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Improving the positional adaptability:structurebased design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

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Acta Pharmaceutica Sinica B 2020年第2期10卷 344-357页

作者： Kaijun Jin Minjie Liu chunlin Zhuang Erik De clercq christophe Pannecouque Ge Meng fener c.en engineering center of catalysis and Synthesis for chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai engineering center of Industrial Asymmetric catalysis for chiral Drugs Shanghai 200433China Rega Institute for Medical Research KU LeuvenLeuven B-3000Belgium

In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines(NP-DATAs),synthesis of a series of novel biphenyl-substituted diaryltriazines(BP-DATAs)with a flexible side chain attached at the c-6 position is *** compounds exhibited excellent potency against wild-type(WT)HIV-1 with Ec50 values ranging from 2.6 to 39 nmol/L and most of them showed low nanomolar anti-viral potency against a panel of HIV-1 mutant *** 5 j and 6 k had the best activity against WT,single and double HIV-1 mutants and reverse transcriptase(RT)enzyme comparable to two reference drugs(EFV and ETR)and our lead compound NP-DATA(1).Molecular modeling disclosed that the side chain at the c-6 position of DATAs occupied the entrance channel of the HIV-1 reverse transcriptase non-nucleoside binding pocket(NNIBP)attributing to the improved *** preliminary structure-activity relationship and PK profiles were also discussed.

关键词： HIV-1 NNRTIs NP-DATAs BP-DATAs Positional adaptability Molecular modeling

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Benzaldehyde lyase-catalyzed enantioselective c-c bond formation and cleavage:A review

Green Synthesis and Catalysis

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Green Synthesis and catalysis 2022年第4期3卷 317-326页

作者： Zhiran Ju Junde Xu Zhiyun Li Jingjie Fang Menglan Li Daniel c.Howell fener c.en Institute of Pharmaceutical Sc.ence and Technology Collaborative Innovation Center of Yangtze River Delta Region Green PharmaceuticalsZhejiang University of TechnologyHangzhou 310014China engineering center of catalysis and Synthesis for chiral Molecules Fudan UniversityShanghai 200433China Shanghai engineering center of Industrial Asymmetric catalysis for chiral Drugs Shanghai 200433China Department of Pharmaceutical Sc.ences Oregon State UniversityCorvallis 97331United States

Benzaldehyde lyase(BAL)is an enzyme which was originally found from Pseudomonas fluorescens biovar *** has long been used in the formation of a c-c *** can exclusively yield(R)-enantioselective products from the synthesis ofα-hydroxy ketones and has so far been explored as an important enzyme to prepare the corresponding intermediate of *** to its substrate spectrum and stereospecificity,this enzyme extends the synthetic potential for carboligations *** this review,we highlight the biotransformation applications of BAL in recent years,some of which have achieved intriguing results and provided the theoretical basis for drug development and industrial purpose in the future.

关键词： Benzaldehyde lyase Pseudomonas fluorescens biovar I c-c bond (R)-enantioselective

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Unified total synthesis of eburnamine-vincamine indole alkaloids based on catalytic asymmetric hydrogenation/lactamization cascade

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Green Synthesis and catalysis 2022年第3期3卷 291-293页

作者： Wen Zhang Yansong Xue Srihari Konduri Guodan Lin Mengjuan Wu Pei Tang fener c.en Sichuan Research center for Drug Precision Industrial Technology West China School of PharmacySichuan UniversityChengdu 610041China engineering center of catalysis and Synthesis for chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai engineering center of Industrial Asymmetric catalysis for chiral Drugs Shanghai 200433China Skaggs School of Pharmacy and Pharmaceutical Sc.ence UC San Diego9500 Gilman DriveLa JollaCA 92093-0934United States

The enantioselective total synthesis of representative members of the eburnamine-vincamine alkaloids(+)-vincamine,(-)-eburnamonine,and(-)-criocerine has been *** synthesis took advantage of a highly stereoselective Ir-catalyzed hydrogenation/lactamization cascade reaction,which allows for the stereo-selective construction of the c/D rings as well as the installation of the critical cis-c20/c21 relative stereo-chemistry of the eburnamine-vincamine alkaloid skeleton in one pot.

关键词： Indole alkaloid Imine Asymmetric hydrogenation Natural product enantioselective synthesis

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Visible-light-driven intramolecular xanthylation of remote unactivated c(sp^(3))-H bonds

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Green Synthesis and catalysis 2023年第4期4卷 350-354页

作者： Hang c.en Yang Zhou Panpan Lei Haifeng Wang Qiongjiao Yan Roberta Properzi Wei Wang Linhai Jing fener c.en Pharmaceutical Research Institute Wuhan Institute of TechnologyWuhan 430205China chemical Synthesis and Pollution control Key Laboratory of Sichuan Province China West Normal UniversityNanchong 637009China engineering center of catalysis and Synthesis for chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai engineering center of Industrial catalysis for chiral Drugs Shanghai 200433China Max-Planck-Institut für Kohlenforschung Mülheim an der Ruhr 45470Germany

Visible light-mediated site-specific c(sp^(3))-H xanthylation of amides has been accomplished using *** N-centered radicals generated by light initiation of N-xanthylamide substrates undergo 1,5-hydrogen atom transfer to form benzylic or alkyl radical intermediates under metal-and catalyst-free *** method exhibits a broad substrate scope,high functional group tolerance,and high ***,this strategy provides straightforward access to a range of derivatives through the subsequent elaboration of the xanthate group.

关键词： c-H functionalization 1,5-Hydrogen atom transfer Photocatalytic Site-specific Xanthylation

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S-DAPYs类似物的分子设计、合成及抑制HIV-1的活性研究

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中国科学：化学 2015年第9期45卷 961-967页

作者：万正勇陈芬儿 Erik De clercq Dirk Daelemans christophe Pannecouque 复旦大学化学系上海200433 复旦大学生物医学研究院上海200433 Rega Institute for Medical Research Katholieke Universiteit Leuven

我们以已上市的etravirine和正在临床研究的VRX-480773两个逆转录酶抑制剂为模板，通过杂交这两个化合物的药效团，获得含酰胺片段的S—DAPYs类似物，该类似物对野生型HIV-1病毒株具有中等强度抑制活性．而Maurizio所发现的另一类无酰... 详细信息

我们以已上市的etravirine和正在临床研究的VRX-480773两个逆转录酶抑制剂为模板，通过杂交这两个化合物的药效团，获得含酰胺片段的S—DAPYs类似物，该类似物对野生型HIV-1病毒株具有中等强度抑制活性．而Maurizio所发现的另一类无酰胺片段的***类似物却表现出优异的抑制活性．为了考察酰胺片段对S-DAPYs类似物抑制HIV-1活性的影响，本文合成了一系列无酰胺片段的S—DAPYs类似物．生物活性结果表明，3个化合物（6g、6m和6s）对野生型HIV-1具有中等强度抑制活性（Ec50在6．5～15．4μmol／L范围内），弱于相应的具有酰胺片段的类似物．此外，分子模拟还揭示了酰胺片段可与K103形成至关重要的氢键作用，这为新型非核苷类逆转录酶抑制剂的设计奠定了理论基础．

关键词：艾滋病逆转录酶抑制剂分子杂交酰胺片段氢键分子模拟

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