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去甲斑蝥素环氧化及溴化衍生物的合成 总被引:1,自引:0,他引:1
去甲斑蝥素环氧化及溴化衍生物的合成方茵,田少雷,赵树纬,殷栋二,廖沈涵(中国医药研究开发中心北京102206)李克庆(南通药品检验所江苏226006)去甲斑蝥素(1)是天然抗癌活性化合物斑螫素(2)的双去甲基类似物,已用于临床治疗早、中期肝癌 ̄[1]... 相似文献
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利用固-液相转移催化法合成了7种α,ω-双[1-(2-甲基-4-硝基咪唑基)]烷烃和20种1-烷基-2-甲基-4-硝基咪唑类化合物,大多数化合物收率在85%以上。初步生物活性试验结果表明,部分化合物具有一定的抗炎、抗菌、镇痛、镇静或抗脑缺氧活性。 相似文献
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建立了2-甲基苯并咪唑类异黄酮衍生物的合成方法. 其中脱氧安息香3以间苯二酚和取代苯乙酸为原料用微波促进法合成, 化合物3再与醋酐反应得到化合物4, 其在酸性条件下转化成化合物5. 化合物5分别与1,2-二溴乙烷和1,3-二溴丙烷在丙酮溶液中回流得到化合物6和7, 最后目标化合物分别由化合物6和化合物7与2-甲基苯并咪唑在无水碳酸钾催化下丙酮中回流得到. 利用IR, 1H NMR, 13C NMR, 元素分析等对目标化合物的结构进行了表征. 在目标化合物的合成中, 不仅对C-O键和C-N键建立的反应条件进行了优化, 而且将微波促进法成功地应用到了目标化合物的合成中, 极大地缩短了反应时间. 目标化合物抗氧化活性研究表明, 12种目标化合物均具有较强的清除羟基自由基的能力. 相似文献
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Iodine as a mild,efficient, and cost-effective catalyst for the synthesis of thiiranes from oxiranes
Jhillu S. Yadav Basi V. Subba Reddy Sandip Sengupta Manoj K. Gupta Gakul Baishya Sukkala J. Harshavardhana Uttam Dash 《Monatshefte für Chemie / Chemical Monthly》2008,139(11):1363-1367
We developed an efficient protocol for the synthesis of thiiranes from oxiranes using a catalytic amount of molecular iodine.
The notable features of this procedure are mild reaction conditions, high conversions, short reaction times, economic viability
of the reagents, compatibility with various functionalities, and simple experimental/product isolation procedures which make
it a useful and attractive process for the synthesis of a range of thiiranes.
Correspondence: Jhillu S. Yadav, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007,
India. 相似文献
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Tran Thu Huong Le Thi Vinh Hoang Thi Khuyen Le Dac Tuyen Nguyen Duc Van Do Thi Thao Ha Thi Phuong 《Molecules (Basel, Switzerland)》2023,28(1)
We present a visual tool and facile method to detect MCF-7 breast cancer cells by using YVO4:Eu3+@silica-NH-GDA-IgG bio-nanocomplexes. To obtain these complexes, YVO4:Eu3+ nanoparticles with a uniform size of 10–25 nm have been prepared firstly by the hydrothermal process, followed by surface functionalization to be bio-compatible and conjugated with cancer cells. The YVO4:Eu3+@silica-NH-GDA-IgG nanoparticles exhibited an enhanced red emission at 618 nm under an excitation wavelength of 355 nm and were strongly coupled with MCF-7 breast cancer cells via biological conjugation. These bio-nanocomplexes showed a superior sensitiveness for MCF-7 cancer cell labelling with a detection percentage as high as 82%, while no HEK-293A healthy cells were probed under the same conditions of in vitro experiments. In addition, the detection percentage of MCF-7 breast cancer cells increased significantly via the functionalization and conjugation of YVO4:Eu3+ nanoparticles. The experimental results demonstrated that the YVO4:Eu3+@silica-NH-GDA-IgG bio-nanocomplexes can be used as a promising labelling agent for biomedical imaging and diagnostics. 相似文献
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Rita Meyer Constance E.J. van Rensburg Helmar Görls 《Journal of organometallic chemistry》2005,690(1):117-125
