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新型二正丁基锡(IV)衍生物:合成、对肿瘤细胞的高细胞毒性和诱导 KB 癌细胞凋亡。

Novel di-n-butyltin(IV) derivatives: Synthesis, high levels of cytotoxicity in tumor cells and the induction of apoptosis in KB cancer cells.

机构信息

Tongji School of Pharmacy, Huazhong University of Science and Technology, 13 Hangkong Road, Wuhan 430030, PR China.

出版信息

Eur J Med Chem. 2012 Feb;48:305-12. doi: 10.1016/j.ejmech.2011.12.032. Epub 2011 Dec 28.

Abstract

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)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 and (n)Bu(4)Sn(2){3-BrC(6)H(4)C(O)NHO}(2){3-BrC(6)H(4)C(NO)O}. 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.

摘要

两类二丁基锡(IV)羟胺配合物,被配方制成单核混合配体二有机锡(IV)配合物[(n)Bu(2)Sn(HL)Cl] a 和四核(n)Bu(4)Sn(2)(HL)(2)(L)b,它们都被充分地进行了特征描述。X 射线衍射分析也对具有代表性的配合物(n)Bu(2)Sn(2,6-F(2)C(6)H(3)C(O)NHO)Cl(n)Bu(4)Sn(2){3-BrC(6)H(4)C(O)NHO}(2){3-BrC(6)H(4)C(NO)O}进行了研究。所有化合物的细胞毒性都通过 MTT 和 SRB 测定法在三种人类肿瘤细胞系 HL-60、BGC-823 和 KB 上进行了测试。1b 和 4a 被证明比其他化合物和顺铂具有更强的抗肿瘤活性。Annexin V FITC-PI 检测与 MTT 结果一致。细胞周期检测结果表明,在低浓度的 1b、4a 作用下,KB 细胞的细胞周期被阻滞在 G(0)/G(1)期,S 期减少。

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