三有机锡(IV) N,C,N螯合物的合成及体外抗真菌和抗肿瘤活性研究

Libor Dostál, Ales Růzicka, Roman Jambor, Vladimír Buchta, Petra Kubanová, Jaroslav Holocek
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引用次数: 3

摘要

化合物1 ~ 3 ({[(CH3)2NCH2]2C6H3}R2SnX的体外抑菌活性(X = Cl, R = n-Bu 1, X = Br, R = 2和X = PF6 n-Bu, R = n = 3部))估计的帮助下修改采用的格式M27-A体外活动的指导方针和与diphenyltin (IV)类似物4和5 (X = Br, R = 4 Ph值和X = PF6, R = Ph值为5),和目前的药物在临床使用(酮康唑、氟康唑、两性霉素B)。这是发现在协调溶剂比苯溶性衍生物2是不活跃(4),化合物1和3甚至是非活性的。本文还报道了离子二苯基锡(IV)复合物4和5对7种人源肿瘤细胞系的体外抗肿瘤活性。本文还介绍了新化合物3的制备和表征(H1、C13和Sn119核磁共振谱和电喷雾电离质谱)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, In vitro Antifungal and Antitumour Activity of Some Triorganotin(IV) N,C,N-Chelates.

The in vitro antifungal activity of compounds 1-3 ({[(CH3)2NCH2]2C6H3}R2SnX; (where X=Cl, R=n-Bu for 1, X=Br, R=n-Bu for 2 and x=PF6, R=n=Bu for 3)) was estimated with the help of a modified microdilution format of the M27-A guidelines and was compared with in vitro activity of their diphenyltin(IV) analogues 4 and 5 (where X=Br, R=Ph for 4 and X=PF6, R=Ph for 5), and of drugs currently in clinical use (ketoconazole, fluconazole and amphotericin B). It was found that in coordinating solvents the more soluble derivative 2 is less active than the phenyl one (4), and compounds 1 and 3 are even inactive.In this paper, the in vitro antitumour activity of ionic diphenyltin(IV) complexes 4 and 5 against seven tumoural cell lines of human origin is also reported. The preparation and characterization (H1, C13 and Sn119 NMR spectroscopy and electrospray ionization mass spectrometry) of the novel compound 3 is mentioned too.

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