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Di-n-butyltin oxide reacted with p-[N,N-bis(2-chloroethyl)amino]benzoic acid to yield the compounds {{4-[(ClCH2CH2)2N]C6H4COOSnBu2}2O}2 (1) and {4-[(ClCH2CH2)2N]C6H4COO}2SnBu2 (2), which have been characterized by IR and ^1H NMR spectra. The X-ray diffractional studies of 1 reveal the structure of the molecule to be a dimer, in which the two Bu2Sn groups were linked via two bridging oxygen atoms to form a central Bu4Sn2O2 unit. And the tin atom adopts two carbons from two n-butyl groups and three oxygen atoms from the acid and the bridging oxygen. In vitro test showed compound 1 to exhibit high cytotoxicity against P388 and HL-60 cell lines. 相似文献
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哌嗪取代卟啉的合成、表征及其抗癌活性 总被引:2,自引:0,他引:2
设计并合成了6个具有抗癌活性的哌嗪取代卟啉化合物,分别为5,10,15,20-四[4-(4'-乙基哌嗪基)苯基]卟啉(TEPPH2,8a),5,10,15,20-四[4-(4'-丁基哌嗪基)苯基]卟啉(TBPPH2,8b),5,10,15,20-四[4-(4'-庚基哌嗪基)苯基]卟啉(THPPH2,8c),5,10,15,20-四[4-(4'-苯基哌嗪基)苯基]卟啉(TPhPPH2,8d),5-[4-(4'-乙基哌嗪基)苯基]-10,15,20-三苯基卟啉(EPTPPH2,8e)和5-[4-(4'-丁基哌嗪基)苯基]-10,15,20-三苯基卟啉(BPTPPH2,8f).这些卟啉化合物都由取代苯甲醛与吡咯缩合而成,每一个卟啉分子中含有一个或四个具有抗癌活性的取代哌嗪结构,结构经元素分析,MS,1H NMR,IR和UV-vis等表征.初步的生物活性研究表明,这些化合物具有一定的抗癌活性,因而在医学上可能具有潜在应用前景. 相似文献
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总结了具有强抗癌活性的天然产物cryptophycins及其结构类似物的研究进展, 内容包括cryptophycin的合成、 活性-结构关系规律以及结构类似物的研究情况. 相似文献
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近年来,我们以荧光素为母体合成了一系列的衍生物,药理试验证实其中许多种对肿瘤细胞有明显的杀伤和抑制增殖作用。本文用非线性映照(NLM)模式识别技术研究其活性分类,得到分类清晰的映照图,确定了该类衍生物抗ECa 109细胞的主要结构因素,为指导合成新化合物建立了预报模型。 1 结构参数选择与非线性映照 相似文献
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合成了13种N-取代靛蓝衍生物,其中6种为新化合物.研究了靛蓝的N-取代衍生物与抗痛活性的关系,发现大多数N-取代靛蓝衍生物与靛玉红有相似的抗癌活性,某些甚至离于綻玉红的抗癌活性. 相似文献
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以胡椒碱为母核进行结构改造,合成了一系列胡椒碱-双环酰胺衍生物;并用核磁共振氢谱(1H NMR),核磁共振碳谱(13C NMR)和高分辨质谱(HRMS)进行了结构确证.噻唑蓝(MTT)比色法测试结果表明,目标化合物对肾细胞(293T)、宫颈癌(HeLa)和乳腺癌(MDA-MB-321)细胞有良好的抑制活性,大多数衍生物对HeLa细胞的抑制活性优于阳性对照药5-氟尿嘧啶(5-FU)和胡椒碱.化合物6b对HeLa细胞的抗增殖活性最高,半数抑制浓度(IC50)为3.49μmol/L,对MDA-MB-321细胞的IC50值为20.89μmol/L.机理研究发现,化合物6b不仅可有效抑制HeLa细胞的迁移、侵袭、黏附和克隆能力,而且对HeLa细胞肿瘤异种移植物的生长表现出强烈的抑制作用.因此,化合物6b有可能成为肿瘤治疗中潜在的先导化合物. 相似文献
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水溶性卟啉及其系列金属化合物的合成、抗癌活性及其作用机制研究 总被引:14,自引:0,他引:14
合成了水溶性四-[(4-三甲铵基)苯基]卟啉TAPP及其金属卟啉化合物MTAPP,其中M=Zn(),Cu(),Fe(),Co(),Ni(),Mn().通过元素分析、紫外-可见光谱确定了化合物的组成和结构.以紫外-可见光谱、荧光光谱及粘度法等手段研究了卟啉化合物TAPP和金属卟啉化合物ZnTAPP与小牛胸腺DNA的相互作用,结果表明,TAPP,ZnTAPP与DNA相互作用使紫外-可见光谱发生了8~12nm的红移,并出现了明显的减色效应.荧光光谱强度明显增大,吸收峰位发生变化.以艾氏腹水癌(Ac)和肝癌(Hept)细胞为靶细胞,采用MTT染色法评价了化合物的抗癌活性,部分化合物表现出较高的抗癌活性 相似文献
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《Journal of Coordination Chemistry》2012,65(14):2091-2101
