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Development of novel Gemini-cholesterol analogues for retinoid-related orphan receptors

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Organic Chemistry Frontiers 2022年第6期9卷 1522-1530页

作者： Uxía Gómez-Bouzó Alioune Fall Judit Osz Yagamare Fall ORCID logo Natacha Rochel Hugo Santalla Departamento de Química Orgánica Facultade de QuímicaUniversity of VigoCampus Lagoas de Marcosende36310 VigoSpain Department of Integrative Structural Biology IGBMC-CNRS UMR7104-Inserm U9641rue Laurent Fries67400 IllkirchFrance

Retinoic-acid-related Orphan Receptors (RORs) regulate the maintenance of the circadian rhythm and immune response among others and are involved in increasing numbers of pathologies including autoimmune diseases, cancer and neurological disorders leading to huge interest in the development of ROR ligands. Here, we describe the synthesis of six novel Gemini cholesterol analogues and the binding mode of one of them to RORγ.

关键词： analogues synthesis numbers

Chemical and chemoenzymatic stereoselectivesynthesis of β-nucleosides and their analogues

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Organic Chemistry Frontiers 2022年第6期9卷 1719-1741页

作者： Hui-Jing Wang Yang-Yang Zhong You-Cai Xiao Fen-Er Chen Sichuan Research Center for Drug Precision Industrial Technology West China School of PharmacySichuan UniversityChengdu610041China Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan UniversityShanghai200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Shanghai 200433ChinaShanghai200433China

β-Nucleosides are fundamental building blocks of biological systems and are widely used as therapeuticagents for the treatment of cancer and viral infections, among others. In the last two years, nucleosideanalogues have been investigated with renewed urgency in the search for agents that are effective againstSARS-CoV-2, the cause of the ongoing global pandemic of COVID-19. This has resulted in an explosionof activities in the field of β-nucleoside synthesis. This review summarizes the historical perspective andthe recent advances in the stereoselective synthesis of β-nucleosides and their analogues. The syntheticstrategies to obtain β-nucleosides can be divided into three categories: (1) N-glycosylation;(2) intramolecular sugar ring formation;and (3) enzymatic transglycosylation.

关键词： synthesis analogues nucleoside

Physicochemical properties of amide–AlCl_3 based ionic liquid analogues and their mixtures with copper salt

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Chinese Journal of Chemical Engineering 2019年第1期27卷 144-149页

作者： Pengcheng Hu Wei Jiang Lijuan Zhong Shufeng Zhou College of Chemical Engineering HuaQiao University

The physicochemical properties of three different amide–AlCl_3 based ionic liquid(IL) analogues and their mixtures with copper salt, such as conductivity, viscosity, density and isobutane solubility were determined over a wide range of temperatures.The effects of amide structure, amide/AlCl_3 molar ratio and CuCl modification on these physicochemical properties were investigated.Results showed that the conductivity of amide–AlCl_3 based IL analogues was much lower than that of traditional Et_3NHCl–AlCl_3 IL with same ligand/AlCl_3 molar ratio due to incomplete splitting of AlCl_3, whereas the density and viscosity of amide–AlCl_3 based IL analogues were slightly higher.The viscosity of amide–AlCl_3 based IL analogues was closely related to the amide structure,and followed the order of DMA–AlCl_3>AA–AlCl_3>NMA–AlCl_3 with same amide/AlCl_3 molar ratio.Meanwhile,the density of amide–AlCl_3 based IL analogues ranked in the following order: AA–AlCl_3>NMA–AlCl_3>DMA–AlCl_3.Increasing the amide/AlCl_3 molar ratio decreased the conductivity and density, while increased the viscosity.The solubility experiment indicated that the isobutane solubility in NMA–AlCl_3 was highest than that in two other IL analogues.Under the modification of CuCl, the conductivity, viscosity and density of these IL analogues increased, whereas the isobutane solubility decreased.These results provide the foundation for the development of a suitable IL analogue catalyst for isobutane alkylation.

