Department of Chemistry, King's College London, London, UK.
Dalton Trans. 2019 May 7;48(18):5892-5896. doi: 10.1039/c8dt04706e.
Copper(ii) coordination complexes, 1 and 2, containing nonsteroidal anti-inflammatory drugs (NSAIDs) potently kill breast cancer stem cells (CSCs) and bulk breast cancer cells. Although detailed biological studies have been conducted to shed light on their mechanism of cytotoxicity, little is known about their molecular level mechanism of action. This biophysical study, aided by the preparation of a fluorophore-containing analogue, 3, reveals that the complexes operate by undergoing reduction to a copper(i) form and releasing the associated NSAIDs.
铜(II)配合物 1 和 2,其中含有非甾体抗炎药(NSAIDs),能够有效杀死乳腺癌干细胞(CSCs)和乳腺癌细胞。尽管已经进行了详细的生物学研究来阐明其细胞毒性机制,但对其分子水平作用机制知之甚少。这项生物物理研究在制备含有荧光团类似物 3 的帮助下,揭示了这些配合物通过还原为铜(I)形式并释放相关的 NSAIDs 来发挥作用。