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用于缺氧癌症治疗的环金属化铱(III)-二甲双胍配合物的设计。

The design of cyclometalated iridium(iii)-metformin complexes for hypoxic cancer treatment.

机构信息

MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, China.

出版信息

Chem Commun (Camb). 2021 Jan 28;57(9):1093-1096. doi: 10.1039/d0cc07104h. Epub 2021 Jan 12.

Abstract

Modulating the hypoxic microenvironment is the priority for tumor treatment. Cytometalated iridium(iii)-metformin conjugates were synthesized for treating hypoxic cancer cells for the first time, which alleviate hypoxia via mitochondria respiration inhibition, thus displaying 10-fold higher cytotoxicity, emerging anti-metastasis and anti-inflammatory activities than a metformin-free Ir(iii) complex and cisplatin against hypoxic cancer cells.

摘要

调控缺氧微环境是肿瘤治疗的重点。首次合成了金属化铱(III)-二甲双胍缀合物用于治疗缺氧癌细胞,通过抑制线粒体呼吸来缓解缺氧,从而显示出比无二甲双胍的 Ir(III)配合物和顺铂对缺氧癌细胞高出 10 倍的细胞毒性、抗转移和抗炎活性。

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