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Synthesis and Evaluation of Graveolinine Derivatives

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Synthesis and Evaluation of Graveolinine Derivatives

河南省化学会2016年学术年会

作者： Ting wang Ying Chen Yacheng Yang Wen Luo chaojie wang Key Laboratory of Natural Medicine and Immuno-Engineering Henan University

A series of graveolinine derivatives were synthesized from 1-(2-aminophenyl) ethanone by four steps, all the compounds were characterized by H NMR, C NMR and HRMS. These compounds showed potent inhibitory activity for both ACh E and BCh E. Compound 5f exhibited the best inhibitory activity for acetylcholinesterase(ACh E) and had surprisingly potentinhibitory activity for Butyrylcholinesterase(BCh E), with IC50 values of 1.33 m M and 0.16 m M, respectively. The results from a Lineweaver–Burk plot and molecular modeling studyindicated non-competitive inhibition of ACh E by compound5 f. Therefore, these graveolinine derivatives should be thoroughly studied for the treatment of Alzheimer’s disease.

关键词： Graveolinine derivatives Acetylcholinesterase Butyrylcholinesterase Alzheimer’s disease

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薄膜热电偶在高温下的防氧化机理

材料研究学报 2017年第2期31卷 123-128页

作者：王超杰陈鹏袁广民王博国防科学技术大学长沙410073 空间物理重点试验室北京100076 航天科技集团公司四院四十四所西安710025 西北工业大学空天微纳系统教育部重点实验室西安710072 北京市第八中学北京100033

根据金属材料的高温氧化和防氧化特性,研究了不同保护膜对薄膜热电偶防氧化的机理,提出使用SiO_2、SiO_xN_y薄膜作为抗氧化的保护膜。用磁控溅射法分别制备了具有SiO_2和SiO_xN_y保护膜和无保护膜的Ni Cr-Ni Si薄膜热电偶样品,并对三种... 详细信息

根据金属材料的高温氧化和防氧化特性,研究了不同保护膜对薄膜热电偶防氧化的机理,提出使用SiO_2、SiO_xN_y薄膜作为抗氧化的保护膜。用磁控溅射法分别制备了具有SiO_2和SiO_xN_y保护膜和无保护膜的Ni Cr-Ni Si薄膜热电偶样品,并对三种样品进行高温热处理。结果表明,根据不同样品的XRD图谱中NiO峰的强度,在800℃高温下有SiO_xN_y保护膜的样品其抗氧化效果约为有SiO_2保护膜样品的3~5倍。同时发现,在高温处理过程中SiO_xN_y薄膜发生轻微氧化使SiO_xN_y薄膜结构更致密,有利于提高SiO_xN_y薄膜对温度敏感薄膜的抗氧化性能。

关键词：材料表面与界面薄膜热电偶高温防氧化氮氧化硅保护膜

Synthesis of β,β-Directly Linked Cyclic Porphyrin Arrays

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Synthesis of β,β-Directly Linked Cyclic Porphyrin Arrays

中国化学会第四届卟啉与酞菁学术研讨会

作者： Kaisheng wang chaojie wang Bangshao Yin Mingbo Zhou Ling Xu Jianxin Song Key Laboratory of Chemical Biology ＆ Traditional Chinese Medicine Research（Ministry of Education） Key Laboratory of Application and Assemble of Organic Functional Molecules Hunan Normal University

Porphyrin arrays have attracted particular attention due to their potential applications for nano-electronic devices,sensors,and soft materials possessing interesting nonlinear optical properties [1].When corresponding β-borylated porphyrins react with β-bromoporphyrins,β,β-directly linked cyclic porphyrin arrays could be successfully afford [2,3]（Fig.1）.Further studies on theirs photophysical properties,electrochemical properties,as well as extension of this coupling strategy for the synthesis of more elaborate porphyrin arrays are in progress in our laboratory.

关键词： porphyrin arrays directly bridged Suzuki-Miyaura cross-coupling

MINS, a Novel Naphthalimide-Polyamine Conjugate, Induced Apoptosis Depending on p53 Status in Human Colon Cancer Cells

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Open Journal of Apoptosis 2014年第4期3卷 59-69页

作者： Ming Li Tao Yang Fujun Dai Qian Li Yahong Zhang Songqiang Xie chaojie wang Institute of Chemical Biology Pharmaceutical College of Henan University Kaifeng China The Key Laboratory of Natural Medicine and Immuno-Engineering Henan University Kaifeng China

Natural polyamine is an ideal antitumor drug carrier because of the great requirement difference between cancer cells and normal cells. Previous data demonstrated that many cytotoxic drugs conjugated with natural or synthetic polyamines have potent antitumor effects. Up to now, the antitumor mechanism of conjugates of naphthalimides with polyamine remains poorly understood in human colon cancer cells. The aim of this study is to evaluate the effect of MINS (a novel naph-thalimide-polyamine conjugate) and mechanism of MINS in human colon cancer cells. Mitochondrial toxicity, which was generated by ROS from mitochondria electron transport chain, might be a major factor in MINS-inducted apoptosis. Our data also demonstrated that MINS-mediated cell apoptosis depend on p53 status, for MINS induced Caco-2 cells (p53 null) only necrosis but not apoptosis. Furthermore, the apoptotic effect of MINS is stronger than that of Amonafide, the parent drug of MINS. Our data suggested that the MINS-mediated cell apoptosis depend on p53 in human colon cancer cells.

