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Acrosin structure-based design,synthesis and biological activities of 7-azaindol derivatives as new acrosin inhibitors

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Chinese Chemical Letters 2011年第3期22卷 272-275页

作者： jun Hang Jiang Xue Fei Liu Can Hui Zhen you jun zhou Ju Zhu Jia Guo Lv Chun Quan Sheng Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China

A series of 7-azaindol derivatives were designed based on the homologous 3D model of human *** compounds were synthesized and evaluated for their human acrosin inhibitory activities in *** 7a,7i,7j,7k and 7n showed highly inhibitory activity against human *** three-dimensional structure-activity relationship was investigated through a CoMFA model,which provided valuable information to further study of potential human acrosin inhibitors.

关键词： Rational design Azaindole Synthesis Acrosin CoMFA

Acidic rearrangement of benzyl group in flavone benzyl ethers and its regioselectivity

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Chinese Chemical Letters 2015年第6期26卷 793-796页

作者： Chong-Qing Wang Xin Chen jun-Hang Jiang Hui Tang Kong-Kai Zhu you-jun zhou Can-Hui Zheng Ju Zhu School of Pharmacy Second Military Medical University School of Biology and Pharmaceutical Engineering Wuhan Polytechnic University Pharmacy Provincial Hospital Affiliated to Shandong University State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

The benzyl-substituted flavone compounds are rare in nature, while some of which have interesting biological activities. The total synthesis of benzyl-substituted flavone derivatives via the acidic rearrangement of benzyl groups in flavone benzyl ethers, and the complicated regioselectivity of the rearrangement were reported. The regioselectivity was proposed to be determined by the steric hindrance as well as the ease of electrophilic substitution reaction for benzyl cations at different positions of corresponding debenzylated fiavone compounds.

关键词： Benzyl-substituted flavone Acidic rearrangement of benzyl group Regioselectivity Quantum chemical calculation

Design, Synthesis and Biological Evaluation of Non-azole Inhibitors of Lanosterol 14α-Demethylase of Fungi

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Chinese Chemical Letters 2006年第9期17卷 1189-1192页

作者： Bin YAO you jun zhou Jü ZHU Jia Guo Lü Yao Wu LI jun CHENG Qing Feng JIANG Can Hui ZHENG School of Pharmacy Second Military Medicial University Shanghai 200433

Novel tetralin compounds were designed and synthesized on the three-dimensional model of lanosterol 14α-demethylase of Candida albicans. All of the lead compounds exhibited potent antifungal activities, especially compounds 16, 20. The mode of the action of the lead compounds was different from that of azoles. The present study affords the possibility to develop novel antifungal agents that specifically interact with the amino acid residues in the active site and avoid the serious toxicity arising from coordination binding with the heme of mammalian P450s.

关键词： Antifungal 2-aminotetralins lanosterol 14α-demethylase inhibitor.

Synthesis and biological evaluation of novel triazole derivatives as antifungal agents

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Chinese Chemical Letters 2013年第3期24卷 219-222页

作者： Hui Tang Can-Hui Zheng Xiao-Hui Ren Jia Liu Na Liu Jia-Guo Lv Ju Zhu you-jun zhou Pharmacy Provincial Hospital Affiliated to Shandong University School of Pharmacy Second Military Medical University

A series of 1-（benzylamino）-2-（2,4-difiuorophenyl）-3-（lH-1,2,4-triazol-l-yl）propan-2-ols compounds were synthesized and evaluated for their antifungal activities in vitro. The results showed that compounds 6A and 6B exhibited good antifungal activity. Compound 6tt8 showed the strongest antifungal activity, which was significantly higher than that of the lead compounds and positive-control drugs Fluconazole and Itraconazole. In particular, the antifungal activity of compound 6/18 against Candida albicans and Candida krusei （MIC80 both at 0.00097 p.g/mL） was 515 and 64 times that of Fluconazole, respectively. The structure-activity relationships of the synthesized compounds were discussed, and the docking model of the target compounds with fungal lanosterol 14a-demethylase （CYP51） was analyzed.

关键词： TriazoleAntifungalStructure-activity relationshipCYP51

Total Synthesis of Phakellistatin 13 by Solution Method

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Chinese Chemical Letters 2006年第8期17卷 995-998页

作者： Qing Feng JIANG you jun zhou Jian Zhong YAO Jia Guo LU Ju ZHU Chun Quan SHENG Can Hui ZHENG Bing YAO Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433

Phakellistatin 13 is a good antitumor lead compound isolated from halobios. It was synthesized first time by solution method in combination of stepwise coupling and segment condensation. Final deprotection and cyclization were achieved according to our designed method, which was different from the reported process. The spectral data of synthetic product is consisted with literatureal data of natural product. Total synthesis of phakellistatin 13 is a significant achievement to further study of its derivatives and developing novel antitumor drugs.

关键词： Phakellistatin 13 solution-phase synthesis cyclopeptide.

