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首页> 外文期刊>Chemistry: A European journal >Reactivity and Antiproliferative Activity of Ferrocenyl-Tamoxifen Adducts with Cyclodextrins against Hormone-Independent Breast-Cancer Cell Lines
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Reactivity and Antiproliferative Activity of Ferrocenyl-Tamoxifen Adducts with Cyclodextrins against Hormone-Independent Breast-Cancer Cell Lines

机译：二茂铁基-他莫昔芬加合物与环糊精对激素非依赖性乳腺癌细胞系的反应性和抗增殖活性

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Hydroxyferrocifen compounds are a new and promising class of ferrocifen-type breast-cancer drug candidates. They possess both endocrine-modulating properties and cytotoxic activity, which come from the tamoxifen skeleton and the presence of a ferrocene moiety, respectively. However, they suffer from reduced solubility in water, which presents a problem for their eventual therapeutic use. Herein, we examined the interactions of hydroxyferrocifen compounds with cyclodextrins (CDs) to evaluate whether or not their electron-transfer oxidation pathways were affected by their inclusion. It has been demonstrated that these inclusion complexes are soluble in pure water, which shows that CDs can be used to deliver these biologically active molecules. Therefore, a series of these compounds has been investigated by cyclic voltametry in various media in the presence of CDs (P-CD and Me-beta-CD). In methanol, the hydroxyferrocifen compounds exhibited a weak interaction with the CD cavity. These interactions became stronger as the amount of added water increased. The complexation effect between the hydroxyferrocifen compounds and beta-CD was found to be stronger if the CD was partially methylated, which is probably due to hydrophobic effects between the cyclopentadienyl ring and/or the aromatic rings and the methoxy groups. Moreover, it appears that the structure of the hydroxyferrocifen compounds affects both their solubility and their complexation dynamics. Investigations in the presence of pyridine show that the base kinetically favors the dissociation of the ferrocifen-CD complex during the electron transfer step, but does not affect the follow-up reactivity of the electrogenerated ferrocenium cation, which leads eventually to the corresponding quinone methide, as reported in the absence of CD. Accordingly, the cytotoxicity of these beta-CD-encapsulated organometallic complexes in hormone-independent breast-cancer cells (MDA-MB231) were confirmed to be similar to those obtained in the absence of cyclodextrin.
机译：羟基二茂铁化合物是一类新的有前途的二茂铁型乳腺癌候选药物。它们具有内分泌调节特性和细胞毒性活性，分别来自他莫昔芬骨架和二茂铁部分的存在。但是，它们在水中的溶解度降低，这给它们最终的治疗用途带来了问题。在本文中，我们研究了羟基二茂铁化合物与环糊精（CD）的相互作用，以评估它们的电子转移氧化途径是否受其包合影响。已经证明这些包合配合物可溶于纯水，这表明CD可用于递送这些生物活性分子。因此，在CDs（P-CD和Me-beta-CD）存在下，通过循环伏安法在各种介质中研究了一系列这些化合物。在甲醇中，羟基二茂铁化合物与CD腔的相互作用较弱。随着添加水量的增加，这些相互作用变得更强。如果CD部分甲基化，发现羟基二茂铁化合物与β-CD之间的络合作用更强，这可能是由于环戊二烯基环和/或芳环与甲氧基之间的疏水作用。而且，看来羟基二茂铁化合物的结构影响了它们的溶解性和它们的络合动力学。在吡啶存在下的研究表明，该碱在动力学上有利于电子转移步骤中二茂铁-CD络合物的分解，但不影响电生成的二茂铁阳离子的后续反应性，最终导致生成相应的醌甲基化物，如无CD报道。因此，证实了这些β-CD-包封的有机金属复合物在激素非依赖性乳腺癌细胞（MDA-MB231）中的细胞毒性类似于在不存在环糊精的情况下获得的细胞毒性。

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