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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis and antiproliferative activity of hydroxyferrocifen hybrids against triple-negative breast cancer cells
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Synthesis and antiproliferative activity of hydroxyferrocifen hybrids against triple-negative breast cancer cells

机译：羟基二茂铁杂化物的合成及其对三阴性乳腺癌细胞的抗增殖活性

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We have recently shown that the combination of chemical motifs of vorinostat (SAHA) and ferrocifen (FcTAM) in the single FcTAM-SAHA hybrid produced beneficial effects in terms of antiproliferative activity of both agents against cancer cells. Since hydroxylation of FcTAM to form hydroxyferrocifen (FcOHTAM) improves the biological response, we explore in this work the anticancer effects of a new family of hybrid phenolic compounds bearing some molecular features of FcOHTAM, OHTAM and SAHA. Results concerning their cytotoxicity on both triple-negative MDA-MB-231 and hormone-dependent MCF-7 breast cancer cells are reported here. Organometallic compounds showed better antiproliferative activities than organic analogs. For instance, FcOHTAM-SAHA (IC_(50) = 1.5 μM) was around seven times more active than OHTAM-SAHA (IC_(50) = 10.9 μM) against MCF-7 cells. In the case of triple-negative MDA-MB-231 cells, the IC_(50) values for ferrocene compounds are in the range of 1.3-4.5 μM and those for organic derivatives are 5.2-34.5 μM. Studies concerning the isomerization and redox behaviors of these compounds are also presented. Despite the potential of FcOHTAM-SAHA to exhibit ex cellulo redox activation, it seems that this feature is not completely expressed in cellulo. This surprising behavior is related to the driving effect of the side chain to direct the new constructs to different targets.
机译：我们最近显示，在单一FcTAM-SAHA杂化物中，伏立诺他（SAHA）和二茂铁（FcTAM）的化学基序的组合在两种药物对癌细胞的抗增殖活性方面均产生了有益的作用。由于FcTAM的羟基化形成羟基二茂铁（FcOHTAM）可以改善生物学反应，因此我们在这项工作中探索了具有FcOHTAM，OHTAM和SAHA某些分子特征的杂酚类化合物的新家族的抗癌作用。此处报道了有关它们对三阴性MDA-MB-231和激素依赖性MCF-7乳腺癌细胞的细胞毒性的结果。有机金属化合物显示出比有机类似物更好的抗增殖活性。例如，针对MCF-7细胞，FcOHTAM-SAHA（IC_（50）= 1.5μM）的活性是OHTAM-SAHA（IC_（50）= 10.9μM）的活性的七倍左右。对于三阴性MDA-MB-231电池，二茂铁化合物的IC_（50）值在1.3-4.5μM的范围内，而有机衍生物的IC_（50）值为5.2-34.5μM。还介绍了有关这些化合物的异构化和氧化还原行为的研究。尽管FcOHTAM-SAHA可能表现出细胞外的氧化还原激活，但似乎该功能并未在纤维素中完全表达。这种令人惊讶的行为与侧链将新构建体导向不同靶标的驱动作用有关。

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