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新型铂(Ⅱ)类配合物的合成、表征和抗肿瘤活性 总被引:2,自引:0,他引:2
Seven novel platinum(Ⅱ) complexes[Pt(Ⅱ)(NH3)(H2O)X](Ⅰ~Ⅶ) {X=(COO-)2(oxalato), 2p-CH3O-C6H4-COO-(p-methyoxbenzolato), 2C6H5-COO-(benzolato), 2CH3COO-(acetato), (CH2)(COO-)2(malonato), (CH2)2(COO-)2(succinato), (CH=CH)(COO-)2(maleato)} have been prepared and characterized by elemental analysis, thermal analysis,IR, UV, and 1H NMR spectroscopy. The antitumor activities of these complexes in vitro against EJ、HCT-8, KB, BGC-823, Bel-7402, HL-60, MCF-7 and Hela cell lines have been studied. Complex Ⅰ and Ⅴ show remarkable antitumor activities against EJ cell line, and the inhibitory rate is 45.96% and 54.32% at concentration of 10 μmol·L-1, respectively. The inhibitory rate of the complexes Ⅱ and Ⅲ is greater than 50% against HL-60, BGC-823, KB and EJ cell lines. The inhibitory rate of the complex Ⅵ is 51.89% and 57.96% against BGC-823 and EJ cell lines. The complexes Ⅳ and Ⅶ have no antitumor activities against tested tumor cell lines. The complexes Ⅱ, Ⅲ and Ⅵ can stem the cell cycle of HL-60 on the G2+M. 相似文献
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替莫唑胺是临床上治疗胶质瘤的一线药物。我们将替莫唑胺进行化学修饰,作为配体引入到四价铂配合物中,合成了2种新型四价铂配合物P1T和P2T,并利用核磁共振氢谱及碳谱对其进行了基础表征。研究结果表明,配合物具有良好的脂溶性和较快的水解速率。进一步使用MTT法、流式细胞术、共聚焦成像及蛋白免疫印迹法对P1T和P2T的抗肿瘤活性及诱导肿瘤细胞死亡机制进行了深入的探究。结果发现,配合物P1T和P2T对胶质瘤细胞株A261表现出了较高的细胞毒性,而对正常神经细胞HT-22毒性较小,表现出了较好的细胞选择性。流式细胞术揭示配合物P1T和P2T将细胞周期阻滞在G2/M期,导致DNA损伤,最终诱导肿瘤细胞凋亡。 相似文献
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以顺-二碘-二环戊胺合铂(Ⅱ)为起始原料,经聚合反应和胺化反应制得顺式-二碘-异丙胺-环戊胺合铂(Ⅱ)(2);2分别与氯化钾,1,1-环丁基二羧酸钾和一水合草酸钾反应,合成了3个新型的铂配合物:顺式-二氯-异丙胺-环戊胺合铂(Ⅱ)(1a,收率36.6%),顺式-1,1-环丁基二羧酸-异丙胺-环戊胺合铂(Ⅱ)(1b,收率43.6%)和顺式-草酸-异丙胺-环戊胺合铂(Ⅱ)(1c,收率28.1%),其结构经1H NMR,IR,ESI-MS和元素分析表征。采用MTT法测定了1a~1c对肝癌(SMMC-7721),肺癌(A-549),乳腺癌(MCF-7)和结肠癌(SW480)的体外抑制活性。结果表明,1a~1c对部分癌细胞的IC50值小于40μm,具有一定的体外肿瘤生长抑制活性。 相似文献
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20世纪60年代,美国密执安州立大学Rosenberg发现了顺铂具有抗癌活性,开辟了金属类抗肿瘤药物研究的新领域.经过40余年的研究,已相继成功开发了卡铂、奈达铂、奥沙利铂、舒铂、洛铂和双环铂等铂类抗肿瘤药物.虽然对于铂类抗肿瘤药物研究取得了一定的成绩,但在临床使用过程中也存在一些问题,如其毒副作用和抗药性,限制了其在临床上的进一步广泛应用.为了解决这些问题,科研工作者开始寻找新的金属类抗肿瘤药物以弥补现有铂类抗肿瘤药物的不足.在金属元素中,唯有钯(II)与铂(II)配合物具有相似或相同的结构特征,进而表现出相近或相似的化学性质.因此,继铂类抗肿瘤配合物后,钯(II)配合物作为潜在抗肿瘤药物成为一个诱人的领域.本文综述了近年来钯(II)类抗肿瘤药物的研究进展,并探讨了其构效关系,这对于指导新型钯(II)类抗肿瘤药物的合成具有重要的参考价值. 相似文献
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合成了一个新型的双核Pt(Ⅳ)配合物{[cis-Pt(NH3)2Cl(OH)2]2(4,4'-methylenedianiline)}(NO3)2(化合物1)及相应的 15N标记化合物{[cis-Pt(15NH3)2Cl(OH)2]2(4,4'-methylenedianiline)}(NO3)2(化合物15N-1).利用1H NMR和ESMS进行了结构表征,化合物15N-1的2D[1H,15N]HSQC NMR发现,该化合物在水溶液中存在同分异构体.2D[1H,15N]HSQC NMR技术跟踪了化合物15N-1与Guanosine-5'-Monophosphate(5'-GMP)和Glutathione(GSH)的反应.结果显示,5'-GMP能在0.5 h内将化合物1还原,而GSH在6 h以后才能够部分的将化合物1还原.化合物1所表现出来的反应性能将有利于提高其治疗效果和降低毒副作用. 相似文献
