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Photocatalytic performance of TiO_2 immobilized on polystyrene (PS) thin film for mineralization of pollutants 被引量:12
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作者 GAO Yuan, YU Wei, CHEN Baohua, MA Yongxiang, and LI HulinDepartment of Chemistry, Lanzhou University, Lanzhou 730000, China (Receeived 2002-02-26) 《Rare Metals》 SCIE EI CAS CSCD 2003年第2期137-143,共7页
A new photocatalyst, TiO_2 powder immobilized on polystyrene (PS) thin films,was prepared using a novel method and its photocatalytic activity on the photodegradation ofacridine dye in aqueous solution was tested. By ... A new photocatalyst, TiO_2 powder immobilized on polystyrene (PS) thin films,was prepared using a novel method and its photocatalytic activity on the photodegradation ofacridine dye in aqueous solution was tested. By this method, the crystal form and grain size of theimmobilized TiO_2 were well maintained. Compared with TiO_2 powder, the photocatalytic activity ofTiO_2/PS thin films was not significantly reduced. The catalyst is stable and can be reused severaltimes without the loss of activity, which makes wastewater treatment using this photocatalyticdegradation technique of this way possible in the practical application. 展开更多
关键词 physical chemistry loaded photocatalyst TiO_2 acridine dye fluidifying sedimentation container
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吖啶类化合物在抗肿瘤方面的研究进展 被引量:11
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作者 郎许亮 栾旭东 +1 位作者 高春梅 蒋宇扬 《化学进展》 SCIE CAS CSCD 北大核心 2012年第8期1497-1505,共9页
吖啶类衍生物是一类含氮的有机杂环化合物,由于其在抗炎、抗菌及抗肿瘤方面体现了较好的生物活性而受到了广泛关注。本文对近年来吖啶类化合物在抗肿瘤方面的国内外研究成果进行了综述,对其主要作用靶点如端粒酶、拓扑异构酶Ⅰ/Ⅱ、微... 吖啶类衍生物是一类含氮的有机杂环化合物,由于其在抗炎、抗菌及抗肿瘤方面体现了较好的生物活性而受到了广泛关注。本文对近年来吖啶类化合物在抗肿瘤方面的国内外研究成果进行了综述,对其主要作用靶点如端粒酶、拓扑异构酶Ⅰ/Ⅱ、微管蛋白、ABCG2/P-glycoprotein(P-gP)以及蛋白激酶等方面的研究进行了介绍,并指出该类化合物的发展方向及应用前景。 展开更多
关键词 吖啶 抗肿瘤 靶点
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微波辐射下9-芳基-10-对甲苯基多氢吖啶衍生物的合成 被引量:5
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作者 王香善 史达清 +1 位作者 王苏惠 屠树江 《有机化学》 SCIE CAS CSCD 北大核心 2003年第11期1291-1293,共3页
芳醛、5 ,5 二甲基 1,3 环己二酮 (达米酮 )与对甲基苯胺在以乙二醇为溶剂 ,微波辐射下反应生成一系列新的 3 ,3 ,6,6 四甲基 1,8 二氧代 9 芳基 10 对甲基苯基 1,2 ,3 ,4,5 ,6,7,8,9,10 十氢吖啶 ,产物的结构通过单晶X射线衍... 芳醛、5 ,5 二甲基 1,3 环己二酮 (达米酮 )与对甲基苯胺在以乙二醇为溶剂 ,微波辐射下反应生成一系列新的 3 ,3 ,6,6 四甲基 1,8 二氧代 9 芳基 10 对甲基苯基 1,2 ,3 ,4,5 ,6,7,8,9,10 十氢吖啶 ,产物的结构通过单晶X射线衍射分析确证 . 展开更多
关键词 微波辐射 9-芳基-10-对甲苯基多氢吖啶衍生物 合成 十氢吖啶 心率失调 药物
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Fluorescence enhancement of acridine orange in a water solution by Au nanoparticles 被引量:6
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作者 ZHENG HaiRong XU LiangMin +3 位作者 ZHANG ZhengLong DONG Jun CHEN ShuTang ZHANG XiaoLing 《Science China(Physics,Mechanics & Astronomy)》 SCIE EI CAS 2010年第10期1799-1804,共6页
