首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Novel di-n-butyltin(IV) derivatives: Synthesis, high levels of cytotoxicity in tumor cells and the induction of apoptosis in KB cancer cells.
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Novel di-n-butyltin(IV) derivatives: Synthesis, high levels of cytotoxicity in tumor cells and the induction of apoptosis in KB cancer cells.

机译:新型二丁基锡(IV)衍生物:肿瘤细胞中的合成,高水平的细胞毒性以及Kb癌细胞中凋亡的诱导。

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摘要

Two classes of dibutyltin(IV) hydroxamates complexes, formulated as the mononuclear mixed-ligand diorganotin(IV) complex [(n)Bu(2)Sn(HL)Cl] a and the tetranuclear [(n)Bu(4)Sn(2)(HL)(2)(L)](2)b were fully characterized. X-ray diffraction analyses were also carried out for the representative complexes [(n)Bu(2)Sn(2,6-F(2)C(6)H(3)C(O)NHO)Cl](4a) and [[(n)Bu(4)Sn(2){3-BrC(6)H(4)C(O)NHO}(2){3-BrC(6)H(4)C(NO)O}](2)](1b). The cytotoxicity of all compounds was tested by MTT and SRB assays against three human tumor cell lines HL-60, BGC-823 and KB. 1b and 4a have been shown to be more potent antitumor agents than other compounds and cisplatin. Annexin V FITC-PI assay was consistent with the MTT results. Cell cycle assay results indicated that KB cells displayed an arrest in the G(0)/G(1) phase and a decrease of S phase of the cell cycle at the low concentrations of 1b, 4a.
机译:两类二丁基锡(IV)羟肟酯配合物,配制为单核混合 - 配体Dirootin(IV)复合物[(N)Bu(2)Sn(HL)Cl] A和四核[(N)Bu(4)Sn( 2)(HL)(2)(L)](2)B完全表征。 X射线衍射分析也用于代表络合物[(n)BU(2)Sn(2,6- F(2)C(6)H(3)C(O)NHO)Cl](4A) [(n)bu(4)sn(2)sn(2){3-brc(6)h(4)c(4)c(o)nho}(2){3-brc(6)h(4)c(no)o }](2)](1B)。 通过MTT和SRB测定对三种人肿瘤细胞系HL-60,BGC-823和KB进行所有化合物的细胞毒性。 已经显示出比其他化合物和顺铂更有效的抗肿瘤剂已经显示为1B和4A。 Annexin V FitC-PI测定与MTT结果一致。 细胞周期测定结果表明,Kb细胞在低浓度为1b,4a的低浓度下显示出G(0)/ g(1)相的捕获和细胞周期的S期降低。

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