共查询到20条相似文献,搜索用时 109 毫秒
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弥拜霉素类似物的合成、表征和杀虫活性研究 总被引:1,自引:0,他引:1
以弥拜霉素类似物依维菌素为原料,根据类同合成法和亚结构连接法原理,对依维菌素进行脱糖,再与相应的酰氯进行酯化、肟化反应制得两个系列弥拜霉素类似物化合物4Ia~5IId,所有目标化合物都通过核磁共振氢谱、高分辨质谱的确认,并分别对朱砂叶螨(Tetranychus cinnabarinus)、南方粘虫(Mythimna sepatara)和蚕豆蚜(Aphis fabae)进行室内杀虫活性测定,结果表明所有衍生物均表现出不同程度的杀虫活性,其中化合物4IIa和4IIb对粘虫和蚜虫表现出很高的杀虫活性. 相似文献
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新型含氟姜黄素类似物的合成、晶体结构及抗肿瘤活性 总被引:7,自引:0,他引:7
采用活性基团拼接法将含氟苯甲醛与酮反应, 合成了5个含氟单羰基姜黄素类似物, 结构经IR, 1H NMR及ESI-MS确认. 对所合成的化合物进行了抗肿瘤活性测试(MTT法), 结果表明, 部分化合物对肿瘤细胞有较强的选择性抑制活性, 其中2,6-二(4-氟亚苯基)环己酮(3a)和2,6-二(2-氟亚苯基)环己酮(3b)的抗肿瘤谱广, 活性较好, 就此对化合物3b作了单晶培养, 并就晶体结构进行了X衍射分析. 结构表明化合物3b属三斜晶系, 空间群 P-1. 晶胞参数 a=0.9222(2) nm, b=0.9732(2) nm, c=1.0127(2) nm, α=88.920(4)°, β=75.672(3)°, γ=62.404(3)°, V=0.7755(3) nm3, Z=2, Dc=1.329 Mg•m-3, μ=0.097 mm-1, F(000)=324, 最终偏离因子R=0.0590, wR=0.1841. 相似文献
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通过简单的溶剂扩散法,在合成E环开环衍生物的配合物的过程中,得到了一个新型喜树碱非内酯环类似物2,并通过元素分析、IR、X-射线单晶衍射对其进行了结构表征。结果表明,化合物2(C19H18N2O4)属于单斜晶系Cc,a=2.2432(5),b=9.7320(19),c=7.4280(15),β=97.95(3)°,Z=2,V=1606.0(6)3,Mr=338.35,F(000)=712,R=0.0456,wR=0.1090。结构分析表明,化合物2的每个分子由1个喜树碱类似物分子和1个水分子组成,2个喜树碱类似物分子通过短程相互作用形成柱状堆积,相邻的柱状堆积通过与水分子之间的氢键作用形成二维网络结构。 相似文献
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以微管菌素为先导化合物, 设计合成了一系列类似物; 所有化合物的结构均经1H NMR, 13C NMR及HRMS确证, 均为新化合物. 采用噻唑蓝(MTT)法对其抗肿瘤活性进行了初步筛选, 结果表明, 化合物Ⅱb具有一定的抗肿瘤活性. 相似文献
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A cyclic analogue 4 of galardin, a known MMP inhibitor, is designed to improve its selectivity. The synthesis of 4 starts from dimethyl (S)‐malate using diaselective alkylation and subsequent cyclization and amide formation as key steps. The compound 4 showed MMP inhibitory activity on all MMPs tested with IC30, ranging from 20.1 μM to 104 μM. 相似文献
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Qinghua Zhang Dr. Shimin Liu Zuopeng Li Jian Li Zhengjian Chen Ruifeng Wang Liujin Lu Youquan Deng Prof. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2009,15(3):765-778
A new series of ionic liquids composed of three cyclic sulfonium cations and four anions has been synthesized and characterized. Their physicochemical properties, including their spectroscopic characteristics, ion cluster behavior, surface properties, phase transitions, thermal stability, density, viscosity, refractive index, tribological properties, ion conductivity, and electrochemical window have been comprehensively studied. Eight of these salts are liquids at room temperature, at which some salts based on [NO3]? and [NTf2]? ions exhibit organic plastic crystal behaviors, and all the saccharin‐based salts display relatively high refractive indices (1.442–1.594). In addition, some ionic liquids with the [NTf2]? ion exhibit peculiar spectroscopic characteristics in FTIR and UV/Vis regions, whilst those salts based on the [DCA]? ion show lower viscosities (34.2–62.6 mPa s at 20 °C) and much higher conductivities (7.6–17.6 mS cm?1 at 20 °C) than most traditional 1,3‐dialkylimidazolium salts. 相似文献