关键词： Naphthalimide-Polyamine Conjugates Apoptosis p53 Mitochondrial Transmembrane Potential Oxidative Stress

Study of the Toxicity of 1-Bromo-3-Chloro-5,5-Dimethylhydantoin to Zebrafish

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Biomedical and Environmental Sciences 2011年第4期24卷 383-390页

作者： LI WanFang WEI JinFeng JIN HongTao HUANG MingFang ZHANG JingXuan LI ChengHe CHEN chaojie LIU Chang wang AiPing Institute of Materia Medica Chinese Academy of Medieal Sciences & Peking Union Medical College Beijing100050 China

Objective 1-Bromo-3-chloro-5,5-dimethylhydantoin （BCDMH） is a solid oxidizing biocide for water *** objective of this study was to investigate the toxic effect of BCDMH on *** The developmental toxicity of BCDMH on zebrafish embryos and the dose-effect relationship was *** effect of BCDMH exposure on histopathology and tissue antioxidant activity of adult zebrafish were observed over *** Exposure to 4 mg/L BCDMH post-fertilization was sufficient to induce a number of developmental malformations,such as edema,axial malformations,and reductions in heart rate and hatching *** no observable effects concentration of BCDMH on zebrafish embryo was 0.5 mg/*** 96 h exposure,the 50% lethal concentration （95% confidence interval （CI）） of BCDMH on zebrafish embryo was 8.10 mg/L （6.15-11.16 mg/L）.The 50% inhibitory concentration （95% CI） of BCDMH on hatching rate was 7.37 mg/L （6.33-8.35 mg/L）.Histopathology showed two types of responses induced by BCDMH,defensive and *** extreme responses were marked hyperplasia of the gill epithelium with lamellar fusion and epidermal *** histopathologic changes in the gills after 10 days exposure were accompanied by significantly higher catalase activity and lipid *** These results have important implications for studies on the toxicity and use of BCDMH and its analogs.

关键词： Developmental toxicity Histopathological effects 1-Bromo-3-chloro-5 5-dimethylhydantoin (BCDMH)

The synthesis and characterization of 2,7-bis(4-bromophenyl)-9-hexylcarbazole

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The synthesis and characterization of 2,7-bis(4-bromophenyl)...

河南省化学会2016年学术年会

作者： wang chaojie Li Kui Yang Zhenqiang Sun Minqing Yang Ruina Institute of Chemistry Henan Academy of Sciences

The derivatives of carbazole designed as blue-light chromospheres, have drawn much attention duo to their unique structures and excellent luminous properties in the electroluminescence. The bromine of2,7-bis(4-bromophenyl)-9-hexylcarbazole can carry out a variety of chemical modification. This method can improve the solubility of the product and the low temperature of the *** an argon atmosphere, 2,7-dibromo-9-hexylcarbazole(5.87 g), P-bromophenylboronic acid(6.53g) and tetrakistriphenylphosphine palladium(40 mg) were dissolved in toluene(20 ml). A 2M aqueous potassium phosphate solution(5ml) was added and the mixture was heated under reflux for 8 *** reaction mixture was poured into water and extracted with CH2Cl2. The organic layer was dried over Mg SO4, filtered and the solvent was removed by rotary evaporation. The product was isolated by recrystallization using toluene-Me OH mixed solvent. The product was a colorless solid(5.26 g). Purity97.5%, yield 65.4%. m.p.: 221.7-222.9 ℃. H NMR(400 MHz, CDCl3), δ: 0.841-0.876(3H, t),1.256-1.887(6H,m),1.869-1.943(2H,m),4.339-4.375(2H,t),7.409-7.433(2H,dd),7.520-7.522(2H,d),7.561-7.616(8H,m),8.113(1H,s),8.134(1H,s).

