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首页> 外文期刊>Polyhedron: The International Journal for Inorganic and Organometallic Chemistry >Cyclopentadienyltin(IV) derivatives: synthesis, characterization and study of their cytotoxic activities
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Cyclopentadienyltin(IV) derivatives: synthesis, characterization and study of their cytotoxic activities

机译:环戊二烯基锡(IV)衍生物:细胞毒性活性的合成,表征和研究

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The organotin compounds. [SnPh3(C5H4R)] (R = Bu' (1), CMe2(CH2CH2CH=CH2) (2)) and [SnPh3(C5Me4R)] (R = H (3), SiMe3 (4)), were prepared by the reaction of SnPh3Cl with the lithium derivative of the corresponding cyclopentadiene. 1-4 have been characterized by multinuclear NMR spectroscopy (H-1, C-13{H-1} and Sn-119{H-1)). In addition. the molecular structures of 1, 2 and 4 were determined by single-crystal Xray diffraction studies. The cytotoxic activity of the organotin(IV) complexes (1-4) was tested against human tumour cell lines 8505C anaplastic thyroid cancer, A253 head and neck turnout. A549 lung carcinoma, A2780 ovarian cancer, DLD-1 colon carcinoma. Compounds 1-4 present higher activities than cisplatin in all the studied cells. The highest sensitivity of the synthesized tin(IV) complexes was observed against A2780 ovarian cancer and DLD-1 colon carcinoma. Complex 3 presents the highest cytotoxic activity of all the studied complexes in all the cancer cells, with IC50 values from 0.037 to 0.085 mu M, however, its trimethylsilyl-substituted analogue (4), showed the lowest activity against all the studied cells with IC50 values from 0.163 to 0.351 mu M. Complexes 1 and 2 presented very similar activities on all the cancer cells (IC50 values from 0.044 to 0.119 mu M).
机译:有机锡化合物。 [SnPh3(C5H4R)](R = Bu'(1),CMe2(CH2CH2CH = CH2)(2))和[SnPh3(C5Me4R)](R = H(3),SiMe3(4))通过SnPh3Cl与相应的环戊二烯的锂衍生物反应1-4已经通过多核NMR光谱法表征(H-1,C-13 {H-1}和Sn-119 {H-1))。此外。通过单晶X射线衍射研究确定1、2和4的分子结构。测试了有机锡(IV)配合物(1-4)对人肿瘤细胞系8505C间变性甲状腺癌,A253头颈部反跳的细胞毒活性。 A549肺癌,A2780卵巢癌,DLD-1结肠癌。在所有研究的细胞中,化合物1-4的活性均高于顺铂。观察到合成的锡(IV)配合物对A2780卵巢癌和DLD-1结肠癌的最高敏感性。复合物3在所有癌细胞中均表现出最高的细胞毒性活性,IC50值为0.037至0.085μM,然而,其三甲基甲硅烷基取代的类似物(4)对所有具有IC50的细胞显示出最低的活性化合物1和2在所有癌细胞上表现出非常相似的活性(IC 50值从0.044到0.119μM),从0.163到0.351μM。

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