Article
Chemistry, Multidisciplinary
Sergey A. Cherkasov, Anastasiya D. Semikina, Polina M. Kaletina, Yulia F. Polienko, Denis A. Morozov, Alexander M. Maksimov, Igor A. Kirilyuk, Elena G. Bagryanskaya, Dmitriy A. Parkhomenko
Summary: The study investigated the kinetics of reactions between 11 different vinyl monomers and nitroxide- and alkoxyamine-containing aldonitrones, determining activation energies and pre-exponential factors. The influence of monomer structure on the rate of 1,3-dipolar cycloaddition was discussed, with different vinyl monomers showing varying rates of reaction.
Article
Chemistry, Organic
Jose Cortes Vazquez, Jacqkis Davis, Vladimir N. Nesterov, Hong Wang, Weiwei Luo
Summary: A formal [3 + 3] cyclization reaction has been developed for the synthesis of 1,3,4-oxadiazinanes with generally high yields (up to 96%). The reaction, catalyzed by Sc(OTf)(3), has a broad substrate scope for both diaziridines and quinones. The synergistic activation of 1,3-dipolar diaziridines and dipolar quinones was found to be essential for enabling this reaction.
Article
Chemistry, Organic
Hao Zeng, Xiaojie Fang, Zhiyi Yang, Chuanle Zhu, Huanfeng Jiang
Summary: A general and practical method for the synthesis of 5-trifluoromethylpyrazoles has been reported, using a coupling reaction between hydrazonyl chlorides and the industrial feedstock 2-bromo-3,3,3-trifluoropropene (BTP). This catalyst-free [3 + 2] cycloaddition shows high regioselectivity, mild conditions, high yields, scalability, broad substrate scope, and tolerance for various functional groups, with application in synthesizing key intermediates for an active agonist of sphingosine 1-phosphate receptor.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Tong-Hao Li, Da-Ming Du
Summary: A highly efficient squaramide-catalysed asymmetric domino Michael/Mannich [3 + 2] cycloaddition synthesis method was used to obtain a new class of complex and diverse-skeleton isoxazole compounds with good yields and excellent diastereoselectivities and enantioselectivities. The potential applications of this method were demonstrated through gram-scale synthesis and further transformation experiments.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Applied
Hongmei Pan, Tong Lu, Xuedan Wu, Chengwen Gu, Naili Tao, Biao Zhang, Ao Wang, Guangmei Chen, Kehua Zhang, Jie Cheng, Jie Jin
Summary: A novel structure of sinomenine isoxazole derivatives was synthesised in six steps from sinomenine hydrochloride and aromatic aldehydes, yielding 19 target compounds. Key intermediates include 4-alkynyl sinomenine and 1,3-dipole, obtained from the reaction of sinomenine hydrochloride with ammonia and substitution reaction with 3-chloropropyne, and from aromatic aldehyde, respectively.
NATURAL PRODUCT RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Yu Zhang, Yanchuan Li, Shao-Fei Ni, Jin-Peng Li, Dingding Xia, Xinyu Han, Jingchuan Lin, Jinxin Wang, Shoubhik Das, Wei-Dong Zhang
Summary: Visible-light-induced [3+2] cycloadditions of donor/donor diazo precursors with alkenes to afford pyrazoles and (spiro)pyrazolines have been reported. Mechanistic and DFT studies suggested the non-covalent interactions promote the reaction.
Article
Chemistry, Organic
Hui Huang, Yiru Pu, Dikai Zhu, Chaozheng Zhang, Jirui Yang, Changqun Liu, Xin Zhang, Feiyan Tao, Mei-Mei Li, Jun Lu
Summary: We presented a general approach for synthesizing isoxazole-containing pyrazolines and pyrazoles through a [3 + 2] cycloaddition reaction. The process involved the in situ generation of nitrile imines and their reaction with 3-methyl-4-nitro-5-alkenyl isoxazoles, resulting in a regioselective synthesis of trans-configured isoxazole-substituted pyrazolines. Aromatization of the cycloadducts with the catalysis of MnO2 or SnCl2 provided access to poly-substituted pyrazoles with excellent selectivity depending on the catalyst used. The method also allowed for the one-pot synthesis of isoxazole-substituted pyrazoles. (c) 2022 Elsevier Ltd. All rights reserved.
