Gryshuk Amy L, Graham Andrew, Pandey Suresh K, Potter William R, Missert Joseph R, Oseroff Allan, Dougherty Thomas J, Pandey Ravindra K
Photodynamic Therapy Center, Roswell Park Cancer Institute, Buffalo, NY 14263, USA.
Photochem Photobiol. 2002 Nov;76(5):555-9. doi: 10.1562/0031-8655(2002)076<0555:afcsop>2.0.co;2.
A first report on the synthesis and comparative in vitro-in vivo photosensitizing efficacy of various fluorinated and the corresponding nonfluorinated, purpurinimide-based photosensitizers is discussed. In preliminary in vivo screening, compared with the nonfluorinated analogs, purpurinimides bearing trifluoromethyl substituents showed enhanced photosensitizing efficacy. Among compounds (isomers) with similar lipophilicity, the position of the substituents was found to play a decisive role in biological efficacy.
本文讨论了关于各种氟化及相应的非氟化、基于紫红素-18的光敏剂的合成及其体外-体内光敏疗效比较的首次报告。在初步的体内筛选中,与非氟化类似物相比,带有三氟甲基取代基的紫红素-18显示出增强的光敏疗效。在具有相似亲脂性的化合物(异构体)中,发现取代基的位置对生物疗效起决定性作用。