Fluorination on non-photolabile dppz ligands for improving Ru(ii) complex-based photoactivated chemotherapy

被引：21

作者：

Boerhan, Rena ^{[1
,2
]}

Sun, Weize ^{[1
,2
]}

Tian, Na ^{[1
,2
]}

Wang, Youchao ^{[1
,2
]}

Lu, Jian ^{[1
,2
]}

Li, Chao ^{[1
]}

Cheng, Xuexin ^{[1
]}

Wang, Xuesong ^{[1
,2
]}

Zhou, Qianxiong ^{[1
]}

机构：

[1] Chinese Acad Sci, Tech Inst Phys & Chem, Key Lab Photochem Convers & Optoelect Mat, Beijing 100190, Peoples R China

[2] Univ Chinese Acad Sci, Beijing 100049, Peoples R China

来源：

DALTON TRANSACTIONS | 2019年 / 48卷 / 32期

基金：

国家重点研发计划;

关键词：

RUTHENIUM(II) POLYPYRIDYL COMPLEXES; TRANSITION-METAL-COMPLEXES; PHOTODYNAMIC THERAPY; CELLULAR UPTAKE; EXCITED-STATES; DNA-BINDING; LIGHT; PHOTOCHEMISTRY; PHOTOPHYSICS; STRATEGY;

D O I：

10.1039/c9dt01594a

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Ru(ii) polypyridine complexes which can undergo photo-induced ligand dissociation and subsequent DNA covalent binding may potentially serve as photoactivated chemotherapeutic (PACT) agents. In this paper, three fluorinated dppz ligand coordinated Ru(ii) complexes (2-4) containing four monodentate pyridine ligands were studied. All complexes released one pyridine and covalently bound to DNA upon 470 nm irradiation. Compared with the parent complex [Ru(dppz)(py)(4)](2+) (1), 2-4 displayed enhanced phototoxicity but diminished dark cytotoxicity, more favorable for PACT application. Complex 3 is the most efficient one with IC50 values of about 8 mu M toward HeLa and SKOV-3 cell lines, and also has a much higher IC50 value toward normal L-02 cells. Our results indicate that fluorination on the retaining ligand may be an efficient way to improve the drug activity of Ru(ii) PACT agents.

引用

页码：12177 / 12185

页数：9

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