The development of a photo‐responsive micellar system capable of triggering cell death is reported. Precursors of the micelles are synthesized by connecting a lipophilic chain to a hydrophilic polyethylene glycol via a photo‐labile nitrobenzyl group. The resulting amphiphilic units are self‐assembled in water forming 12 nm micelles that are readily internalized into cells. Upon photo‐irradiation, micelles undergo cleavage and yield a cytotoxic nitrosobenzaldehyde derivative, which significantly inhibits the proliferation of MDA‐MB‐231 cells under standard in vitro conditions.
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