Article
Chemistry, Multidisciplinary
Yu Zhang, Yanchuan Li, Shao-Fei Ni, Jin-Peng Li, Dingding Xia, Xinyu Han, Jingchuan Lin, Jinxin Wang, Shoubhik Das, Wei-Dong Zhang
Summary: Visible-light-induced [3+2] cycloadditions of donor/donor diazo precursors with alkenes to afford pyrazoles and (spiro)pyrazolines have been reported. Mechanistic and DFT studies suggested the formation of non-covalent interactions promote the reaction.
Article
Chemistry, Inorganic & Nuclear
Keita Tanaka, Martin-Louis Y. Riu, Brian Valladares, Christopher C. Cummins
Summary: In this study, a new class of Azophosphines and N-heterocyclic iminophosphoranes (NHIPs) were successfully synthesized. The NHIPs exhibited tunability of steric demands and good basicity. The facile and scalable synthesis of NHIPs suggests their potential applications in synthetic chemistry.
INORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Keita Tanaka, Martin-Louis Y. Riu, Brian Valladares, Christopher C. Cummins
Summary: This study presents the preparation and cycloaddition reactions of Azophosphines. The results show that these compounds have good adaptability to phosphorus atom substituents and can generate structures similar to cyclic (alkyl)(amino)carbenes. The NHIPs exhibit strong sigma-donor strengths and basicity, and display unique reactivity in certain reactions. The tunability of steric demands and scalability of these compounds suggest that they may have a wide range of applications in synthetic chemistry.
INORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Mamta Gill, Arko Das, Vinod K. Singh
Summary: An enantioselective (3+2) cycloaddition reaction has been reported for the synthesis of chiral polysubstituted pyrrolidines. The reaction displays opposite regioselectivity with excellent enantioselectivities and yields. Interestingly, changing the alpha-substituents of the iminoesters results in the formation of normal (3+2) cycloaddition products with excellent enantioselectivities as well.
Article
Chemistry, Organic
Kelvin J. Y. Wu, Amy E. Benedetto, Andrew G. Myers
Summary: The regioselectivity of a [3+2] dipolar cycloaddition reaction between a stabilized azomethine ylide and an electron-deficient dipolarophile is contrary to a previous report in this journal.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Jevgenija Luginina, Martin Linden, Maris Bazulis, Viktors Kumpins, Anatoly Mishnev, Sergey A. Popov, Tatiana S. Golubeva, Siegfried R. Waldvogel, Elvira E. Shults, Maris Turks
Summary: Novel lupane-type triterpenoid-isoxazole conjugates were synthesized by combining electro-organic synthesis and conventional methods. These conjugates exhibited cytostatic properties against various cancer cell lines, while being non-toxic to human fibroblasts.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Wan-Yu Chen, Wei-Han Lin, Chia-Jou Kuo, Chien-Fu Liang
Summary: N-Sulfonylthioimidate is converted to ketenimine under basic conditions. The reaction with vinyl/aryl azides induces dipolar cycloaddition to form 5-amino-1-vinyl/aryl-1,2,3-triazoles. The method boasts high efficiency, diverse product structures, favorable yields, and applicability to gram-scale operations.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Organic
Xiao-Long He, Cheng Wang, You-Wu Wen, Yi-Bing Zhao, Huan Yang, Shan Qian, Lingling Yang, Zhouyu Wang
Summary: A highly stereoselective dearomative [3 + 2] cycloaddition between cyclic pyridinium ylides and nitroolefins has been developed, using novel cyclic pyridinium salts as ylide precursors. This protocol offers advantages such as broad substrate scope, mild conditions, high yield, and stereoselectivity, providing a concise and efficient method for the construction of spiro-indolizidine scaffolds.
ORGANIC CHEMISTRY FRONTIERS
(2021)
Article
Multidisciplinary Sciences
Yingpeng Yao, Ying Yang, Wenhui Guo, Lifan Xu, Menghao You, Yi-Chang Zhang, Zhen Sun, Xiao Cui, Guotao Yu, Zhihong Qi, Jingjing Liu, Fang Wang, Juanjuan Liu, Tianyan Zhao, Lilin Ye, Yun-Gui Yang, Shuyang Yu
Summary: This study demonstrates the importance of RNA methylation in T-FH effector differentiation and subsequent antibody formation by stabilizing Tcf7 transcripts.