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支链/环链烷氧基乙酸为离去配体的铂(Ⅱ)配合物的体外活性研究 总被引:1,自引:0,他引:1
合成了12个带支链/环链烷氧基乙酸为离去基团的顺铂类配合物,通过元素分析、红外光谱、核磁共振氢谱和质谱对配合物进行了表征。研究了所有化合物对人非小细胞肺癌A549、人肝癌细胞BEL-7402和人乳腺癌细胞MCF-7细胞系的体外抗肿瘤活性。测试结果表明,12个配合物中有5个对人乳腺癌细胞系MCF-7有较好的体外活性。其中化合物2(顺-二(异丙氧基乙酸根)·二氨合铂(Ⅱ))在所有的化合物中显示最高的活性,对所测3个细胞系都是如此。 相似文献
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长链线性配合物具有特有的结构、成键和性质,在分子器件和特殊性能低维材料等方面展示出潜在的应用前景。在低价状态下,铂系金属可自聚合形成一类含有多个金属原子的线性金属链式簇合物。本文就有关线性低价铂系金属簇合物的研究进展作一简述。 相似文献
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Ajai K. Singh P. Kumar Raghavendra Garima Singh Sumit Bali 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3-4):903-911
Abstract The ligand chemistry of telluroethers, halotellurium ligands, and polytellurides has received good attention in the last decade. Tellurium-containing species have been used to design clusters. In the recent past the ligation of di and tri-telluroethers (including bis(4-methoxyphenyltelluro)methane) has been studied. Hybrid organotellurium ligands, N-[2-(4-methoxyphenyltelluro)propyl]phthalimid (L 1 ), 2-(4-ethoxyphenyltelluromethyl)-tetrahydro-2H-pyran (L 2 ), 2-(2-{4-ethoxyphenyl} telluroethyl)-1,3-dioxane (L 3 ), N-{2-(4-methoxyphenyltelluro)ethyl}morpholine (L 4 ), N-{2-(4-methoxyphenyltelluro)ethyl}-pyrrolidine (L 5 ), bis{2-(pyrrolidine-N-yl)ethyl}telluride (L 6 ), 1-(4-methoxyphenyltelluro)-2-[3-(6-methyl-2-pyridyl) propoxy]ethane (L 7 ), and 2-[2-(4-methoxyphenyltelluro)ethyl]thiophene (L 8 ) have been designed recently and studied for their complexation reactions. The (Te, N) and (N, Te, N) ligands, L 5 and L 6 , coordinate with Hg(II) through Te and N both, but the bonding with N is some what weak. The morpholine nitrogen of L 4 does not coordinate with Pd(II) or Pt(II) along with Te. The L 7 behaving as a (Te, N) ligand has formed 20-membered metallomacrocycle ring with Pt(II). Tellurated Schiff bases 4-MeOC6H4TeCH2CH2N═C(CH3)C6H4-2-OH (L 9 ) and 2-HO-C6H4-(CH3)C═NCH2CH2TeCH2CH2N═C(CH3)C6H4-2-OH (L 10 ) and their reduction products 4-MeOC6H4TeCH2CH2NHCH(CH3)C6H4-2-OH (L 11 ) and 2-HO-C6H4-(CH3)CHNHCH2CH2TeCH2CH2NHCH(CH3)C6H4-2-OH (L 12 ) respectively have been synthesized and studied for ligation behaviour. The L 9 on reaction with the [Ru(p-cymene)Cl2]2 results in [Ru(p-cymene)(4-MeOC6H4TeCH2CH2NH2)Cl]Cl · H2O whereas in the reaction of L 10 with [Ru(p-cymene) Cl2]2, p-cymene ligand is lost resulting in [RuCl(L 10 -H)]. The recent developments, particularly designing of L 1 to L 12 and their ligand chemistry, are reviewed in the present paper. 相似文献
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