The titanocene complexes [TiCp2(Cl)R] (1), [TiCp2(Cl)SR] (2), [TiCp2(SR)2] (3) with R = benzothienyl (BT) A and dibenzothienyl (DBT) B, were synthesized and the molecular structures of [TiCp2(Cl)DBT] (1B) and [TiCp2(Cl)SDBT] (2B) confirmed by single crystal X-ray diffraction studies. The dibenzothiophene rings are planar and for 1B in the plane of the titanium and chloro ligand. The chloro ligand is in a trans position to the sulfur atom with respect to the titanium-carbon bond. The complexes were studied for their electronic and structural features and preliminary tests were conducted for their tumor inhibiting properties against HeLa and COLO 320M tumor cell lines. These antitumor activities were compared against those observed for titanocene dichloride (S-01) under similar conditions and the highest antitumor activity was recorded for 2B. 相似文献
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?eljko Petrovski Susana S. Braga Márcia L. Matos Martyn Pillinger Carlos C. Romão 《Journal of organometallic chemistry》2008,693(4):675-684
Seven different ferrocene derivatives have been tested in vitro against Ehrlich ascites tumor cells. Neither ferrocene nor the monosubstituted derivative N,N-dimethylaminomethylferrocene showed cytotoxic activity (IC50 > 1000 μM for 3 h treatments). Better results were obtained with 1,2-disubstituted derivatives. The IC50 values ranged from 376.6 μM for 1,2-diformylferrocene to 71.2 μM for racemic 2-(N,N-dimethylaminomethyl)ferrocenecarboxamide. The latter derivative was also encapsulated in native β-cyclodextrin (CD), heptakis-2,3,6-tri-O-methyl-β-CD (TRIMEB) and 2-hydroxypropyl-β-CD (HPβCD) to give 1:1 (host:guest) inclusion compounds. The existence of true inclusion complexes in the solid state was confirmed by a combination of powder X-ray diffraction, thermogravimetric analysis, FTIR and 13C CP MAS NMR spectroscopy. The IC50 value for the β-CD inclusion compound was identical to that obtained for the nonincluded ferrocene derivative. By contrast, the inclusion compounds comprising TRIMEB and HPβCD yielded IC50 values of 25.2 and 20.0 μM, respectively. No obvious relationship could be established between the redox behavior of the compounds determined by cyclic voltammetry and the biochemical data. 相似文献
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采用樟脑衍生物为配体,分别合成了氰基桥联Cu(Ⅱ)-Fe(Ⅲ)-Cu(Ⅱ)三核配合物[{Cu(D,L-La)2}2Fe(CN)6](ClO4) (1)和Mn(Ⅲ)-Fe(Ⅲ)双核配合物[Mn(D,L-Lb)(DMF)(Tp)Fe(CN)3]·(H2O)6 (2)。晶体结构分析表明,化合物1中Cu(Ⅱ)离子处于五配位的配位环境,分别和1个D-La,1个L-La及[Fe(CN)6]3-中的1个氰基配位,2个Cu(Ⅱ)离子通过[Fe(CN)6]3-桥联。通过分子间氢键作用,化合物1形成二维超分子网络结构。化合物2中,[(Tp)Fe(CN)3]-通过其中的1个氰基与[Mn(D,L-Lb)]+桥联,其中Mn(Ⅲ)离子为六配位,分别和四齿配体Lb的2个氧原子和2个氮原子、DMF的1个氧原子及[(Tp)Fe(CN)3]-中的氰基氮原子配位。磁性研究表明,在化合物1中,Cu(Ⅱ)离子与Fe(Ⅲ)离子之间表现出铁磁相互作用,用哈密顿函数H=-2J(S1·S2+S2·S3)对其χMT-T曲线进行拟合,得到1的朗日因子g为2.190,交换常数J为0.55 cm-1。 相似文献
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Weihua Liu Donghai Zhao Zhiwen He Yiming Hu Yuxia Zhu Lingjian Zhang Lianhai Jin Liping Guan Sihong Wang 《Molecules (Basel, Switzerland)》2022,27(24)