The surface enhanced fluorescence effect of acridine orange fluorophore in the proximity of Au nanoparticles has been investigated experimentally in the system of aqueous solution.Significant enhancement of the fluore... The surface enhanced fluorescence effect of acridine orange fluorophore in the proximity of Au nanoparticles has been investigated experimentally in the system of aqueous solution.Significant enhancement of the fluorescence intensity was observed when the system was excited with 532 nm or 442 nm CW lasers.The influence of the distances between neighboring Au particles as well as that between the fluorophore molecules and the Au surface were explored experimentally.The results demonstrated that a compact distribution of metallic particles was able to produce stronger fluorescence enhancement.Proper separation between the fluorophore molecules and the metal surface was favorable for a better enhancement. 展开更多
关键词 surface enhanced fluorescence local field enhancement acridine orange hydrophilic Au nanoparticle
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潜在的抗肿瘤试剂二吖啶胺衍生物的合成新方法 被引量:5
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作者 朱燕舞 赵广超 周运友 《合成化学》 CAS CSCD 2002年第1期65-67,共3页
优化了 3种潜在的抗肿瘤试剂 9,9 -乙二胺二吖啶、9,9 -丙二胺二吖啶和 9,9 -三乙烯四胺二吖啶的合成方法。该法具有产率高、条件温和。
关键词 抗肿瘤试剂 合成 二吖啶胺衍生物 9 9′→乙二胺二吖啶 9 9′-丙二胺二吖啶 9 9′→三乙烯四胺二吖啶
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Covalent functionalization of graphene oxide by 9-(4-aminophenyl)acridine and its derivatives 被引量:5
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作者 Yi Si Feng Jing Jing Ma +4 位作者 Xin Yan Lin Jia Song Zhang Peng Lv Hua Jian Xu Lin Bao Luo 《Chinese Chemical Letters》 SCIE CAS CSCD 2012年第12期1411-1414,共4页
Graphene/acridine (G-Acr) hybrid structures were synthesized through covalent functionalization of graphene oxide with 9-(4- aminophenyl)acridine (APA) and its derivatives. The G-Act hybrids were characterized b... Graphene/acridine (G-Acr) hybrid structures were synthesized through covalent functionalization of graphene oxide with 9-(4- aminophenyl)acridine (APA) and its derivatives. The G-Act hybrids were characterized by Fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometry, thermal gravimetric analysis and Raman spectroscopy. X-ray photoelectron spectroscopy confirms that the binding energies of APA and its derivatives shifted to higher values, revealing pronounced charge transfer at the interface of graphene and organic molecules. 展开更多
关键词 Graphene oxide Covalent functionalization Hybrid material acridine derivative
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Novel synthetic 9-benzyloxyacridine analogue as both tyrosine kinase and topoisomerase I inhibitor 被引量:5
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作者 Xu-Liang Lang Qin-Sheng Sun +5 位作者 Yu-Zong Chen Lu-Lu Li Chun-Yan Tan Hong-Xia Liu Chun-Mei Gao Yu-Yang Jiang 《Chinese Chemical Letters》 SCIE CAS CSCD 2013年第8期677-680,共4页
Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of cancers.Discovery of new multi-target scaffolds are important for developing such agents. A series ... Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of cancers.Discovery of new multi-target scaffolds are important for developing such agents. A series of five novel acridine analogues,LXL 1-5,were synthesized and their antiproliferative activity against HepC-2 cell lines were evaluated,among which the 9-benzyloxyacridine analogue,LXL-5, showed inhibitory activity against tyrosine kinases,VEGFR-2 and Src.The results of UV-visible absorption spectra and fluorescence emission spectra,as well as DNA topoisomerase I inhibition assay, indicated topoisomerase I inhibitory activity.Our study suggested that acridine scaffold,previously shown to have no multi-target kinase and topoisomerase inhibitory activity,might be potentially developed as a multi-target inhibitor of tyrosine kinases and topoisomerase I. 展开更多
