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...
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...
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...
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...
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...
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...
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...
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...
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...
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...