一种针对癌症的奥沙利铂释放型 Pt(iv)-前药。

A cancer specific oxaliplatin-releasing Pt(iv)-prodrug.

机构信息

Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.

出版信息

Dalton Trans. 2018 May 15;47(19):6679-6682. doi: 10.1039/c8dt01458b.

DOI:10.1039/c8dt01458b

PMID:29708261

Abstract

We prepared a Pt(iv)-prodrug, which under cancer specific conditions (elevated concentration of reactive oxygen species, ROS) releases a DNA-binding drug oxaliplatin as well as ROS-amplifying drugs p-quinone methide and N-alkylferrocenium. Due to the concerted action of these components, an excellent anticancer effect was achieved: IC50 = 0.4 ± 0.1 μM for human ovarian carcinoma A2780 cells. Importantly, the prodrug was found to be 45-fold less toxic to normal cells (HDFa).

摘要

我们制备了一种 Pt(iv)-前药，该前药在癌症特异性条件下（活性氧物种（ROS）浓度升高）释放出 DNA 结合药物奥沙利铂以及 ROS 放大药物对醌甲醚和 N-烷基二茂铁。由于这些成分的协同作用，实现了优异的抗癌效果：对人卵巢癌细胞 A2780 的 IC50 = 0.4 ± 0.1 μM。重要的是，该前药对正常细胞（HDFa）的毒性低 45 倍。