Amino-BODIPY conjugates with various 2-phenyl-3-hydroxyquinolinones (3-HQs) connected via cleavable disulfide linker and non-cleavable maleimide linker were prepared and tested on cytotoxic activity and fluorescent ratiometric “OFF-ON” monitoring of cleavage inside the cells was demonstrated. Disulfide conjugates exhibited improved cytotoxicity compared to the free 3-HQs whereas non-cleavable maleimide conjugates stayed inactive proving that disulfide linker is responsible for cleavage inside the cells and therefore resulting in cytotoxicity of disulfide Amino-BODIPY-3HQ conjugates.

中文翻译：

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通过与 2-苯基-3-羟基-4(1H)-喹啉酮缀合调节氨基-BODIPY 的细胞毒性

制备了通过可裂解二硫键和不可裂解马来酰亚胺接头连接的各种 2-苯基-3-羟基喹啉酮 (3-HQ) 的氨基-BODIPY 缀合物，并测试了细胞毒性活性和细胞内裂解的荧光比例“OFF-ON”监测被证明。与游离的 3-HQ 相比，二硫键缀合物表现出改善的细胞毒性，而不可裂解的马来酰亚胺缀合物保持非活性，证明二硫键接头负责细胞内的裂解，因此导致二硫键 Amino-BODIPY-3HQ 缀合物的细胞毒性。