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以D-半乳糖和二缩三乙二醇为原料,经乙酰化、糖基化和叠氮化钠取代等反应合成了带叠氮连接臂的半乳糖配基,通过点击化学反应将其与炔丙基修饰的马蹄金素(MTS)衍生物进行连接,设计合成了6个具有潜在肝靶向性的半乳糖糖基化MTS衍生物.通过1H NMR,13C NMR,1H-1H COSY,HMQC,DEPT和ESI-MS对其结构进行了表征;采用Hep G2 2.2.15细胞模型初步评价了目标化合物的抗乙型肝炎病毒(HBV)活性.结果表明,所有目标化合物对HBV DNA的复制均有抑制作用,且具有一定的量效关系;化合物15f在50μg/m L浓度下对Hep G2 2.2.15细胞株的抑制率为83%,具有进一步研究的价值. 相似文献
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以具有抗HBV活性的苯丙氨酸二肽化合物马蹄金素(MTS)为先导化合物,设计并合成了23个新型的苯丙氨酸三肽衍生物(4a~4h, 5, 6a, 6b和8a~8k),其结构经1H NMR, 13C NMR和MS(ESI)表征。采用HepG2 2.2.15细胞为乙肝病毒载体,评价了目标化合物的抗HBV活性。结果表明:化合物5(IC50=2.98 μM)、 6b(IC50=0.62 μM)和8k(IC50=5.07 μM)对HBV DNA复制的抑制活性优于MTS(IC50=11.16 μM)。 相似文献
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以马蹄金素[N-(N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇,MTS]为先导化合物,设计并合成了11个NO供体型马蹄金素衍生物,所有目标产物均未见文献报道,其结构经NMR,ESI-MS确认.以HepG2 2.2.15细胞为乙肝病毒载体,对合成的马蹄金素衍生物进行了抗乙肝病毒活性测试.结果表明,在测试浓度范围内,化合物6d,6e,6g具有抗HBV活性,其半数抑制浓度分别为6.88,37.51,11.07μmol/L.其中,化合物6d和6g的半数抑制浓度优于MTS(11.16μmol/L),且具有较高的抑制率,具有进一步研究开发的价值. 相似文献
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《有机化学》2016,(10)
以β-蒎烯的衍生物诺蒎酮为原料,合成了系列新型蒎烷基噻唑衍生物,并对其生物活性进行了研究.β-蒎烯经高锰酸钾氧化所得到的诺蒎酮与氨基硫脲进行缩合反应,得到诺蒎酮缩氨基硫脲;诺蒎酮缩氨基硫脲再与α-卤代酮进行环化,得到新型蒎烷基噻唑衍生物2a~2l.采用FTIR,1H NMR,13C NMR和HRMS对化合物2a~2l的结构进行了表征.探讨了化合物2a~2l的抑菌活性、对人脐静脉内皮细胞(HUVECs)的抗炎活性以及对紫薇蚜虫的杀虫活性.结果表明,化合物2b具有很好的抗菌活性,对细菌和真菌的抑制效果分别与阿米卡星和酮康唑的效果相当;化合物2a则具有显著的抗炎活性,化合物2e、2h、2i和2k对紫薇蚜虫具有一定的杀虫活性. 相似文献
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以丹皮酚和对氯苯甲醛为起始原料,通过Claisen-Schmidt反应得到2-羟基-4-甲氧基-4"-氯查尔酮(3),再经过Mannich反应得到10个查尔酮曼尼希碱衍生物(4a~4e, 5a ~ 5e)。目标化合物结构均经高分辨质谱(HR-MS)、核磁共振氢谱(1H-NMR)、核磁共振碳谱(13C-NMR)进行确证。采用MTT法测试了上述化合物对人肺癌细胞A549、人肝癌细胞HepG2的体外抗增殖活性。实验结果表明,目标化合物对肿瘤细胞A549、HepG2均具有较强的细胞增值抑制作用,且明显优于阳性对照药5-氟尿嘧啶(5-FU)。 相似文献
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以2-巯基咪唑类化合物为原料,室温下与含有端基炔的二芳基高碘盐反应,一步合成苯并咪唑并[2,1-b]噻唑衍生物,其结构经1H NMR、13C NMR、 单晶X-衍射和HR-MS表征。在最佳反应条件[n(2-巯基苯并咪唑)/n(二芳基高碘盐)=1/1,二氯甲烷为溶剂,反应12 h]下,目标化合物的产率最高为84%。同时对该反应的机理进行了详细探讨,并采用MTT法研究了目标化合物对人肝癌细胞(HepG2)生长情况的影响。结果表明:当浓度为4 μg/mL时,化合物3b具有较强的抑制HepG2细胞增殖的活性,抑制率为52%。 相似文献
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<正>Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition-elimination reactions.The structures of these novelly synthesized compounds were verified by ~1H NMR,ESI-MS and single crystal X-ray diffraction.Furthermore,all four compounds(most notably compound 7a) were found to be highly efficient against hepatitis B virus (HBV) in cultured HepG2 2.2.15 cell,making them promising drug candidates for potential bioactive molecule against hepatitis B. 相似文献
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《结构化学》2017,(12)
In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1 Hbenzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) ?, Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702. 相似文献
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LIU Xiu-jie WANG Song-qing ZHANG jing ZHANG Feng-xia LI Gui-zhu WANG Bao-jie SHAO Ying-lu ZHANG Li-guang FANG Lin CHENG Mao-sheng 《高等学校化学研究》2006,22(3):356-359
Introduction Themeritsofantiplatelettherapyforthepreven tionofthrombosisincardiovasculardiseaseareevi dent.Meta analysisresultshaveshownthatsecondary preventionbyantiplateletaggregationagentscanreduce theriskofnonfatalmyocardialinfarction(MI)and strokeby2… 相似文献
