 16302418) for financial support of this research。
The development of innovative strategies and methods to provide natural product-like macrocycles not accessible by biosynthesis, but endowed with novel bioactivities and simplified structure, is highly desirable. Insp...
关键词:Rh-catalyzed C–H alkylation Late stage macrocyclization DFT calculation Anti-inflammation 
Protein macrocyclization by a recombinant asparaginyl endopeptidase
《Acta Biochimica et Biophysica Sinica》2021年第11期1567-1570,共4页Xiaoyun Hu Hui Liu Jie Li Jiewen Wang Wenfang Peng 
This work was supported by the grants from the Teaching Construction Project of Hubei University(No.2020C01);the Scientific Research Program of Hubei Provincial Development of Education(No.Q20161007);the Innovation Base for Introducing Talents of Discipline of Hubei Province(No.2019BJH021);the State Key Laboratory of Biocatalysis and Enzyme Engineering.
Protease is abundant in nature and has a wide variety,playing a vital role in a series of cell processes.Most proteases cause protein degradation by cleaving substrate sequence within the target or altering proteins i...
关键词:CYCLIZATION thereby RENDER 
Palladium-Catalzyed Atroposelective 16-Membered Macrocyclization: Total Synthesis of lsoplagiochin D
《Chinese Journal of Chemistry》2020年第10期1081-1085,共5页Junwei Xi Zhenhua Gu 
This work was financially supported by the National Natural Science Foundation of China(No.21871241);the Fundamental Research Funds for the Central Universities(WK2060190086).
Summary of main observation and conclusion Isoplagiochin D is a ring-strained macrocyclic bisbibenzylis,which showed stable axial chirality in one biaryl structure,and semistable axial chirality in the other biaryl mo...
关键词:CYCLIZATION BENZYL CATALYZED 
Synthesis of novel disulfide-bridged dilactam crown ethers
《Chinese Chemical Letters》2007年第12期1439-1442,共4页Hossein Eshghi Seyed Mohammad Seyedi Reza Sandarooss 
The novel macrocyclic dilactams with redox-switched disulfide linkage were synthesized. These compounds were obtained from 2,2′-dithiodibenzoyl chloride in the macrocyclization step by fast addition method in moderat...
关键词:Dilactam DISULFIDE Fast addition MACROCYCLIZATION Redox SWITCHABLE 
β-Lactam Templated Macrocyclization:Synthesis of 12-Membered Macrolide
《Chinese Chemical Letters》2005年第5期601-603,共3页GuoJuanLIANG JinZhongZHANG AnQiCHEN 
This work is supported by the National Natural Science Foundation of China (grant No: 20372056);a Research Fund from the Royal Society of Chemistry. UK.
A novel macrolactonization method was developed using a chiral β-lactam as the template. This novel method features that the macrocyclization is simultaneously achieved while a TBS protected hydroxy group is deprotec...
关键词:LACTAM macrolactonization MACROLIDE templated cyclization. 
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