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男性非甾体类抗生育化合物的研究进展

生殖与避孕 2010年第6期30卷 402-407页

作者：宁微微朱驹周有骏吕加国解放军第二军医大学药学院上海200433

男性非甾体避孕药是抗生育药物研究的重要方向之一。近年来随着对精子支持细胞、精子顶体酶、精子离子通道等抗生育药物重要靶点研究的不断深入,基于这些新靶标的非甾体抗生育化合物研究取得了显著进展。其中一些小分子顶体酶抑制剂、... 详细信息

男性非甾体避孕药是抗生育药物研究的重要方向之一。近年来随着对精子支持细胞、精子顶体酶、精子离子通道等抗生育药物重要靶点研究的不断深入,基于这些新靶标的非甾体抗生育化合物研究取得了显著进展。其中一些小分子顶体酶抑制剂、男性避孕复合物的临床前研究与临床研究值得深入研究。本文就近年来非甾体小分子抗生育化合物研究现状进行了系统综述。这些研究为设计新型男性非甾体抗生育药物提供了参考。

关键词：男性避孕非甾体支持细胞精子顶体酶抑制剂影响精子化合物离子通道阻滞剂

Design,synthesis,and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins:Characteristics of broad-spectrum protein binding and its effects on anti-tumor activity

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Design,synthesis,and activity evaluation of broad-spectrum s...

Mechanistic insight into the synergy between nickel single atoms and nanoparticles on N-doped carbon for electroreduction of CO2

2011年全国药物化学学术会议——药物的源头创新

作者： Can-Hui Zheng,Hui Yang,you-jun zhou~*,Ju Zhu~* School of Pharmacy,Second Military Medical University,325 Guohe Road,Shanghai,China

The anti-apoptotic members of the Bcl-2 protein family have become attractive targets for anti-cancer drug development,and broad-spectrum small-molecule inhibitors targeting it may be ideal anti-cancer *** the basis of the comparison of the structure of the Bim BH3:Bcl-x complex and that of the ABT-737:Bcl-x complex,a series of class A compounds were *** compounds

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来源： cnki会议评论

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Journal of Energy Chemistry 2025年第1期100卷 327-336页

作者： Mingdong Sun Wenwen Guan Cailing Chen Chao Wu Xiaoling Liu Biao Meng Tao Chen Yu Han jun Wang Shibo Xi Yu zhou State Key Laboratory of Materials-Oriented Chemical Engineering College of Chemical Engineering Nanjing Tech University Advanced Membranes and Porous Materials Center Physical Sciences and Engineering Division King Abdullah University of Science and Technology Institute of Sustainability for Chemicals Energy and Environment A*STAR (Agency for Science Technology and Research) College of Materials Science and Engineering Sichuan University

The synergy of single atoms （SAs） and nanoparticles （NPs） has demonstrated great potential in promoting the electrocatalytic carbon dioxide reduction reaction （CO2RR）;however,the rationalization of the SAs/NPs proportion remains one challenge for the catalyst ***,a Ni2+-loaded porous poly（ionic liquids）(PIL) precursor synthesized through the free radical self-polymerization of the ionic liquid monomer,1-allyl-3-vinylimidazolium chloride,was pyrolyzed to prepare the Ni,N co-doped carbon materials,in which the proportion of Ni SAs and NPs could be facilely modulated by controlling the annealing *** catalyst Ni-NC-1000 with a moderate proportion of Ni SAs and NPs exhibited high efficiency in the electrocatalytic conversion of CO2into *** Ni K-edge X-ray absorption near-edge structure （XANES） spectra and theoretical calculations were conducted to gain insight into the synergy of Ni SAs and *** charge transfer from Ni NPs to the surrounding carbon layer and then to the Ni SAs resulted in the electron-enriched Ni SAs active *** the electroreduction of CO2,the coexistence of Ni SAs and NPs strengthened the CO2activation and the affinity towards the key intermediate of*COOH,lowering the free energy for the potential-determining*CO2→*COOH step,and therefore promoted the catalysis efficiency.

关键词： Activation energy

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重视脂蛋白胆固醇的检测

上海医学检验杂志 2001年第6期16卷 358-360页

作者：有军任丽敏周强上海市浦东新区公利医院上海200135

目的了解病人血清中高、低密度脂蛋白胆固醇 (HDL - C,L DL - C)和载脂蛋白 A、B(Aop- A、B)的关系。方法将市场上的某公司载脂蛋白检测试剂和具国际标准化的试剂 ,对病人血清作对比测定 ,了解差距 ;同时对血清作 HDL - C、L DL - C,总... 详细信息

目的了解病人血清中高、低密度脂蛋白胆固醇 (HDL - C,L DL - C)和载脂蛋白 A、B(Aop- A、B)的关系。方法将市场上的某公司载脂蛋白检测试剂和具国际标准化的试剂 ,对病人血清作对比测定 ,了解差距 ;同时对血清作 HDL - C、L DL - C,总胆固醇 (TC) ,三酰甘油 (TG)测定。结果实验用国产载脂蛋白试剂和标准化试剂的检测结果对比差距很大 ,HDL - C、L DL - C含量和相应 Aop A1、Aop B间无明确的数量关系。结论对高血脂和糖尿病病人作心脏损害的危险程度的了解时 ,应重视作 HDL - C、L DL -

关键词：脂蛋白高脂血症脂蛋白胆固醇检测