NATURE COMMUNICATIONS
(2021)
Article
Environmental Sciences
Yan Chen, Lifan Xu
Summary: The level of water-energy-food security in the Yangtze River Economic Belt improved significantly from 2008 to 2017, with different provinces performing differently in different subsystems. According to the scenario prediction results for Jiangsu Province and Hubei Province in 2025, implementing moderate management in accordance with current management objectives can increase the overall security of the system to level 4.
Article
Immunology
Yifei Wang, Qin Tian, Yaxing Hao, Wei Yao, Jinjin Lu, Cheng Chen, Xiangyu Chen, Yao Lin, Qizhao Huang, Lifan Xu, Jianjun Hu, Shun Lei, Zhengping Wei, Yuan Luo, Zhirong Li, Li Hu, Jianfang Tang, Qing Wu, Xinyuan Zhou, Yuzhang Wu, Zhinan Yin, Jianqing Xu, Lilin Ye
Summary: The study reveals that the mTORC2-Akt-GSK3 beta axis plays a crucial role in maintaining long-term persistence of virus-specific memory CD4(+) T cells by preventing ferroptosis, thus promoting cell self-protection mechanisms.
Article
Biochemical Research Methods
Huayu Lin, Haoqiang Wang, Qiao Liu, Zhiming Wang, Shuqiong Wen, Lisha Wang, Junyi Guo, Ling Ran, Zhengliang Yue, Qing Wu, Jianfang Tang, Zhirong Li, Li Hu, Lifan Xu, Qizhao Huang, Lilin Ye
Summary: Follicular regulatory T cells (Tfrs) play a significant role in controlling follicular helper T cell-driven germinal center reactions. Researchers have developed a method using spleen-chimeric mice and retrovirus transduction to investigate the differentiation of regulatory T cells into Tfrs.
JOURNAL OF IMMUNOLOGICAL METHODS
(2022)
Article
Oncology
Minglu Xiao, Luoyingzi Xie, Guoshuai Cao, Shun Lei, Pengcheng Wang, Zhengping Wei, Yuan Luo, Jingyi Fang, Xingxing Yang, Qizhao Huang, Lifan Xu, Junyi Guo, Shuqiong Wen, Zhiming Wang, Qing Wu, Jianfang Tang, Lisha Wang, Xiangyu Chen, Cheng Chen, Yanyan Zhang, Wei Yao, Jianqiang Ye, Ran He, Jun Huang, Lilin Ye
Summary: The study demonstrates that heterologous prime-boost vaccination can effectively inhibit tumor growth and enhance the expansion, effector function, and clonal breadth of tumor-specific CD8(+) T cells. Additionally, this vaccination strategy also enhances the antitumor effects of PD-1/PD-L1 immunotherapy, while preventing the re-exhaustion of tumor-specific CD8(+) T cells.
JOURNAL FOR IMMUNOTHERAPY OF CANCER
(2022)
Article
Immunology
Yao Lin, Shuai Yue, Yang Yang, Sen Yang, Zhiwei Pan, Xiaofan Yang, Leiqiong Gao, Jing Zhou, Zhirong Li, Li Hu, Jianfang Tang, Qing Wu, Shun Lei, Qin Tian, Yifei Wang, Yaxing Hao, Lifan Xu, Qizhao Huang, Bo Zhu, Yaokai Chen, Xiangyu Chen, Lilin Ye
Summary: In a small-scale clinical trial, it was found that a nasal spray based on the 35B5 antibody formulation effectively neutralizes SARS-CoV-2 variants within 24 hours, demonstrating potential prophylactic effects, especially for high-risk populations.