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通过溶液聚合制备了一种新型不饱和聚磷酸酯(Polymer Ⅰ), 经季铵化得到了侧基含季铵基的不饱和聚磷酸酯(PolymerⅡ). 对聚合物的结构和热性能进行了表征. 研究了PolymerⅡ与聚丁二酸丁二醇酯(PBS)的共混片基(Polymer Ⅱ的质量分数分别为5%, 10%和20%)在pH=7.4的磷酸缓冲溶液中的溶胀和降解性能. 结果表明, 以纯三甲胺为季铵化试剂, 在V(氯仿): V(异丙醇): V(DMF)=3: 5: 5的混合溶剂中, 于60℃反应24 h可得到季铵化率高达48%的PolymerⅡ. 在PBS中PolymerⅡ的含量越多, 达到溶胀平衡时, 共混片基的溶胀率越高, 越容易降解. 磷酸酯的引入使聚合物的熔点(Tm)和热稳定性(Td)降低. 相似文献
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Zao Ying LI* Yue Ning ZHANG Zhen Ting GAO Yi LIU Xun Jin ZHU Department of Chemistry Wuhan University Wuhan 《中国化学快报》2001,(12)
Water-soluble metal porphyrins can sensitize photocatalytic water reduction1, oxidation2, and are of potential use in photogalvanic cells3. In recent years, porphyrins have been used as photosensitizer for the photodynamic therapy (PDT) of cancers. To constitute a good PDT photosensitizer, a compound must be soluble in the bodys tissue fluids so that it can be injected and carried around the body to the tumour site4. Research on the anti-tumor activity of metalloporphyrins has also been r… 相似文献
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以酮和硝基甲烷为原料,经3步反应合成了2种氮取代的二氮杂双环结构化合物N-二氯乙酰基-9-氧代-1,5-二氮杂二环[4.3.0]壬烷,采用红外光谱、核磁共振和元素分析对产物结构进行了表征。并利用土培法对化合物进行了初步的生物活性试验。结果表明,化合物能够减轻普施特对玉米的伤害。 相似文献
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XU Liang-zhong XU Zhong-jie ZHANG Gong-sheng ZHOU Kai ZHAI Zhi-wei College of Chemistry Molecule Engineering Qingdao University of Science Technology Qingdao P. R. China 《高等学校化学研究》2008,24(5):575-578
With dimethomorph and flumorph as the leading compounds, four novel acrylamide compounds with two types of structure were designed and synthesized by means of the method of "me too chemistry". The target compounds were characterized by 1H NMR, IR, MS, and elemental analysis. The influences of solvent and raw material on the yield were investigated and optimum processing conditions were determined. The results of preliminary biological tests show that all those compounds exhibit certain antifungal activities. 相似文献
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以丁炔二醇为起始原料,用叔丁基二甲基氯硅烷进行单保护后,与2-(6-羟基-2,3-二氢苯并呋喃)乙酸甲酯经Mitsunobu反应制得2-{6-[4-(叔丁基二甲硅烷氧基)丁-2炔基氧基]-2,3-二氢苯并呋喃}乙酸甲酯(3); 3脱除保护后与苯酚衍生物发生Mitsunobu反应,随后经水解合成了6个结构新颖的苯并二氢呋喃衍生物(7a~7f),其结构经1H NMR, 13C NMR和HR-EI-MS表征。GPR40激动活性测试结果表明:7a~7f对GPR40均有激动作用,其中7e和7f激动活性最强,EC50分别为0.593 μmol·L-1和0.596 μmol·L-1。 相似文献
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以含取代基团的苯酚和氯代环氧丙烷为原料,经多步反应合成了4种含芳香结构的化学修饰单体,针对靶向Mdm2 mRNA序列的siRNA,在其3'末端加入不同化学修饰的单体制备获得9个siRNAs.采用四甲基偶氮唑盐(MTT)法对所合成的siRNAs进行体外抗肿瘤活性、稳定性测试,结果显示化学修饰的siRNA8,siRNA11,siRNA15对人乳腺癌MCF-7细胞的活性和核酸酶稳定性均有显著提高,其中siRNA11体外对RNA水解酶的半衰期提高了10倍. 相似文献