We report the synthesis of the first transplatin‐BODIPY conjugates for application in photodynamic therapy (PDT). The distyryl BODIPYs containing two iodine atoms were designed to absorb in the red region, easily undergo intersystem crossing for efficient singlet oxygen generation, and additionally offer the possibility for coordination with mono‐activated transplatin. We were able to demonstrate that coordination of the BODIPYs with a mono‐activated transplatin increases the phototoxic index of the photosensitizers significantly, giving rise to highly phototoxic distyryl BODIPY derivatives, of which one was shown to have the highest ever reported phototoxic index against any cell line. Furthermore, the photophysical mechanism of singlet oxygen generation in distyryl BODIPYs undergoing intramolecular charge transfer was studied experimentally and using time‐dependent density functional theory.

中文翻译：

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用于光动力疗法的高光毒性转铂修饰的二苯乙烯基-BODIPY 光敏剂

我们报告了第一个用于光动力疗法 (PDT) 的转铂-BODIPY 偶联物的合成。含有两个碘原子的二苯乙烯基 BODIPY 被设计为在红色区域吸收，容易进行系统间交叉以有效产生单线态氧，并另外提供与单活化转铂配位的可能性。我们能够证明 BODIPY 与单活化转铂的配位显着增加了光敏剂的光毒性指数，产生了高光毒性二苯乙烯基 BODIPY 衍生物，其中一种被证明对任何细胞具有最高的光毒性指数线。此外，