共查询到14条相似文献,搜索用时 0 毫秒
1.
Aruna Chhikara Praveen K. Roayapalley Hiroshi Sakagami Shigeru Amano Keitaro Satoh Yoshihiro Uesawa Umashankar Das Swagatika Das Edgar A. Borrego Cristina D. Guerena Clare R. Hernandez Renato J. Aguilera Jonathan R. Dimmock 《Molecules (Basel, Switzerland)》2022,27(19)
Two series of novel unsymmetrical 3,5-bis(benzylidene)-4 piperidones 2a–f and 3a–e were designed as candidate antineoplastic agents. These compounds display potent cytotoxicity towards two colon cancers, as well as several oral squamous cell carcinomas. These compounds are less toxic to various non-malignant cells giving rise to large selectivity index (SI) figures. Many of the compounds are also cytotoxic towards CEM lymphoma and HL-60 leukemia cells. Representative compounds induced apoptotic cell death characterized by caspase-3 activation and subG1 accumulation in some OSCC cells, as well as the depolarization of the mitochondrial membrane potential in CEM cells. A further line of inquiry was directed to finding if the SI values are correlated with the atomic charges on the olefinic carbon atoms. The potential of these compounds as antineoplastic agents was enhanced by an ADME (absorption, distribution, metabolism, and excretion) evaluation of five lead molecules, which revealed no violations. 相似文献
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Russian Journal of General Chemistry - Erratum 相似文献
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以4-羟基香豆素为原料,经氯化、醚化和异硫氰酸化3步反应制得中间体——4-(4-异硫氰酸酯苯氧基)香豆素(3);3与取代芳香胺经加成反应合成了9个新型的1-(4-取代苯基)-3-[4-(4-氧香豆素基)苯基]硫脲衍生物(4a~4i),其结构经1H NMR,13C NMR,IR和MS(ESI)表征。采用浑浊度法测试了4的抑菌活性。结果表明:4a、4b、4e和4f抑制烟草青枯菌活性EC50值分别为112.02、121.39、88.72和86.90μg·mL~(-1),优于噻菌铜(130.25μg·mL~(-1));4a、4b、4e和4f抑制番茄青枯菌活性EC50值分别为107.89、110.69、82.43和82.48μg·mL~(-1),优于噻菌铜(123.94μg·mL~(-1))。 相似文献
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Sheena Varghese 《Supramolecular chemistry》2016,28(3-4):293-304
This paper describes the synthesis of carbon nanoparticle (CNP) from natural sources such as kitchen soot, synthesis of a chromophoric system {5-[4-(dimethylamino) benzylidene]-4-oxo-2-thioxo1, 3-thiazolidin-3-yl} acetic acid and its incorporation into β-cyclodextrin (β-CD) through the esterification of the hydroxyl group with the free carboxyl function of the chromophoric system by DCC coupling. Encapsulation of CNP into functionally modified β-CD system was achieved. Characterisation of the products was undertaken by UV–visible, FT-IR, NMR, fluorescence spectroscopic methods, SEM, TEM and X-ray diffraction methods. Their antibacterial activities were addressed. The antibacterial activity of CNP and functionally modified β-CD-CNP products were tested against various pathogenic bacterial strains such as Streptcoccus haemoliticus (+ve), Staphylococcus aureus (+ve), Klebsiella pneumonia (?ve) and E. coli (MTCC1687) (?ve) by disc diffusion method. The results showed that the CNPs and functionally modified products have good antibacterial activity against selected pathogenic bacterial strains. 相似文献
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Skrypska O. V. Lytvyn R. Z. Rusnak O. V. Melnyk D. O. Pitkovych Kh. Ye. Yagodinets P. I. Obushak M. D. 《Russian Journal of General Chemistry》2020,90(4):602-609
Russian Journal of General Chemistry - 4-[4-(2-Bromoacetyl)phenyl]-3-hydroxy-2H-chromen-2-one reacted with pyridine and 4-methylpyridine to give the corresponding quaternary pyridinium salts. The... 相似文献
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以2-甲基苯甲酰甲酸甲酯为起始原料, 通过与甲氧基胺的盐酸盐、甲胺、N-溴代丁二酰亚胺(NBS)和1H-1,2,4-三氮唑钠反应合成了两个系列共计22个2-{2-[3-(取代苯基)-3-氧代-2-1,2,4-三唑-1-基-丙基]-苯基}-2-甲氧亚氨基乙酸甲酯和乙酰甲胺类的衍生物. 经IR, 1H NMR和MS对目标化合物进行了结构表征. 用浓度为 10 µg8226;mL-1的目标化合物进行了初步离体杀菌活性试验, 结果表明: Ha4, Ha5, Ha7对油菜菌核病有杀菌活性; Ha2, Hb8对小麦纹枯病有杀菌活性; Hb4对蔬菜灰霉病有杀菌活性; Hb4, Hb5对小麦赤霉病和小麦纹枯病均有杀菌活性. 相似文献
