共查询到20条相似文献,搜索用时 15 毫秒
1.
A series of novel Schiff base derivatives was designed and synthesized from 3,3'-azobenzaldehyde and 3,3'-azoxybenzaldehyde. The newly synthesized compounds were characterized by FTIR, 1H NMR, MS and elemental analysis and tested for their in vitro antiproliferative activities against HeLa cell lines. At the same time, the impact on the antitumor activity of the sulfanilamido, benzamido, phenolic hydroxyl or thiourea groups was investigated and discussed. Compounds 4, 6 and 10 were found to exhibit strong cytotoxic activity. 相似文献
2.
3.
4.
以(取代)水杨醛、间(对)羧基苯胺和氨基甲酰肼为原料,分别采用冰浴法合成了4-(二乙基氨基)水杨醛-3-羧基苯胺(3a),4-(二乙基氨基)水杨醛-4-羧基苯胺(3b)和水杨醛-3-羧基苯胺(3c);采用固相法合成了4-(二乙基氨基)水杨醛-氨基甲酰肼(3d);采用水浴回流法合成了3,5-二溴水杨醛-4-羧基苯胺(3e)和2-羟基-1-萘甲醛-4-羧基苯胺(3f),3a~3f均为新化合物,其结构经1H NMR,IR,ESI-MS和元素分析表征。研究了3a~3f对大肠杆菌、金黄色葡萄球菌及欧文氏草生杆菌的抑菌活性。结果表明:3a~3f对受试菌种均有一定的抑菌活性,其中3e的抑菌活性最好。 相似文献
5.
Isatin undergoes regioselective 1,3‐dipolar cycloaddition reactions with porphyrin azomethine ylides derived from Ni(II) β‐formyl‐meso‐tetraphenylporphyrins in the presence of N‐methylglycine to afford novel spiro porphyrin derivatives. 相似文献
6.
Two novel porphyrin derivatives, 5,10,15,20-tetra(4-(N-octane-carboxamide)phenyl)porphyrin (4NC8-TPP) and 5,10,15,20-tetra(4-(N-stearyl-carboxamide)phenyl)porphyrin (4NC18-TPP), were synthesized. Their molecular structures were characterized by means of time-of-flight mass spectrometer (TOF-MS), nuclear magnetic resonance (NMR), and infrared spectra (IR). The thermal behavior and morphologies of 4NC8-TPP and 4NC18-TPP were examined by thermal gravity (TG), differential scanning calorimetry (DSC), x-ray diffraction (XRD), and polarizing optical microscope (POM). It was found that both 4NC8-TPP and 4NC18-TPP had mesogenic properties. 相似文献
7.
根据拼合原理, 设计并合成了21个未见报道的新的二芳醚基哌嗪类衍生物, 其结构用1H NMR, ESI-MS, HRMS进行了确证, 初步生物活性测定实验证明部分目标化合物具有良好的细胞毒活性. 化合物4i分别对人食管癌(Eca109)细胞株和人鼻咽癌(CNE)细胞株的IC50为7.13和4.54 μmol8226;L-1, 与对照品顺铂(DDP)相近. 化合物5d对人鼻咽癌细胞株也表现较好的活性, 其IC50为8.49 μmol8226;L-1. 相似文献
8.
以乙酰乙酸乙酯、4-羟基苯甲醛、碳酸氢铵和二溴烷烃为原料,经两步反应合成溴烷氧基1,4-二氢吡啶;再将其与5-对羟基苯基-10,15,20-三苯基卟啉缩合,得到了12种新型的卟啉-二氢吡啶及其金属锌配合物,结构通过NMR,IR和HRMS进行详细表征.研究中测试了这些复杂的卟啉-二氢吡啶化合物对金黄色葡萄球菌(Staphylococcus aureus,ATCC 25923)和大肠杆菌(Escherichia coli,ATCC 25922)的抑菌活性,实验结果显示这12种化合物都有很好的抑菌活性,其中对金黄色葡萄球菌抑菌效果较好,且卟啉-二氢吡啶二元化合物的抑菌效果优于两种单体. 相似文献
9.
以汉防己甲素为原料,经溴代反应制得关键中间体5-溴汉防己甲素(2); 2与硼酸衍生物经Suzuki反应合成了6个新型的汉防己甲素衍生物(4a~4f),其结构经1H NMR, 13C NMR和ESI-MS表征。采用CCK-8法初步考察了4a~4f对人早幼粒白血病细胞(HL60)和人肺癌细胞(A549)的抑制活性;并采用MTT法对活性较好的化合物进行复筛。采用酶联免疫吸附法考察4a~4f对多种受体酪氨酸激酶的抑制活性。结果表明:4b, 4c和4e对HL60和A549有一定的抑制活性; 4b和4c对受体酪氨酸激酶FGFR1的抑制活性大于50%。 相似文献
10.
