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首页> 外文期刊>Photodiagnosis and Photodynamic Therapy >Lead structures for applications in photodynamic therapy. 5. Synthesis and biological evaluation of water soluble phosphorus(Ⅴ) 5,10,15,20-tetraalkylporphyrins for PDT
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Lead structures for applications in photodynamic therapy. 5. Synthesis and biological evaluation of water soluble phosphorus(Ⅴ) 5,10,15,20-tetraalkylporphyrins for PDT

机译：用于光动力疗法的铅结构。 5，PDT用水溶性磷（Ⅴ）5,10,15,20-四烷基卟啉的合成及生物学评价

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摘要

Improved photosensitizers for use in photomedicine must possess good water-solubility and optimal photophysical properties. Phosphorus(Ⅴ) porphyrins fulfill these criteria and are a class of porphyrins with significant potential applications in phototherapy. Five phos-phorus(Ⅴ) porphyrins bearing alkyl substituents have been synthesized. Reasonable to good yields were obtained for all P(Ⅴ) insertions and all compounds underwent biological evaluation for their PDT activity on two esophageal cancer cell lines, OE33 and SKGT-4. Their cellular uptake was investigated using a high content screening method. Notably, three compounds displayed good uptake and using the MTS cell proliferation assay, two were shown to have photocytotoxicity comparable to mTHPC (Temoporfin~®) with IC_(50) values of 6.5 and 5.5 μM.
机译：用于光医学的改进的光敏剂必须具有良好的水溶性和最佳的光物理性质。磷（Ⅴ）卟啉符合这些标准，是一类卟啉，在光疗中具有重要的潜在应用。合成了五种带有烷基取代基的磷（Ⅴ）卟啉。对于所有P（Ⅴ）插入物均获得了合理的良好产量，并且对所有化合物在两种食道癌细胞系OE33和SKGT-4上的PDT活性进行了生物学评估。使用高含量筛选方法研究了它们的细胞摄取。值得注意的是，三种化合物显示出良好的摄取，并且使用MTS细胞增殖测定法，其中两种具有与mTHPC（Temoporfin®）相当的光细胞毒性，IC_（50）值为6.5和5.5μM。

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  • 来源
    《Photodiagnosis and Photodynamic Therapy》 |2014年第4期|510-515|共6页
  • 作者

    Aoife A. Ryan; Mothi M. Ebrahim; Rosine Petitdemange; Gisela M. Vaz; Edyta Paszko; Natalia N. Sergeeva; Mathias O. Senge;

  • 作者单位

    School of Chemistry, SFI Tetrapyrrole Laboratory, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Trinity College Dublin, The University of Dublin, Dublin 2, Ireland;

    School of Chemistry, SFI Tetrapyrrole Laboratory, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Trinity College Dublin, The University of Dublin, Dublin 2, Ireland;

    School of Chemistry, SFI Tetrapyrrole Laboratory, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Trinity College Dublin, The University of Dublin, Dublin 2, Ireland;

    Medicinal Chemistry, Institute of Molecular Medicine, Trinity Centre for Health Sciences, Trinity College Dublin, St. James's Hospital, Dublin 8, Ireland;

    Medicinal Chemistry, Institute of Molecular Medicine, Trinity Centre for Health Sciences, Trinity College Dublin, St. James's Hospital, Dublin 8, Ireland;

    Medicinal Chemistry, Institute of Molecular Medicine, Trinity Centre for Health Sciences, Trinity College Dublin, St. James's Hospital, Dublin 8, Ireland;

    Medicinal Chemistry, Institute of Molecular Medicine, Trinity Centre for Health Sciences, Trinity College Dublin, St. James's Hospital, Dublin 8, Ireland;

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  • 正文语种 eng
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  • 关键词

    Photodynamic therapy; Photosensitizers; Phosphorus; Porphyrins; Cancer; Esophageal cancer;

    机译：光动力疗法;光敏剂;磷;卟啉;癌症;食道癌;

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