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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Fluorination on non-photolabile dppz ligands for improving Ru(ii) complex-based photoactivated chemotherapy
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Fluorination on non-photolabile dppz ligands for improving Ru(ii) complex-based photoactivated chemotherapy

机译：用于改善Ru（II）复合光活化化疗的非光型DPPZ配体氟化

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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.
机译：Ru（II）可以接受光诱导的配体解离和随后的DNA共价结合的息肉配合物可能潜在用作光活化的化学治疗性（PACT）试剂。 本文研究了三种含有四种单齿吡啶配体的三种氟化DPPZ配体配位Ru（II）配合物（2-4）。 所有复合物释放出一个吡啶并在470nm辐射时与DNA共价结合。 与亲本复合物[Ru（DPPZ）（py）（4）（4）]（2+）（1），2-4显示出增强的光毒性，但暗细胞毒性减少，对PACT应用更有利。 复杂3是最有效的IC50值，朝向HeLa和Skov-3细胞系约8μm，并且还具有更高的IC50值朝向正常的L-02细胞。 我们的结果表明，保持配体上的氟化可以是改善ru（ii）分解剂的药物活性的有效方法。

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    Boerhan Rena; Sun Weize; Tian Na; Wang Youchao; Lu Jian; Li Chao; Cheng Xuexin; Wang Xuesong; Zhou Qianxiong;

  • 作者单位

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

    Chinese Acad Sci Tech Inst Phys &

    Chem Key Lab Photochem Convers &

    Optoelect Mat Beijing 100190 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;无机化学;
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