关键词 acridine Topoisomerases Tyrosine kinases Antitumor DNA-binding
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微波辐射下4-(4-羟基-3-甲氧基)苯基-3,3,6,6-四甲基-1,8-二氧代1,2,3,4,5,6,7,8,9,10-十氢吖啶的合成和晶体结构 被引量:2
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作者 屠树江 缪春宝 +4 位作者 于晨侠 姚昌盛 刘芳 高原 吴德公 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2002年第3期313-316,共4页
标题化合物C24H29NO4?1/2C2H5OH稨2O)由香兰素、5,5-二甲基-1,3-环己二酮、醋酸铵在微波辐射下干反应并经95%乙醇重结晶而得C24H29NO4穀2(C2H5OH稨2O)晶体。结构通过单晶X-射线衍射法确定,其晶体属单斜晶系,空间群P21/n, a = 9.810(2), ... 标题化合物C24H29NO4?1/2C2H5OH稨2O)由香兰素、5,5-二甲基-1,3-环己二酮、醋酸铵在微波辐射下干反应并经95%乙醇重结晶而得C24H29NO4穀2(C2H5OH稨2O)晶体。结构通过单晶X-射线衍射法确定,其晶体属单斜晶系,空间群P21/n, a = 9.810(2), b = 14.516(3), c = 17.008(3) ? b = 101.03(2), V = 2377.2(8) ?, Z = 4, Mr = 427.52, Dc = 1.195 g/cm3 , m(MoKa) = 0.082 mm-1, F(000) = 920。晶体结构用直接法解出,经全矩阵最小二乘法对原子参数进行修正,最终的偏离因子为R = 0.0406, wR = 0.0892。X-射线衍射分析结果表明,吡啶环和与之稠合的2个六员环均为信封式构象。 展开更多
关键词 微波辐射 吖啶 晶体结构 X射线衍射
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人附红细胞体感染实验诊断方法的建立 被引量:7
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作者 王剑飚 樊绮诗 +2 位作者 倪麟 倪培华 姚玉峰 《检验医学》 CAS 北大核心 2011年第11期784-790,共7页
目的比较瑞氏-吉姆萨染色、吖啶橙荧光染色以及聚合酶链反应(PCR)对人附红细胞体的检出率,探索最可靠的检测人附红细胞体病的方法。方法选取体检健康人50名,同时从白血病及肾移植患者中分别选取50例,使用瑞氏-吉姆萨染色法以及吖啶橙荧... 目的比较瑞氏-吉姆萨染色、吖啶橙荧光染色以及聚合酶链反应(PCR)对人附红细胞体的检出率,探索最可靠的检测人附红细胞体病的方法。方法选取体检健康人50名,同时从白血病及肾移植患者中分别选取50例,使用瑞氏-吉姆萨染色法以及吖啶橙荧光染色法检测附红体的感染率,同时选取1例2种方法检测结果均为强阳性的标本,根据GenBank中已收录的猪、牛、羊、猫、鼠等5种附红细胞体的16S rRNA基因序列设计一对特异性引物,初步建立人附红体病的分子诊断方法。结果体检健康人群中瑞氏-吉姆萨染色法以及吖啶橙荧光染色法检出率分别为32%和24%,白血病组的检出率分别为94%和62%,肾移植组的检出率分别为88%和68%,同时初步建立了人附红细胞体病的分子诊断方法,但需进一步研究将其完善。结论吖啶橙荧光染色法最适合临床作为人附红细胞体病的临床检测方法。 展开更多
关键词 附红细胞体 瑞氏-吉姆萨染色 吖啶橙 PCR 16S RRNA
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Fast hydrogenation kinetics of acridine as a candidate of liquid organic hydrogen carrier family with high capacity 被引量:4
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作者 Ming Yang Xile Xing +3 位作者 Ting Zhu Xuedi Chen Yuan Dong Hansong Cheng 《Journal of Energy Chemistry》 SCIE EI CAS CSCD 2020年第2期115-119,共5页
Hydrogen has been deemed as one of the most efficient energy carriers for a broad variety of industrial applications[1,2].Large-scale,low-cost hydrogen production,safe storage and delivery represent a tremendous techn... Hydrogen has been deemed as one of the most efficient energy carriers for a broad variety of industrial applications[1,2].Large-scale,low-cost hydrogen production,safe storage and delivery represent a tremendous technological challenge and have become a subject of intense research and development activities in the past few decades[3–5]. 展开更多
关键词 acridine Catalytic HYDROGENATION Liquid ORGANIC HYDROGEN CARRIER High capacity KINETICS