CLINICAL INFECTIOUS DISEASES
(2023)
Article
Immunology
Qiao Liu, Lisha Wang, Huayu Lin, Zhiming Wang, Jialin Wu, Junyi Guo, Shuqiong Wen, Ling Ran, Zhengliang Yue, Xingxing Su, Qing Wu, Jianfang Tang, Zhirong Li, Li Hu, Lifan Xu, Lilin Ye, Qizhao Huang
Summary: Cytotoxic CD8(+) T cells are the main focus of anti-tumor immunity and immunotherapy research, but transferred tumor-specific CD8(+) T cells have limited effect on suppressing tumor growth. On the other hand, CD4(+) T cells play an important role in curtailing tumor metastasis.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Qizhao Huang, Xia Wu, Zhiming Wang, Xiangyu Chen, Lisha Wang, Yijun Lu, Dan Xiong, Qiao Liu, Yuhan Tian, Huayu Lin, Junyi Guo, Shuqiong Wen, Wei Dong, Xiaofan Yang, Yuchen Yuan, Zhengliang Yue, Shun Lei, Qing Wu, Ling Ran, Luoyingzi Xie, Yifei Wang, Leiqiong Gao, Qin Tian, Xinyuan Zhou, Beicheng Sun, Lifan Xu, Zhonghui Tang, Lilin Ye
Summary: Blocking PD-1/PD-L1 signaling can unleash tumor-specific CD8+ T cells in the tumor draining lymph nodes and enhance anti-tumor therapeutic efficacy.
Review
Chemistry, Medicinal
Lifan Xu, Peng Lu, Yubin Wang
Summary: This article provides an overview of inflammatory bowel disease (IBD), including its clinical manifestations and current treatment options. It explores the advantages of small molecules over biological therapies and discusses the mechanisms of action of sphingosine 1-phosphate (S1P) and S1P receptors (S1PRs). The article also presents clinical data on various S1PR modulators.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Editorial Material
Multidisciplinary Sciences
Qizhao Huang, Xia Wu, Zhiming Wang, Xiangyu Chen, Beicheng Sun, Lifan Xu, Zhonghui Tang, Lilin Ye
CHINESE SCIENCE BULLETIN-CHINESE
(2022)
Letter
Immunology
Qiao Liu, Ling Ran, Zhengliang Yue, Xingxing Su, Lisha Wang, Shuqiong Wen, Shun Lei, Xiaofan Yang, Yan Zhang, Jianjun Hu, Jianfang Tang, Zhirong Li, Li Hu, Bo Zhu, Lifan Xu, Lilin Ye, Qizhao Huang
CELLULAR & MOLECULAR IMMUNOLOGY
(2023)
Proceedings Paper
Engineering, Electrical & Electronic
Lifan Xu, Ruxin Zheng, Shunqiao Sun
Summary: In this paper, a deep reinforcement learning approach is proposed for designing an automotive radar system with integrated sensing and communication. The system learns to intelligently adjust its beamforming vector through interaction with the environment, to enhance the performance of radar sensing and communication.
2022 IEEE 12TH SENSOR ARRAY AND MULTICHANNEL SIGNAL PROCESSING WORKSHOP (SAM)
(2022)
Correction
Multidisciplinary Sciences
Lisha Wang, Zhiming Wang, Junyi Guo, Huayu Lin, Shuqiong Wen, Qiao Liu, Yiding Li, Qing Wu, Leiqiong Gao, Xiangyu Chen, Luoyingzi Xie, Qin Tian, Jianfang Tang, Zhirong Li, Li Hu, Juan Wang, Lifan Xu, Qizhao Huang, Lilin Ye
JOVE-JOURNAL OF VISUALIZED EXPERIMENTS
(2022)
Article
Biochemistry & Molecular Biology
Xiaofei Wang, Ao Hu, Xiangyu Chen, Yixin Zhang, Fei Yu, Shuai Yue, Arong Li, Junsong Zhang, Zhiwei Pan, Yang Yang, Yao Lin, Leiqiong Gao, Jing Zhou, Jing Zhao, Fang Li, Yaling Shi, Feng Huang, Xiaofan Yang, Yi Peng, Luoyang Tu, Huan Zhang, Huanying Zheng, Jun He, Hui Zhang, Lifan Xu, Qizhao Huang, Yongqun Zhu, Kai Deng, Lilin Ye
Summary: This study demonstrates an antibody that efficiently neutralizes both SARS-CoV-2 and its variants, providing insights for the development of universal vaccines.
