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杂化钛(IV)邻苯二酚/哌嗪体系及其抗癌性能。

Heteroleptic titanium(IV) catecholato/piperazine systems and their anti-cancer properties.

机构信息

Department of Chemistry, University of Bath, Claverton Down, Bath BA2 7AY, UK.

出版信息

Dalton Trans. 2014 Jan 21;43(3):1380-5. doi: 10.1039/c3dt52583j. Epub 2013 Nov 7.

Abstract

In this paper we report the synthesis and full characterisation of a range of Ti(IV)-catecholato systems complexed to piperazine or homopiperazine salan ligands. The steric/electronic environment of the catecholate moiety has been varied and the effect this has on cytotoxicity discussed. It was observed that the 7-membered homopiperazine complexes are more stable to hydrolysis than their piperazine cousins in biological media. In general the homopiperazine complexes show higher cytotoxicity than the piperazine complexes, with the most cytotoxic complex exhibiting IC50 (μM) values of 3 ± 0.5 μM (HT-29) and 4 ± 1 μM (OVCAR).

摘要

在本文中,我们报告了一系列与哌嗪或六亚甲基二胺-salan 配体配位的 Ti(IV)-邻苯二酚体系的合成和全面表征。改变了邻苯二酚部分的立体/电子环境,并讨论了其对细胞毒性的影响。观察到 7 元杂环哌嗪配合物在生物介质中比其哌嗪同类物更稳定,不易水解。一般来说,杂环哌嗪配合物的细胞毒性比哌嗪配合物高,最具细胞毒性的配合物的 IC50(μM)值分别为 3±0.5μM(HT-29)和 4±1μM(OVCAR)。

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