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等色吸收荧光猝灭法快速测定食品中苏丹红Ⅰ 被引量:5
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作者 刘保生 王云科 +1 位作者 曹冬林 傅丽 《分析试验室》 CAS CSCD 北大核心 2007年第8期87-90,共4页
在乙醇介质中,强荧光染料吖啶的荧光波长478 nm与苏丹红Ⅰ的吸收光波长480 nm十分接近,由于等色性苏丹红Ⅰ能够有效吸收吖啶发出的荧光,使吖啶在激发波长λex=410 nm、荧光波长λem=478 nm处荧光猝灭,依此建立了荧光猝灭测定苏丹红... 在乙醇介质中,强荧光染料吖啶的荧光波长478 nm与苏丹红Ⅰ的吸收光波长480 nm十分接近,由于等色性苏丹红Ⅰ能够有效吸收吖啶发出的荧光,使吖啶在激发波长λex=410 nm、荧光波长λem=478 nm处荧光猝灭,依此建立了荧光猝灭测定苏丹红Ⅰ的新方法。该方法快速、简便,其线性范围为3.72-37.2 mg/L,方法检出限为1.1 mg/L。用于辣椒、辣椒酱食品中痕量苏丹红Ⅰ的测定。6次平行测定,相对标准偏差为0.8%-2.7%,加标回收率为89.5%-104.0%。 展开更多
关键词 荧光猝灭 苏丹红Ⅰ 吖啶
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吖啶-多胺类缀合物的合成、抗肿瘤活性及与 DNA 键合作用 被引量:6
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作者 李小六 马东来 +5 位作者 杨海龙 谭官海 杜会茹 王克让 张平竹 陈华 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2014年第6期1181-1188,共8页
设计合成了系列吖啶-多胺类衍生物(ACP1~ ACP6),并通过四甲基偶氮唑蓝(MTT)染色法研究了化合物对 K562(人白血病细胞)、 A549(人肺癌细胞)和 Hela(人宫颈癌细胞)细胞株的体外抗肿瘤活性。结果显示,化合物对肿瘤细胞具有一... 设计合成了系列吖啶-多胺类衍生物(ACP1~ ACP6),并通过四甲基偶氮唑蓝(MTT)染色法研究了化合物对 K562(人白血病细胞)、 A549(人肺癌细胞)和 Hela(人宫颈癌细胞)细胞株的体外抗肿瘤活性。结果显示,化合物对肿瘤细胞具有一定的抑制作用,尤其是化合物 ACP2的抗肿瘤活性优于阳性对照顺铂。通过 UV-Vis 光谱、荧光光谱、圆二色谱和热变性实验研究了合成化合物与小牛胸腺 DNA(Ct-DNA)的键合作用。结果表明,三乙烯四胺修饰的化合物 ACP2具有较好的抗肿瘤活性,与 DNA 分子具有较强的结合能力。 展开更多
关键词 吖啶 多胺 缀合物 DNA键合 抗肿瘤活性
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用于H_(2)PO_(4)^(-)检测的比率型荧光探针合成及性能研究
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作者 郭昌晟 陈君霞 +3 位作者 刘忆茹 卢钰盛 董智云 席福贵 《化学试剂》 CAS 2024年第6期33-38,共6页
设计合成了一种基于吖啶-苯并咪唑鎓的大环受体ABIM,可作为H_(2)PO_(4)^(-)的荧光比率传感器。借助荧光光谱研究了受体ABIM对H_(2)PO_(4)^(-)的选择性识别,在大环受体ABIM的乙腈溶液中加入H_(2)PO_(4)^(-)后,在426 nm处荧光发射明显“... 设计合成了一种基于吖啶-苯并咪唑鎓的大环受体ABIM,可作为H_(2)PO_(4)^(-)的荧光比率传感器。借助荧光光谱研究了受体ABIM对H_(2)PO_(4)^(-)的选择性识别,在大环受体ABIM的乙腈溶液中加入H_(2)PO_(4)^(-)后,在426 nm处荧光发射明显“关闭”,506 nm处荧光发射明显“打开”,溶液荧光颜色由蓝色变为蓝绿色,新的荧光发射峰可能是由于H_(2)PO_(4)^(-)诱导两个受体中的吖啶环之间形成Excimer产生的。ABIM与H_(2)PO_(4)^(-)以1∶1的化学计量比结合,结合常数为(7.13±0.48)×10^(6)L/mol,检出限为2.38×10-7 mol/L,最佳响应时间为2 min。回收实验表明,ABIM可应用于样品中H_(2)PO_(4)^(-)的检测。 展开更多
关键词 吖啶 苯并咪唑鎓 H 2PO-4 大环 比率型荧光探针
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Correlation Analysis of the Results of Double Fluorescence(AO/PI) Staining and Clinical Outcomes 被引量:2
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作者 Yu-bao WANG Lei-wen ZHAO +3 位作者 Zu-qiong XIANG Xiu-zhuang ZHOU You-lun GUI Chang-hai HE 《Journal of Reproduction and Contraception》 CAS 2012年第2期111-118,共8页
Objective To estimate the predictive value of double fluorescence [acridine orange (AO)/propidium iodide (PI)] staining results for fertilization rate and clinical outcomes and analyze the correlation between th... Objective To estimate the predictive value of double fluorescence [acridine orange (AO)/propidium iodide (PI)] staining results for fertilization rate and clinical outcomes and analyze the correlation between the results of AO/P1 staining and sperm apoptosis. Methods A prospective study was carried out, 235 infertile couples remedied using traditional in vitro fertilization (IVF) were included. Semen collected from 235 patients were stained by fluorescence dye, AO and PL at the same time the spermatozoa apoptosis rate was calculated by using flow