关键词： Ionic liquid analogues Conductivity Density Viscosity Isobutane solubility

Design,Synthesis and Biological Evaluation of Bengamide analogues as ClpP Activators

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Chinese Journal of Chemistry 2020年第10期38卷 1111-1115页

作者： Xue-Qing Kong Bing-Yan Wei Chen-Xi Yu Xiang Na Guan Wei-Ping Ma Gang Liu Cai-Guang Yang Fa-Jun Nan Chinese National Center for Drug Screening CAS Key Laboratory of Receptor ResearchStote Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaNo.39Science and Technology AvenueHigh-tech Industrial Development ZoneYantaiShandong 264000China

Summary of main observation and conclusion To combat multidrug-resistant Gram-positive bacteria,new antimicrobials particularly those with novel mechanism of action are badly needed.Different with conventional antibiotics which are typical inhibitors,small-molecule activators of bacterial CIpP represent a new class of antibiotics.No ClpP activator has been developed for clinical trial.Herein,we conducted a screening on our library of benga-mide-like ring opened analogues and found that L472-2 possesses a low minimum inhibitory concentration(MIC)against S.aureus and shows no activity for ClpP activation in vitro,but it displayed reduced antibacterial activity against S.aureus with clpP deletion.In order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity,we perform further structural modifications starting from L472-2.Compound 37 re-mains the antimicrobial activity and activation of ClpP protein in vitro,which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.

关键词： analogues activation starting

Synthesis and Antiproliferative Activities of OSW-1 analogues Bearing 2"-0-p-Acylaminobenzoyl Residues

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Chinese Journal of Chemistry 2020年第10期38卷 1091-1097页

作者： Lijun Sun Di Zhu Laura Olde Groote Beverborg Ruina Wang Yongjun Dang Mingming Ma Wei Li Biao Yu Deportment of Chemistry University of Science and Technology of Chino96 Jinzhai RoadHefeiAnhui 230026China State Key Laboratory of Bio-organic and Natural Products Chemistry Center for Excellence in Molecular SynthesisShanghai Institute of Organic ChemistryChinese Academy of Sciences345 Lingling RoadShanghai 200032China Key Laboratory of Metabolism and Molecular Medicine the Ministry of EducationDepartment of Biochemistry and Molecular BiologySchool of Basic Medical SciencesFudan UniersityShanghai 200032China Department of Medicinal Chemistry China Pharmaceutical University639 Lon gmian AvenueNanjingJiangsu 211198China

Summary of main observation and conclusion OSW-1 is a well-known natural saponin with potent antitumor activities.We have designed and pre-pared a small library of 22 OSW-1 analogues with a variety of p-acylamino-benzoyl groups installed at C2"of the xylose residue,wherein a regioselective(1>3)-glycosylation of arabinoside 3,4-diol has been achieved by manipulatian of the protecting groups on the imidate donors.Bioassays lead to new structure-activity relationships as well as two aplicable fluorescent probes,which are found to localize to lysosomes in HeLa cells and could be used in further antitumor mechanism studies of OSW-1 in living cells.

关键词： benzoyl analogues conclusion

Synthesis of (S)-(+)-tylophorine and its seco analogues using free radical reaction

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Science China Chemistry 2009年第9期52卷 1288-1299页

作者： WANG ZiWen WANG KaiLiang CUI MingBo WANG QingMin State Key Laboratory of Elemento-Organic Chemistry Tianjin Key Laboratory of Pesticide ScienceResearch Institute of Elemento-Organic ChemistryNankai UniversityTianjin 300071China

The synthesis of (S)-(+)-tylophorine and its seco analogues has been accomplished by using free radical reaction. -N-(2,3,6,7-Tetramethoxyphenanthren-9-ylmethyl)-2-bromomethylpyrrolidine (7) and -N-(2,3,6,7-tetramethoxyphenanthren-9-ylcarbonyl)-2-bromomethylpyrrolidine (9) have been obtained for the first time in three and two linear steps from 2,3,6,7-tetramethoxyphenanthrene-9-carboxylic acid (4), respectively. When bromide 7 was subjected to the action of tri-n-butyltin hydride and catalytic amount of azobisisobutyronitrile in acetonitrile at reflux, only a new structural N-((2,3,6,7-tetramethoxyphenanthren-9-yl)methyl)piperidine (2) was obtained in excellent yield, without expected (+)- ty- lophorine. As an alternative route, when bromide 9 was treated with azobisisobutyronitrile and tri-n-butyltin hydride in toluene at reflux, tylophorin-9-one (10) was provided in 33.6% yield. At the same time, a new structural (+)-N-((2,3,6,7-tetramethoxyphenanthren-9-yl)carbonyl)-2-methylpyrrolidine (11) was afforded as the main product in 65% yield. Notably, azobisisobutyronitrile plays dual roles in this reaction, and the possible mechanism has been described. Compounds 10 and 11 were reduced by lithium aluminum hydride to give (+)-tylophorine and (+)-N-((2,3,6,7-tetramethoxyphenanthren-9-yl) methyl)-2-methylpyrrolidine (3), respectively.

