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The synthesis and properties of unsymmetrical 3,7-diaminophenothiazin-5-ium iodide salts: Potential photosensitisers for photodynamic therapy
Dyes and Pigments ( IF 4.1 ) Pub Date : 2006 , DOI: 10.1016/j.dyepig.2005.06.011
S GORMAN , A BELL , J GRIFFITHS , D ROBERTS , S BROWN

A series of unsymmetrical 3,7-(N,N-disubstituted-amino)-phenothiazin-5-ium iodides have been prepared by stepwise reaction of secondary amines with phenothiazin-5-ium tetraiodide hydrate. The singlet oxygen generating efficiencies and polarity characteristics of the dyes are compared with those of Methylene Blue, and the factors influencing the potential value of these compounds as photosensitisers for photodynamic therapy are discussed. Preliminary data for the in vivo anti-tumour efficacy of the compounds suggest that high lipophilicity is an important requirement for high activity.

中文翻译:

不对称的3,7-二氨基吩噻嗪-5-碘化物盐的合成和性质:光动力疗法的潜在光敏剂

通过仲胺与吩噻嗪-5-四碘化物水合物的逐步反应,已经制备了一系列不对称的3,7-(NN-二取代-氨基)-吩噻嗪-5-碘化物。将染料的单线态氧产生效率和极性特性与亚甲基蓝的相比,并讨论了影响这些化合物作为光动力疗法光敏剂的潜在价值的因素。该化合物的体内抗肿瘤功效的初步数据表明,高亲脂性是高活性的重要要求。
更新日期:2017-01-31
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