cytometry to detect the rate of Annexin V+/ PI- . The result of fluorescence was divided into 3 groups as green (G), yellow (Y) and red (R) according to the color of fluorescence. The correlation between the percent of the 3 colors and clinical outcomes and spermatozoa apoptosis rate was evaluated. Results Significant negative correlation was observed between the percentage of Y and fertilization rate (r= -0.42, P=0.04), no significant correlation was observed between the percentage of G, R and fertilization rate. The percentage of G, Y, R was not significantly different between pregnant patients and non-pregnant patients, respectiw,ly, while the percentage of Y was significant different between miscarriage patients and liveborn patients (r=0.6L P=0.01) and no significant difference exist in the percentage of G and R between liveborn patients and miscarriage patients. There was a significant positive correlation between the percentage of Y and the rate of Annexin V+/ PI (r=0.53, P=0.04), and no significant correlation was shown between the percentage of G, R and the rate of Annexin V+/ PI-.Conclusion The percentage of yellow group of double fluorescence (AO/PI) staining will affect the fertilization rate and the miscarriage rate, and this group of spermatozoa may be connected with the spermatozoa apoptosis. 展开更多
关键词 acridine orange (AO) propidium iodide (PI) SPERMATOZOA in vitro fertilization (1VF)
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荧光光谱滴定法研究对磺酸基杯[4]芳烃对吖啶的包结作用 被引量:2
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作者 周运友 卢琴 +3 位作者 刘春 佘世科 杨续来 王伦 《光谱学与光谱分析》 SCIE EI CAS CSCD 北大核心 2006年第9期1627-1630,共4页
合成了对磺酸基杯[4]芳烃(1),并用荧光光谱滴定法研究了不同温度下(1)在柠檬酸缓冲溶液(pH=5.92,0.1mol.L-1)中对吖啶的包结行为。在一定的浓度范围内,当加入(1)后,吖啶的荧光峰有红移,且荧光强度随着所加的(1)浓度的增大而发生猝灭。... 合成了对磺酸基杯[4]芳烃(1),并用荧光光谱滴定法研究了不同温度下(1)在柠檬酸缓冲溶液(pH=5.92,0.1mol.L-1)中对吖啶的包结行为。在一定的浓度范围内,当加入(1)后,吖啶的荧光峰有红移,且荧光强度随着所加的(1)浓度的增大而发生猝灭。结果显示二者形成了1∶1的稳定包合物。计算了在15.0,20.0,25.0及30.0℃下的包结稳定常数,它们依次为3.08×105,4.45×104,2.58×104和8.90×103,并计算了热力学参数ΔG,ΔH和ΔS。结果说明反应是放热的且是焓变驱动的。其包结机理可能为吖啶部分进入了对磺酸基杯[4]芳烃的空腔中,且吖啶稠环的质子化的N原子与(1)的一个SO3-基团之间以较强的静电作用成键;在此强静电作用的驱动下以及较弱的范德瓦耳斯力、疏水作用的辅助下主客体形成了1∶1的配合物。 展开更多
关键词 芳烃 吖啶 荧光光谱滴定 包结稳定常数 静电作用
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对苯二甲醛或间苯二甲醛与5,5-二甲基-1,3-环己二酮的反应:含有双4(H)-吡喃、1,4-二氢吡啶结构单元的杂环化合物的合成 被引量:4
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作者 冯友健 章晓镜 +2 位作者 缪春宝 蒋虹 屠树江 《有机化学》 SCIE CAS CSCD 北大核心 2004年第8期950-952,共3页
用对苯二甲醛或间苯二甲醛与 5 ,5 二甲基 1,3 环己二酮反应 ,在不同条件下得到了含有双 4(H) 吡喃、1,4 二氢吡啶结构单元的双 氧杂蒽衍生物、双 吖啶衍生物、以及双 N
关键词 对苯二甲醛 间苯二甲醛 5 5-二甲基-1 3-环己二酮 双4(H)-吡喃 1 4-二氢吡啶 杂环化合物 合成
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吖啶作为检测试剂的磷霉素间接光度反相高效液相色谱研究 被引量:4
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作者 胡玉玲 达世禄 +1 位作者 冯钰 张庆合 《色谱》 CAS CSCD 北大核心 1999年第3期271-274,共4页
以吖啶为紫外检测试剂,研究了强极性弱紫外吸收磷霉素的间接光度色谱,探讨了检测试剂性质、浓度、pH值等因素对色谱保留和检测灵敏度的影响,提出一种测定磷霉素的新色谱方法。
关键词 间接光度检测 HPLC 吖淀 磷霉素 测定
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Subcellular chemical imaging of structurally similar acridine drugs by near-field laser desorption/laser postionization mass spectrometry 被引量:4