AbstractDinuclear ruthenium complexes [Ru2(bpy)4BL](ClO4)2 (Ru-1), where bpy = 2,2′-bipyridine and BL = 2,2′-((1E,1′E)-((E)-diazene-1,2-diyl-bis(2,1-phenylene))-bis(azanylylidene))bis(methanylylidene))diphenol (a bidentate bridging ligand), and mononuclear ruthenium complexes [Ru(bpy)2L](ClO4) (Ru-2), where L = (E)-2-((phenylimino)methyl)phenol, were synthesized and characterized by elemental analysis and electrospray ionization mass spectrometry. Their photophysical and electrochemical properties were also studied. The cytotoxicity of the two complexes in vitro was evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The results indicated that Ru-1 and Ru-2 exhibited significant dose-dependent cytotoxicity to human breast cancer (MCF-7), gastric cancer (SGC-7901), cervical cancer (Hela), and lung cancer (A549) tumor cell lines. Ru-1 showed excellent antitumor effects in a cellular study (IC50 values of 3.61 μM for MCF-7 human breast cancer cells in vitro). However, Ru-2 exhibited the highest cytotoxicity to Hela cells; the IC50 value is 3.71 μM. The results reveal that Ru-1 and Ru-2 have obvious selectivity and might be a potential anticancer agent that could improve the efficacy of common anticancer therapies. 相似文献
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Cheng-Ting Zi Liu Yang Fa-Wu Dong Qing-Hua Kong Zhong-Tao Ding Jun Zhou 《Natural product research》2020,34(16):2301-2309
Abstract Two new compounds (9 and 10) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound 10 showed highly potent against HL-60 cell line tested, with IC50 value 17.69?±?0.19?μM. This compound suggested its potential as anticancer agents for further development. 相似文献
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Pelin Koparir 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):1028-1034
AbstractThiosemicarbazides (2a–e) were obtained by the interaction of furan-2-carboxylic acid hydrazide (1) with five different isothiocyanate (RNCS) derivatives. By addition of KOH to the reaction medium, ethyl, allyl, phenyl and benzyl, p-tolyl substituted 1,2,4-triazoles (3a–e) were obtained. 3a–e were dissolved in dry acetone containing K2CO3 in the presence of 2-chloro-1-(3-methyl-3-mesitylcyclobutyl) ethanone (4) to give 3,4,5-trisubstituted 1,2,4-triazole sulfanyl compounds containing a cyclobutane ring (5a–e). The structures of the final compounds were confirmed by elemental analyses, FT-IR, 1H-NMR and 13C-NMR. The antioxidant and antitumor properties of the synthesized compounds were also investigated. Three of the triazole derivatives with p-tolyl, benzyl and phenyl substituents (5c–e) displayed good antioxidant and antitumor activity in comparison to the standards. 相似文献