关键词： free radical reaction azobisisobutyronitrile tri-n-butyltin hydride (S)-(+)–tylophorine seco analogues

Synthesis and Antitumor Activity of Tanshinone analogues

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Chinese Journal of Chemistry 2003年第7期21卷 720-722页

作者：阿吉艾克拜尔.艾萨吕伟蔡俊超 Xinjiang Technical Institute of Physics & Chemistry Chinese Academy of SciencesUrumqiXinjiang 830011China Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 200031China

8,8-Dimethyl-5,6,7, 8-tetrahydrophenanthrene-3, 4-dione (3) and 8,8-dhnethyl-2-(1-hydroxy ethyl)-5,6,7,8-tetrahydrophe-nanthrene-3,4-dione (4), two analogues of the antitumor active tanshinone, were synthesized from anisole. The synthesized compounds 3 and 4 were shown to be highly active against leukemia P-388 cell line as assayed by in vitro MTT method.

关键词： synthesis tanshinone analogues

Synthesis of (+) 8-O-Cinnamyl-p-chlorogoniotriol and its analogues

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Chinese Chemical Letters 1999年第6期10卷 449-452页

作者： Hong CHEN Long En ZHOU Yan Jun ZHANG De Quan YU(Institute of Meteria Medica Chinese Academy of Medical Sciences &Peking Union Medical College. Beijing 100050) Institute of Meteria Medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

(+) 8-O-Cinnamyl-p-chlorogoniotriol (p-chlorohowjinol A) and its analogues have beensynthesized in nine steps from a-D-glucoheptonic-r-lactone. Pharmacological tests showed thatmost of the compounds possessed antitumo... 详细信息

关键词： Stereoselective synthesis (+) 8-O-cinnamy-p-chlorgoniotriol (p-chlorohowiibnol A) antitumor activiyty analogues

Sensorized tissue analogues enabled by a 3D-printed conductive organogel

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npj Flexible Electronics 2021年第1期5卷 51-58页

作者： Michael R.Crump Sophia L.Bidinger Felippe J.Pavinatto Alex T.Gong Robert M.Sweet Devin MacKenzie Department of Materials Science&Engineering University of WashingtonSeattleWAUSA Center for Research in Education and Simulation Technologies University of WashingtonSeattleWAUSA Department of Surgery University of WashingtonSeattleWAUSA Department of Mechanical Engineering University of WashingtonSeattleWAUSA

State-of-the-art tissue analogues used in high-fidelity,hands-on medical simulation modules can deliver lifelike appearance and feel but lack the capability to provide quantified,real-time assessment of practitioner performance.The monolithic fabrication of hybrid printed/textile piezoresistive strain sensors in a realistic Y/V plasty suture training pad is demonstrated.A class of 3D-printable organogels comprised of inexpensive and nonhazardous feedstocks is used as the sensing medium,and conductive composite threads are used as the electrodes.These organogels are comprised of a glycol-based deep-eutectic solvent(DES)serving as the ionic conductor and 3-trimethoxysilylmethacrylate-capped fumed silica particles serving as the gelating agent.Rheology measurements reveal the influence of fumed silica particle capping group on the mixture rheology.Freestanding strain sensors demonstrate a maximum strain amplitude of 300%,negligible signal drift,a monotonic sensor response,a low degree of hysteresis,and excellent cyclic stability.The increased contact resistance of the conductive thread electrodes used in place of wire electrodes do not make a significant impact on sensor performance.This work showcases the potential of these organogels utilized in sensorized tissue analogues and freestanding strain sensors for widespread applications in medical simulation and education.

关键词： stability analogues conductive