| Autor: |
Jian Lu, Chao Li, Rena Boerhan, Xuexin Cheng, Qianxiong Zhou, Weize Sun, Na Tian, Xuesong Wang, Youchao Wang |
| Rok vydání: |
2019 |
| Předmět: |
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| Zdroj: |
Dalton transactions (Cambridge, England : 2003). 48(32) |
| ISSN: |
1477-9234 |
| Popis: |
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 μM 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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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