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Six novel diorganotin(IV) complexes have been synthesized in good yields by the reaction of R2SnCl2 (R= methyl, phenyl) with the Schiff base derived from salicylaldehyde and substituted thiosemicarbazide. The complexes were characterized by elemental analysis, IR, 1H NMR and MS spectra. The structure of 2f was confirmed by single crystal X‐ray diffraction. The crystal of 2f is triclinic, space group P‐1 with a = 0.84996(12), b = 1.1204(2), c = 1.27597(12) nm, β = 81.908(9)°, V=1.0904(2) nm3, Z = 2, Dc= 1.551 g/cm3. The final discrepancy factors are R = 0.0211 and Rw = 0.0536 for 3710 independent reflections. Tests of antitumor activities in vitro showed that the obtained complexes had relative inhibition interaction to the KB, HCT‐8 and BEL‐7402 tumor cell lines. 相似文献
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Junhu Qin Mei Zhu Hongmei Zhu Liqiong Zhang Yihong Fu Jiamin Liu 《Phosphorus, sulfur, and silicon and the related elements》2020,195(7):592-599
AbstractA series of novel pyridazinone derivatives containing the 1,3,4-thiadiazole moiety were synthesized and characterized by 1H NMR, 13C NMR, spectroscopies HRMS and IR. Among them, the structure of compound 5c (2-(Tert-butyl)?4-chloro-5-((5-((2-ethylphenyl)amino)?1,3,4-thiadiazol-2-yl)thio)pyridazin-3(2H)-One) was unambiguously confirmed via single crystal X-ray diffraction analysis. The inhibitory activity of all the target compounds against MGC-803 and Bcap-37 was determined by MTT assay, with doxorubicin (the inhibition rates were 95.5?±?0.4% and 95.7?±?1.0% respectively) as a control. The preliminary results showed that the inhibitory activity of compound 5n (2-(Tert-butyl)?4-chloro-5-((5-((3-fluorophenyl)amino)?1,3,4-thiadiazol-2-yl)thio)pyridazin-3(2H)-One) was superior to the others. The inhibition rates of MGC-803 and Bcap-37 cells were 86.3?±?2.2% and 92.3?±?0.6% at a concentration of 10?μmol/L, respectively. The preliminary structure-activity relationship showed that when the 2-position of the benzene ring was substituted by a methyl group, such as compound 5j (2-(Tert-butyl)?4-chloro-5-((5-((2,3-dimethylphenyl)amino)?1,3,4-thiadiazol-2-yl)thio)pyridazin-3(2H)-One), it exhibited good anticancer activity on MGC-803 cells. Besides, introducing fluorine, chlorine, or trifluoromethyl group onto the benzene ring, such as compound 5?m (2-(Tert-butyl)?4-chloro-5-((5-((4-(trifluoromethoxy)phenyl)amino)?1,3,4-thiadiazol-2-yl)thio)pyridazin-3(2H)-One), displayed good anticancer activity on MGC-803 and Bcap-37 cells. 相似文献
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以N-甲基-4-氯-2-吡啶甲酰胺为原料,经过4步共合成4个化合物(S-1,S-2,R-1和R-2),其中2个为新的化合物(S-1和R-2)。经过1H NMR,13C NMR,HR-MS等方法对其结构表征。最后通过CTG法,测试4种化合物对四种人肝癌细胞(PLC/PRF/5,Hep3B,HepG2,BEL-7402)的抑制活性。结果表明:S-1,S-2,R-1和R-2均表现较明显的对4种细胞的抑制活性,且呈现出浓度依赖关系。IC50值从1304nM到11228nM。其中化合物R-1(瑞格非尼)对PLC/PRF/5和HepG2细胞,S-1对Hep3B细胞的抑制活性,R-2对HepG2的细胞活性均较高于原药索拉非尼。 相似文献