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通过5-取代苯基异噁唑-3-甲基胺与2-氰基-3,3-二甲硫基丙烯酸取代酯的缩合反应,合成了一系列含5-取代苯基异噁唑环结构的氰基丙烯酸酯类衍生物,并采用核磁共振波谱和元素分析对化合物的结构进行了表征.初步的生物活性测试结果表明,部分化合物显示出较好的除草活性,在1500 g/ha剂量下,化合物7h,7i和7m对芥菜的茎叶处理抑制率分别为90%,40%和100%;化合物7m和7n对繁缕的茎叶处理抑制率分别为100%和80%;化合物7m和7n对小藜的茎叶处理抑制率分别为100%和85%.此外,化合物7b和7c还表现出良好的抗肿瘤活性,其对HepG2细胞的IC50值分别为3.2和10.1μmol/L. 相似文献
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以大黄酸为原料,经酯化、烷基化、水解及缩合等反应步骤合成了12个大黄酸-缬氨酸加合物.目标化合物经1H NMR,~(13)C NMR和HRMS进行了结构确证.以顺铂和阿霉素为阳性对照药,采用四甲基偶氮唑盐(MTT)法考察了目标化合物的体外抗肿瘤(Hela,MCF-7,HepG2,KB和HEK293T等5株细胞)活性.结果表明,化合物5l显示出较好的抗肿瘤活性,其IC50值在1.6~9.4μmol/L之间.作用机制研究结果表明,化合物5l能够与DNA发生较强的结合作用. 相似文献
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《Journal of heterocyclic chemistry》2018,55(7):1574-1578
A series of 1‐azaaurone derivatives were designed and synthesized from 3,5‐dimethoxyaniline and 2‐chloroacetonitrile. Their structures were characterized by melting point, 1H NMR, IR, and elemental analysis, as well as 13C NMR. The target compounds were evaluated for antitumor activities against human hepatocellular liver carcinoma cell line (HepG‐2) and human cervix carcinoma cell line (Hela) using methyl thiazolyl tetrazolium method. The results revealed that several 1‐azaaurones exhibited strong proliferation inhibition efficacy against HepG‐2 and Hela with an IC50 range of 5.6–8.8 μg/mL without damaging normal cell. 相似文献
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Li J Tang MT Wu Q Chen H Niu XT Guan XL Li J Deng SP Su XJ Yang RY 《Natural product communications》2012,7(5):599-602
A new lignan, (7'R,8'R)-threo-strebluslignanol-2-O-beta-D-glucopyranoside, along with 8 known compounds (2-9) were isolated from the water-soluble part of the MeOH extract of the heartwood of Streblus asper. Their structures were elucidated through various spectroscopic methods, including 1D NMR (1H NMR, 13C NMR), 2D NMR (HMQC, HMBC, and NOESY), and HRMS. The stereochemistry at the chiral centers was determined using the CD spectrum, as well as analyses of coupling constants and optical rotation data. In the preliminary bioassay, the isolated compounds did not show anti-HBV activities in vitro using the HBV transfected HepG2.2.15 cell line. 相似文献
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Synthesis and Biological Activities of Novel 6‐Alkylamino‐11,12‐dihydro‐11‐arylbenzo[c]phenanthridine Derivatives 下载免费PDF全文
Min Zhang Li Liu Huifeng Xiao Ting Zhao Liuqing Yang Xiaohua Xu 《Journal of heterocyclic chemistry》2016,53(1):234-240
A series of novel benzo[c]phenanthridine derivatives 2a , 2b , 2c , 2d , 2e , 2f , 2g , 2h , 2i , 2j , 2k , 2l , 2m and 3a , 3b , 3c , 3d , 3e , 3f bearing an alkylamino side chain at their 6‐position were synthesized. All of the target compounds were confirmed by 1H NMR, 13C NMR, and HRMS, and some of them were also characterized by IR and 19F NMR. The preliminary bioassays showed that the target compounds displayed fungicidal activities; for example, compound 2l showed 60.0% and 70.0% inhibitive activity against Alternaria solani and Cercospora arachidicola at 50 mg/L, respectively, and some compounds also displayed plant growth‐regulating activities. 相似文献