Currently, no suitable clinical drugs are available for patients with neurodegenerative diseases complicated by depression. Based on a fusion technique to create effective multi–target–directed ligands (MTDLs), we synthesized a series of (R)–N–(benzo[d]thiazol–2–yl)–2–(1–phenyl–3,4–dihydroisoquinolin–2(1H)–yl) acetamides with substituted benzothiazoles and (S)–1–phenyl–1,2,3,4–tetrahydroisoquinoline. All compounds were tested for their inhibitory potency against monoamine oxidase (MAO) and cholinesterase (ChE) by in vitro enzyme activity assays, and further tested for their specific inhibitory potency against monoamine oxidase B (MAO–B) and butyrylcholinesterase (BuChE). Among them, six compounds (4b–4d, 4f, 4g and 4i) displayed excellent activity. The classical antidepressant forced swim test (FST) was used to verify the in vitro results, revealing that six compounds reduced the immobility time significantly, especially compound 4g. The cytotoxicity of the compounds was assessed by the MTT method and Acridine Orange (AO) staining, with cell viability found to be above 90% at effective compound concentrations, and not toxic to L929 cells reversibility, kinetics and molecular docking studies were also performed using compound 4g, which showed the highest MAO–B and BuChE inhibitory activities. The results of these studies showed that compound 4g binds to the primary interaction sites of both enzymes and has good blood–brain barrier (BBB) penetration. This study provides new strategies for future research on neurodegenerative diseases complicated by depression. 相似文献
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Summary. In order to setup structure-activity relationships and to explore the possibilities of improving the anticancer activity of oxaliplatin, which was recently approved for combination chemotherapy of metastatic colorectal cancer, new oxaliplatin analogues have been synthesized. The cytotoxicity was determined in nine human tumor cell lines and revealed a comparable or even higher cytotoxic potency in leukemia, ovarian and colon cancer cell lines in the case of small substituents at position 4 of the cyclohexane-1,2-diamine ligand. Introduction of bigger substituents at this position and thereby increasing the steric demand of the diamine ligands and the lipophilicity of the oxaliplatin derivatives resulted in platinum complexes with reduced cytotoxic properties. 相似文献
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Lubov’ V. Snegur Alexander A. Simenel Elena A. Morozova Svetlana M. Peregudova Valery N. Babin Natalia V. Bluchterova 《Journal of organometallic chemistry》2004,689(15):2473-2479
The syntheses, structures, electrochemical properties of the series of ferrocenylalkyl azoles, FcAlkAz, as well as the antitumor activity of ferrocenylmethyl benzimidazole (8) have been studied. Above mentioned compounds were investigated by the method of cyclic voltametry. All of them exhibited a reversible one-electron oxidation-reduction wave owing to the ferrocene-ferrocenium redox couple with a positive shift (0.50-0.65 V) compared with that of ferrocene (0.42 V). The X-ray determination of molecular structures of 1-(ferrocenylmethyl)imidazole (4), 1-(ferrocenylbenzyl)imidazole (7) and 1-(ferrocenylmethyl)bezimidazole (8) was carried out. Compound 4 with imidazolyl substituent was found to be present in N-protonated form. Antitumor activity of 1-(ferrocenylmethyl)benzimidazole (8) against some solid tumor models such as adenocarcinoma 755 (Ca755), melanoma B16 (B16) and Lewis lung carcinoma was studied. The antitumor activity of compound 8 was compared with cisplatin effectiveness against some experimental tumor systems. 相似文献