Two new flavanols, (8S,9R)‐9,10‐dihydro‐5,9‐dihydroxy‐8‐(3,4,5‐trimethoxyphenyl)‐2H,8H‐benzo[1,2‐b:3,4‐b′]dipyran‐2‐one ( 1 ) and (2S,3R)‐3,4‐dihydro‐3,5‐dihydroxy‐2‐(3,4,5‐trimethoxyphenyl)‐2H,8H‐benzo[1,2‐b:3,4‐b′]dipyran‐8‐one ( 2 ), were isolated from the stems of Glycosmis pentaphylla. The structures of these compounds were determined by extensive spectroscopic (UV, IR, HR‐ESI‐MS, 1D‐ and 2D‐NMR) analyses. The cytotoxic activities of these compounds were evaluated using the MTT method. The results showed that compounds 1 and 2 exhibited considerable cytotoxic activities against HL‐60 and A549 cell lines. 相似文献
11.
从中药陈皮中提取橙皮苷,通过酸水解制备橙皮素,再分别与苯肼类、苯甲酰肼类、苯氨基脲类、苯氨基硫脲类、苯乙酰肼类、苯氧乙酰肼类和苯氨基乙酰肼类化合物缩合得到相应的橙皮素席夫碱类化合物。 用紫外、红外、核磁共振氢谱、质谱及元素分析等技术手段对化合物的结构进行了表征。 测定并比较了橙皮苷、橙皮素及其席夫碱新化合物清除超氧自由基(O-·2)、羟自由基(·OH)和2,2-二苯基-1-苦味酰基自由基(DPPH·)的活性及总还原能力。 结果表明,在1.0 g/L时,这些化合物均具有抗氧化活性,其中部分橙皮素席夫碱化合作用强于橙皮苷和橙皮素。 相似文献
12.
13.
A series of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives was designed and synthesized.All of them were screened for their cytotoxic activities against large cell lung cancer(H460),colon cancer (HT-29) and adenocarcinomic lung cancer(A549) cell lines in vitro.The pharmacological results indicate that most of the target compounds show moderate to significant activities.Especially compound 17 exhibits the most potent antitumor activities against H460,HT-29 and A549 cell lines with IC50 values of 0.57,0.45 and 1.45 μmol/L,respectively. 相似文献
14.
15.
Marcin Stolarczyk Aleksandra Wolska Aleksandra Mikoajczyk Iwona Bryndal Jerzy Cieplik Tadeusz Lis Agnieszka Matera-Witkiewicz 《Molecules (Basel, Switzerland)》2021,26(8)
Enterococcus faecalis is known as a significant nosocomial pathogen due to its natural resistance to many antibacterial drugs. Moreover, it was found that E. faecalis infection causes inflammation, production of reactive oxygen species, and DNA damage to human gastric cancer cells, which can induce cancer. In this study, we synthesized and tested the biological activity of a new Schiff base, 5-[(4-ethoxyphenyl)imino]methyl-N-(4-fluorophenyl)-6-methyl-2-phenylpyrimidin-4-amine (3), and compared its properties with an analogous amine (2). In the biological investigation, 3 was found to have antibacterial activity against E. faecalis 29212 and far better anticancer properties, especially against gastric adenocarcinoma (human Caucasian gastric adenocarcinoma), than 2. In addition, both derivatives were non-toxic to normal cells. It is worth mentioning that 3 could potentially inhibit cancer cell growth by inducing cell apoptosis. The results suggest that the presence of the –C=N– bond in the molecule of 3 increases its activity, indicating that 5-iminomethylpyrimidine could be a potent core for further drug discovery research. 相似文献
16.
17.
《Arabian Journal of Chemistry》2014,7(2):219-226
A series of 1-methyl-N-[(substituted-phenylmethylidene)-1H-benzimidazol-2-amines (4a–4g) were prepared via the formation of 1-methyl-1H-benzimidazol-2-amine (3), which was prepared by the cycloaddition of o-phenylenediamine (1) with cyanogen bromide in the presence of aqueous base followed by N-methylation with methyl iodide in the presence of anhydrous potassium carbonate in dry acetonitrile. Moreover, the four-membered β-lactam ring was introduced by the cycloaddition of 4a–4g and chloroacetyl chloride in the presence of triethylamine catalyst to give 3-chloro-1-(1-methyl-1H-benzimidazol-2-yl)-(4′-substituted)-phenylazetidin-2-one 5a–5g. A total of 14 compounds were synthesized and characterized by IR, 1H NMR, 13C NMR and Mass spectral technique, in addition they were evaluated for anti-bacterial and cytotoxic properties. Among the chemicals tested 4a, 4b, 5a, 5b, 5g exhibited good antibacterial activity and 5f, 5g shown good cytotoxic activity in vitro. 相似文献
18.
19.
Eight Schiff bases have been synthesized using 3‐alkyl‐4‐amino‐1,2,4‐triazole‐5‐thione and substituted benzaldehyde as starting materials. The structures of the compounds have been confirmed by 1H NMR, IR and elemental analysis and their biological activities to five vegetable pathogens have been tested. The results showed that they exhibited good fungicidal activities. 相似文献