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Design,synthesis and antifungal activities in vitro of novel tetralin compounds

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Chinese Chemical Letters 2008年第3期19卷 264-268页

作者： hui Tang You Jun Zhou Yao Wu Li Jia Guo Lv can hui zheng Jun Chen Ju Zhu Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China

Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhihitars of fungi.

关键词： Antifungal Chiral tetralins Lanosterol 14α-demethylase Design Synthesis

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.

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.

Synthesis and biological evaluation of 5,6,7-trimethoxy-1-benzylidene-3,4-dihydro-naphthalen-2-one as tubulin-polymerization inhibitors

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Chinese Chemical Letters 2015年第5期26卷 607-609页

作者： Jun-Hang Jiang can-hui zheng Chong-Qing Wang Juan Wang Wei Tian Chao Yang Yun-Long Song Yong Hu Ju Zhu You-Yun Zhou School of Pharmacy Second Military Medical University Shanghai Institute of Pharmaceutical Industry Department of Neonatology Shanghai Children's HospitalShanghai Jiao Tong University

A series of new combretastatin-A4 analogs were synthesized, in which a six-membered ring connects the linking bridge and A ring, and their tumor cell growth and tubulin-polymerization inhibitory activity were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors, Compounds 1b with amino substituted on position 3 of B ring conferred optimal bioactivity, higher than that of the lead compound 22b and equivalent to that of CA-4. The binding modes of these compounds to tuhulin were obtained by molecular docking, which can explain the structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.

关键词： Tubulin polymerization inhibitor Antitumor agent Combretastatin-A4 analog

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...

Decoding the nexus:branched-chain amino acids and their connection with sleep,circadian rhythms,and cardiometabolic health

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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Neural Regeneration Research 2025年第5期20卷 1350-1363页

作者： hui Li Laurent Seugnet Department of Neurology Xijing HospitalXi’anShaanxi ProvinceChina Centre de Recherche en Neurosciences de Lyon Integrated Physiology of the Brain Arousal Systems(WAKING)UniversitéClaude Bernard Lyon 1INSERM U1028CNRS UMR 5292BronFrance

The sleep-wake cycle stands as an integrative process essential for sustaining optimal brain function and,either directly or indirectly,overall body health,encompassing metabolic and cardiovascular *** the heightened metabolic activity of the brain,there exists a considerable demand for nutrients in comparison to other *** these,the branched-chain amino acids,comprising leucine,isoleucine,and valine,display distinctive significance,from their contribution to protein structure to their involvement in overall metabolism,especially in cerebral *** the first amino acids that are released into circulation post-food intake,branched-chain amino acids assume a pivotal role in the regulation of protein synthesis,modulating insulin secretion and the amino acid sensing pathway of target of ***-chain amino acids are key players in influencing the brain's uptake of monoamine precursors,competing for a shared *** their involvement in protein synthesis,these amino acids contribute to the metabolic cycles ofγ-aminobutyric acid and glutamate,as well as energy ***,they impact GABAergic neurons and the excitation/inhibition *** rhythmicity of branchedchain amino acids in plasma concentrations,observed over a 24-hour cycle and conserved in rodent models,is under circadian clock *** mechanisms underlying those rhythms and the physiological consequences of their disruption are not fully *** sleep,obesity,diabetes,and cardiovascular diseases can elevate branched-chain amino acid concentrations or modify their oscillatory *** mechanisms driving these effects are currently the focal point of ongoing research efforts,since normalizing branched-chain amino acid levels has the ability to alleviate the severity of these *** this context,the Drosophila model,though underutilized,holds promise in shedding new light on these *** findings indicate its po

关键词： branched-chain amino acids cardiovascular health circadian clock drosophila insulin metabolism sleep γ-aminobutyric acid

益气活血化瘀法干预老年股骨干骨折患者术后高凝状态临床研究

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安徽中医药大学学报 2017年第3期36卷 25-28页

作者：李灿辉吴征杰佛山市中医院骨科广东佛山528000

目的观察益气活血化瘀法对老年股骨干骨折患者术后高凝状态的影响。方法将60例老年股骨干骨折患者随机分为中药组和西药组各30例,两组均采用闭合穿针髓内钉治疗,中药组术后给予益气活血化瘀法治疗,西药组给予利伐沙班治疗,比较两组干预... 详细信息

目的观察益气活血化瘀法对老年股骨干骨折患者术后高凝状态的影响。方法将60例老年股骨干骨折患者随机分为中药组和西药组各30例,两组均采用闭合穿针髓内钉治疗,中药组术后给予益气活血化瘀法治疗,西药组给予利伐沙班治疗,比较两组干预前后D-二聚体、凝血酶原时间(prothrombin time,PT),血小板计数(platelet count,PLC)以及患肢周径的变化。结果两组患者术后凝血指标均较术前明显降低,差异均有统计学意义(P0.05)。两组术后均无下肢静脉血栓发生。中药组干预前后患肢周径的变化值大于西药组,差异有统计学意义(P<0.05)。结论益气活血化瘀法与利伐沙班均能改善股骨干骨折患者术后的高凝状态,预防DVT的发生,但益气活血化瘀法治疗效果优于利伐沙班。

关键词：股骨干骨折高凝状态益气活血化瘀法利伐沙班

RF Optimizer Model for Predicting Compressive Strength of Recycled Concrete

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Journal of Wuhan University of Technology(Materials Science) 2025年第1期40卷 215-223页

作者： LIU Lin WANG Liuyan WANG hui SUN Huayue School of Civil Engineering and Architecture Shenyang UniversityShenyang 110000China

Traditional machine learning(ML)encounters the challenge of parameter adjustment when predicting the compressive strength of reclaimed *** address this issue,we introduce two optimized hybrid models:the Bayesian optimization model(B-RF)and the optimal model(Stacking model).These models are applied to a data set comprising 438 observations with five input variables,with the aim of predicting the compressive strength of reclaimed ***,we evaluate the performance of the optimized models in comparison to traditional machine learning models,such as support vector regression(SVR),decision tree(DT),and random forest(RF).The results reveal that the Stacking model exhibits superior predictive performance,with evaluation indices including R2=0.825,MAE=2.818 and MSE=14.265,surpassing the traditional ***,we also performed a characteristic importance analysis on the input variables,and we concluded that cement had the greatest influence on the compressive strength of reclaimed concrete,followed by ***,the Stacking model can be recommended as a compressive strength prediction tool to partially replace laboratory compressive strength testing,resulting in time and cost savings.

关键词： machine learning recycled concrete compressive strength