Development of Tailor‐Made Cytostatics Activable by Acid‐Catalyzed Hydrolysis for Selective Tumor Therapy

The diamidophosphate 1, which is hardly toxic at physiological pH (7.2), undergoes cleavage at pH 6.2 (the pH value found in tumor cells) to glucose, methanol, and a cytotoxic ketone (t½ = 15 h). The survival rate of tumor cells can thereby be decreased in vitro by a factor of 5×104.