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2022)
Article
Medicine, Research & Experimental
Xiangyu Chen, Yao Lin, Shuai Yue, Yang Yang, Xinxin Wang, Zhiwei Pan, Xiaofan Yang, Leiqiong Gao, Jing Zhou, Zhirong Li, Li Hu, Jianfang Tang, Qing Wu, Yifei Wang, Qin Tian, Yaxing Hao, Lifan Xu, Bo Zhu, Qizhao Huang, Lilin Ye
Summary: Exhausted CD8(+) T (Tex) cells caused by chronic viral infection or tumor development can partially regain their effector functions when immune inhibitory receptors (IRs) such as PD-1 are blocked. In this study, researchers discovered that tumor-derived Tex cells selectively upregulate immune inhibitory receptor NKG2A, while virus-derived Tex cells do not. This dichotomous expression of NKG2A further determines the different responsiveness of Tex cells to NKG2A immune checkpoint blockade. These findings provide new insights into the distinct regulatory mechanisms of T cell exhaustion between tumor and chronic viral infection.
Article
Chemistry, Organic
Dilek Isik Tasgin, Irem Bayraktar
Summary: We present a synthetic method for pyrrolizine-3-one derivatives and investigate their photophysical properties. These compounds are prepared through a series of reactions involving substituted pyrroles in one-pot, two-step oxidation, and intramolecular cyclization processes. The photophysical properties of the synthesized compounds are studied using UV-Vis and fluorescence spectroscopy in various solvents. The introduction of pyrrolyl substituents has a significant impact on Stokes shifts and quantum yield values.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Satish Kumar Burra, Vaikunta Rao Lakinani, Raghunadh Akula, Chiranjeevi Yankkanti
Summary: A novel and green strategy for the construction of biologically relevant substituted indolyl-4H-chromenes scaffolds is reported, using L-proline as a catalyst and water as a promoter solvent. This catalytic system offers wider applicability, shorter reaction times, and high yields, making it an ideal condition for green chemistry.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Abouelhaoul El Alami, Amine El Maraghi, Fatima Youssoufi, Assiya Atif, Hamid Sdassi
Summary: Nitrobenzimidazoles have become increasingly important in the design of new compounds in medicinal, therapeutic and chemical fields. This review provides an overview of the synthesis strategies and biological activities of nitrobenzimidazole derivatives.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Nilesh Raghunath Khedkar, Alex Joseph, Milind Sindkhedkar
Summary: In this study, a new library of 3-(2-(pyrimidin-5-yl)thiazol-4-yl)-1,2,4-oxadiazole compounds was designed and synthesized as potential anticancer agents using in silico fragment-based drug design. The compounds were tested for their anticancer activity in vitro, and one compound exhibited excellent activity against multiple cancer cell lines.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Terungwa H. Iorkula, Bryce A. Tolman, Scott R. Burt, Matt A. Peterson
Summary: A new method for synthesizing C-6 substituted products has been discovered in this study, which utilizes lower doses of fluoride and CsF as a catalyst, with high reaction yields and cost-effectiveness under suitable conditions.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Ranjana Aggarwal, Swati Sharma
Summary: This review article mainly focuses on the synthesis of 3(5)-trifluoromethylpyrazoles via condensation reaction of trifluoromethyl-beta-diketones with hydrazines. It emphasizes the importance of fluorine-containing compounds and pyrazoles in the field of biology. The literature reported condensation reactions of trifluoromethyl-beta-diketones with hydrazines are covered.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
F. M. Alshareef, Sami A. Al-Harbi, Esam S. Allehyani, Omeima Abdullah, Magdy A. Ibrahim
Summary: This study aimed to construct a novel category of linear annulated chromeno[3',2':5,6]pyrido[2,3-d][1,3]thiazolo[3,2-a]pyrimidines. The chemical reactivity of the synthesized compounds was investigated, and they showed significant antimicrobial activity against various strains.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Preethi Dhanapal, S. L. Manju
Summary: Thiazole based Schiff base scaffolds have become an integral part of drug development in recent years, playing a versatile role as building blocks for lead drug molecules. This study presents a facile one pot synthetic method for producing novel 4-aryl thiazoles with high yield, shorter reaction time, and milder conditions, without the need for catalysts or purification techniques.
SYNTHETIC COMMUNICATIONS
(2024)