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作者 Xiaoling Cheng Zhibin Yin +1 位作者 Liu Rong Wei Hang 《Nano Research》 SCIE EI CAS CSCD 2020年第3期745-751,共7页
Insights into the pharmacologic effect on cellular processes and the potential toxicological effects are vital to new drug development and evaluation,yet research on these subjects remains a great challenge due to the... Insights into the pharmacologic effect on cellular processes and the potential toxicological effects are vital to new drug development and evaluation,yet research on these subjects remains a great challenge due to the lack of information regarding the spatiotemporal distribution of drugs and metabolites within a single cell.Mass spectrometry imaging(MSI)has proven to be a label-free and high-throughput approach for visualizing drug distribution in spatial and temporal domains.However,single-cell drug imaging has been limited so far by detection sensitivity and microscale lateral resolution.Herein,we report near-field laser desorption/laser postionization mass spectrometry(NDPI-MS)for single-cell imaging of two structurally similar drugs,proflavine and ethacridine,and subcellular distributions of proflavine at different drug concentrations were investigated.The NDPI-MS imaging results indicate that proflavine was accumulated in lysosomes,which was verified by laser scanning confocal microscopy(LSCM).Additionally,a distinguished subcellular distribution pattern of ethacridine from proflavine could be visualized,highlighting the complexity of the interaction between the drugs and biological environment even though these two drugs possess similar structures.Taken together,the present results demonstrate the great potential of the integrated single-cell MSI platform for characterizing the drug distribution and its phenotype changes within individual cells,expediting the identification and evaluation of newly developed drugs. 展开更多
关键词 NEAR-FIELD mass spectrometry acridine drugs single cell imaging laser postionization
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9-氨基-1,2,3,4-四氢吖啶衍生物的合成 被引量:3
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作者 李加荣 韩方斌 +2 位作者 张广 李文婷 马淑玲 《北京理工大学学报》 EI CAS CSCD 北大核心 2005年第2期169-171,共3页
为了降低第一个用于治疗老年痴呆症药物他克林的毒副作用 ,提高其药理活性 ,对其侧链氨基进行了改性研究 .分别对他克林进行了乙酰化、丁酰化及氯乙酰化反应 ,制备了相应的衍生物 .鉴于哌嗪基团的亲水性 ,将其引入吖啶分子中 ,合成出化... 为了降低第一个用于治疗老年痴呆症药物他克林的毒副作用 ,提高其药理活性 ,对其侧链氨基进行了改性研究 .分别对他克林进行了乙酰化、丁酰化及氯乙酰化反应 ,制备了相应的衍生物 .鉴于哌嗪基团的亲水性 ,将其引入吖啶分子中 ,合成出化合物 9- (2 -哌嗪乙酰氨基 ) - 1,2 ,3,4 -四氢吖啶 .所有化合物的结构均经元素分析、红外光谱。 展开更多
关键词 老年性痴呆症 吖啶 他克林衍生物 合成
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Novel synthetic acridine-based derivatives as topoisomerase Ⅰ inhibitors 被引量:1
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作者 Bin Li Chun-Mei Gao +4 位作者 Qin-Sheng Sun Lu-Lu Li Chun-Yan Tan Hong-Xia Liu Yu-Yang Jiang 《Chinese Chemical Letters》 SCIE CAS CSCD 2014年第7期1021-1024,共4页
Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and He... Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV-vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization. 展开更多
关键词 acridine DNA binding agent TOPOISOMERASE ANTICANCER
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