关键词： 2,7-dibromocarbazol 2,7-bis(4-bromophenyl)-9-hexyl-9H-carbazole

池沸腾孤立气泡生长过程中微液层蒸发影响的实验和模拟耦合分析

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化工学报 2021年第5期72卷 2514-2527页

作者：潘丰王超杰母立众贺缨大连理工大学能源与动力学院辽宁大连116024

微液层蒸发是沸腾过程中重要的换热机理。本文旨在通过单个气泡池沸腾实验中测得的气泡动态参数探究孤立气泡生长过程中加热表面的换热机理。首先通过沸腾池和加热表面的严格设计实现了单个气泡沸腾。进一步通过对孤立气泡生长时序图像... 详细信息

微液层蒸发是沸腾过程中重要的换热机理。本文旨在通过单个气泡池沸腾实验中测得的气泡动态参数探究孤立气泡生长过程中加热表面的换热机理。首先通过沸腾池和加热表面的严格设计实现了单个气泡沸腾。进一步通过对孤立气泡生长时序图像的处理,得到了气泡在一个生长周期内气泡直径、纵横比以及气泡根部基圆半径的变化。对比发现,气泡生长速率与气泡根部基圆半径随时间的变化呈现显著正相关,而与大液层区域的变化相关程度较低,这表明微液层蒸发直接影响气泡体积变化,在孤立气泡沸腾过程中起主导作用。在此基础上进一步建立了加热表面换热过程的数值模型,基于实验中测得的气泡动态参数对气泡底层的微液层厚度进行了预测;通过多次迭代计算并匹配气泡生长速率和加热棒的温度发现,当表面过热度为4.82 K时,气泡底层微液层厚度约为3.43μm,与相关文献中的微液层厚度测量值基本一致,进一步证实了微液层蒸发在孤立气泡沸腾换热过程中的重要性。本研究揭示了孤立气泡池沸腾过程中近壁面处的换热机制,为进一步的孤立气泡沸腾传热过程数值模拟奠定了理论基础。

关键词：相变蒸发气泡气泡生长速率基圆半径变化微液层厚度预测

The synthesis and characterization of(7-bromo-9,9-dimethyl-9H-fluoren-2-yl)methanol

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The synthesis and characterization of(7-bromo-9,9-dimethyl-9...

河南省化学会2016年学术年会

作者： Chen Pengli wang chaojie Qu Fengbo Yang Zhenqiang Yang Ruina Institute of Chemistry Henan Academy of Sciences

Organic electroluminescent materials are one of the hotspot in the field of photoelectric information functional materials. Fluorene derivatives have attracted considerable attention in recent years as organic light-emitting materials with development prospect and practical value of blue light emitting materials.(7-bromo-9,9-dimethyl-9H-fluoren-2-yl) methanol is a very promising blue-ray material *** nitrogen atmosphere, 7-bromo-9,9-dimethyl-9H-fluorene-2-carbaldehyde was synthesized with THF as solvent and 2,7-dibromo-9,9-dimethylfluorene as starting material at-78 °C. n-Bu Li was slowly added drop wise. After stirring for 1 hr, DMF was added at-78 °C. The reaction solution was poured into HCl and extracted with ethyl acetate. Recrystallization by Me OH as yellow solid. Yield: 52%。1HNMR(400 MHz, DMSO-d6), δ/ppm: 10.053(s,1H), 8.105-8.085(d, J=7.96 Hz, 2H), 7.956-7.914(m,3H), 7.622-7.597(m, 1H), 1.501(s, 6H).(7-bromo-9,9-dimethyl-9H-fluoren-2-yl)methanol was synthesized with reduction of7-bromo-9,9-dimethyl-9H-fluorene-2-carbaldehyde by Na BH4. Recrystallization by Me OH as white solid. Yield: 90%.1HNMR(400 MHz, DMSO-d6), δ/ppm:7.796-7.741(m, 3H), 7.523-7.486(m, 2H), 7.315-7.293(m,1H), 5.256-5.227(t, J=5.80 Hz 1H), 4.572-4.558(d, J=5.60 Hz, 2H), 1.438(s, 1H).

关键词： 2,7-dibromo-9,9-dimethylfluorene 7-bromo-9,9-dimethyl-9H-fluorene-2-carbaldehyde (7-bromo-9,9-dimethyl-9H-fluoren-2-yl) methanol

二元酸茄呢醇乳糖和麦芽糖糖酯合成及生理活性测试研究

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有机化学 2003年第10期23卷 1102-1106页

作者：王超杰宋金勇赵瑾河南大学特种功能材料省级重点实验室开封475001

七个二元酸茄呢基单酯分别与溴代乙酰乳糖和溴代乙酰麦芽糖在四丁基溴化铵催化下反应生成对应的糖酯 ,制得的十四个化合物均为新化合物 ,其结构经过了元素分析、IR ,1HNMR和MS确证 .并对六个化合物做了KB(人口腔上皮癌细胞 )、Bel 740 ... 详细信息

七个二元酸茄呢基单酯分别与溴代乙酰乳糖和溴代乙酰麦芽糖在四丁基溴化铵催化下反应生成对应的糖酯 ,制得的十四个化合物均为新化合物 ,其结构经过了元素分析、IR ,1HNMR和MS确证 .并对六个化合物做了KB(人口腔上皮癌细胞 )、Bel 740 2 (人肝癌细胞 )、HCT 8(人结肠癌细胞 )三种癌细胞初步生理活性测试 .

关键词：二元酸茄呢醇乳糖麦芽糖糖酯合成生理活性测试溴代乳糖溴代麦芽糖药物