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Synthesis and anti-cancer activities of a water soluble gold(III) porphyrin
Journal of Porphyrins and Phthalocyanines ( IF 0.9 ) Pub Date : 2015-02-27 , DOI: 10.1142/s1088424615500236
Aaron D Lammer 1 , Melissa E Cook 1 , Jonathan L Sessler 1
Affiliation  

Gold(III) compounds continue to be explored for their potential utility as anticancer agents. A recognized limitation is the reactivity of gold(III), which is typically reduced to the more labile gold(I) state under physiological conditions. The use of porphyrins can overcome this problem. However, to date the stabilization provided by the use a strongly chelating porphyrin is offset by the poor solubility of the resulting complex in aqueous media. In this work, we describe the synthesis and in vitro anti-cancer activity of a gold(III)porphyrin complex with relatively good aqueous solubility. As judged from standard antiproliferation assays, this complex displays an IC50 of 9 μM for the A2780 human ovarian cancer cell line. This is a higher level of potency than displayed by two related control systems.

中文翻译:


水溶性金(III)卟啉的合成及其抗癌活性



金(III)化合物作为抗癌剂的潜在用途仍在不断探索。公认的限制是金 (III) 的反应性,在生理条件下通常会还原为更不稳定的金 (I) 状态。卟啉的使用可以克服这个问题。然而,迄今为止,通过使用强螯合卟啉提供的稳定性被所得络合物在水性介质中的溶解度差所抵消。在这项工作中,我们描述了具有相对良好水溶性的金(III)卟啉配合物的合成和体外抗癌活性。根据标准抗增殖测定判断,该复合物对 A2780 人卵巢癌细胞系的 IC50 为 9 μM。这比两个相关控制系统所显示的效力更高。
更新日期:2015-02-27
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