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1-脱氢松香酰基-3-取代硫脲以及5-(脱羧脱氢松香-4-基)-3-芳氨基- 1H-1,2,4-三唑化合物的合成与生物活性 总被引:2,自引:0,他引:2
以广西的优势资源松香为原料, 脱氢松香酸与亚硫酰氯、硫氰化钾分别在回流条件下反应6 h和1.5 h, 得到脱氢松香酰异硫氰酸酯, 产率52%; 然后与胺在加热回流条件下反应1.5 h, 得到11种1-脱氢松香酰基-3-取代硫脲4, 产率63%~94%; 4a~4f 分别与水合肼在搅拌下回流反应3~6 h, 得到6种5-(脱羧脱氢松香-4-基)-3-芳氨基-1H-1,2,4-三唑化合物5, 产率70%~94%; 所有化合物的结构均经IR, 1H NMR, 13C NMR和元素分析确认. 初步生物活性测试表明, 4e, 4f, 4j, 5b对枯草杆菌抑菌率较高, 特别是4j在浓度为50 mg/L时就达到较好效果; 4b, 4h, 4i, 5e在100 mg/L时对大肠杆菌的抑菌效果较好. 相似文献
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O. V. Yelenich R. Z. Lytvyn O. V. Skrypska Kh. Ye. Pitkovych A. D. Kachkovskii M. D. Obushak P. I. Yagodinets 《Russian Journal of General Chemistry》2016,86(8):1838-1844
The reaction of 3-(4-bromoacetylphenyl)-1-methylquinolin-2(1Н)-one with pyridine and 4-methylpyridine has afforded the corresponding pyridinium salts. Condensation of 4-methyl-1-{2-[4-(1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)phenyl]-2-oxoethyl}pyridinium bromide with 4-dimethylaminobenzaldehyde has given a new biscyanine dye, 1-{1-[4-(1,2-dihydro-1-methyl-2-oxo-3-quinolinyl)benzoyl]-2-[4-(dimethylamino)-phenyl]ethynyl}-4-{2-[4-(dimethylamino)phenyl]ethynyl}pyridinium bromide. Its electronic spectrum has been analyzed, and quantum-chemical simulation of spatial and electronic structure of its possible isomers has been performed. 相似文献
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Sakram B. Ravi D. Ashok K. Rambabu S. Sonyanaik B. Kurumanna A. 《Russian Journal of General Chemistry》2018,88(4):780-788
Russian Journal of General Chemistry - The Buchwald–Hartwig amination reaction between 2-chloro-3-aryl-1,8-naphthyridines and 2-(4-aminophenyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione in the... 相似文献
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Pragathi Y. J. Sreenivasulu R. Veronica D. Madhavi S. Raju R. R. 《Russian Journal of General Chemistry》2019,89(5):1009-1014
Russian Journal of General Chemistry - A novel series of benzothiazole bearing 1,2,3-triazole derivatives 11a–11j are synthesized, and their structures are confirmed by 1H and 13C NMR, and... 相似文献
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1 INTRODUCTION Triarylamines constitute a well known class of hole conducting material[1~4]. On the other hand , oxadiazole-based compounds as good electron- transporting materials[5,6] have played an important role in the fabrication of multiple-layer light- emitting diode devices. It is well known that, to achieve good performance in electroluminescence (EL) devices, the injection of electron and hole should be in balance[7]. The requirement might be met in a new compound containing … 相似文献
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N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物的合成及除草活性 总被引:2,自引:0,他引:2
为了寻找高效、安全的除草活性化合物, 合成了12个全新的N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物, 其化学结构经IR, 1H NMR, LC/MS和元素分析确证. 初步生物活性测定结果表明, 该类化合物具有一定的除草活性, 如7a, 7b, 7c, 7g, 7h, 7i, 7k和7l在有效成分75 g/hm2剂量下, 茎叶处理对苘麻(Abutilon theophrasti)、刺苋(Amaranthus spinosus)等阔叶杂草具有良好的除草活性, 其抑制率达100%. 相似文献
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Michael A. Beckett Elliot L. Bennett Michael B. Hursthouse 《Journal of organometallic chemistry》2010,695(7):1080-1083
The salts, [Ph2B{OCH2CH2N(Me)(CH2)n}2][Ph4B3O3] (n = 4, 5), were prepared in moderate yields in MeOH solution from reaction of Ph2BOBPh2 with [N(CH2)n(Me)(CH2CH2OH)][OH] and PhB(OH)2 in a 1:2:4 ratio. The reactions also lead to Ph3B3O3. Both salts were characterized by NMR (1H, 13C, 11B) IR, and single-crystal XRD studies. The salts are comprised of cationic monoborates (zwitterionic, 2N+ and 1B−) and tetraphenylboroxinate anions. 相似文献