Light‐Triggered Anticancer Strategies via Azobenzene Photoisomerization

Cancer therapy encounters challenges such as systemic toxicity and poor targeting specificity. Light‐ triggered anticancer strategies enable precise spatiotemporal control over drug activity. Azobenzene, as a key photoswitch due to its reversible trans ‐to‐ cis isomerization, can modulate molecular geometry, dipole moment, and electron distribution. Owing to these properties, azobenzene‐based intelligent anticancer strategies have gained widespread attention. This review systematically reports two azobenzene‐based anticancer strategies: one is light‐triggered drug release, achieved by integrating azobenzene into nanocarriers. The second strategy is photo‐controlled activity, where azobenzene is directly incorporated into bioactive molecules (e.g., functional proteins inhibitors, tubulin binders, G4 DNA ligands) to reversibly modulate their activity via conformational switching. This work consolidates these advanced applications to provide a framework for developing intelligent anticancer therapies with enhanced precision and minimized side effects.