LAUSR

An increasing number of novel Ru(II) polypyridyl complexes have been successfully applied as photosensitizers (PSs) for photodynamic therapy (PDT). Despite recent advances in optimized PSs with refined photophysical properties, the lack of tumoral selectivity is often a major hurdle for their clinical development. Here, classical maleimide and versatile NHS‐activated acrylamide strategies were employed to site‐selectively conjugate a promising Ru(II) polypyridyl complex to the N‐terminally Cys‐modified Bombesin (BBN) targeting unit. Surprisingly, the decreased cell uptake of these novel Ru‐BBN conjugates in cancer cells did not hamper the high phototoxic activity of the Ru‐containing bioconjugates and even decreased the toxicity of the constructs in the absence of light irradiation. Overall, although deceiving in terms of selectivity, our new bioconjugates could still be useful for advanced cancer treatment due to their nontoxicity in the dark.