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This problem can be addressed by selectively releasing the desired drugs with light. In a screening approach, we modified known antimetabolite cytostatics with photoremovable protecting groups (PPGs). Sixteen new light\u2010activatable cytostatics with a blue light\u2010activatable diethylaminocoumarin group (DEACM) were synthesized, and their (photo\u2010)chemical properties were tested. The most promising compounds were subjected to cytotoxicity studies with HT\u201029 colon cancer cells. In our experiments, the DEACM\u2010gemcitabine derivative showed the best properties with full recovery of gemcitabine activity after irradiation. In the absence of blue light, this compound was 29 times less toxic. In the next step, based on these results, we designed a red\u2010light activatable derivative of gemcitabine, featuring a heptamethine (Cy7) PPG. We were able to confirm the photorelease of gemcitabine with tissue\u2010penetrating red light in HT\u201029 cells. 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