Platinum(IV) prodrugs with heavy-atom-free BODIPY in axial position: instant photoactivation, enhanced biosafety and improved phototoxicity

Two new photoactivable Pt^IV prodrugs bearing heavy-atomfree BODIPY in the axial position and differing in the linker length were prepared using CuAAC cycloaddition. Under 530 nm green light, both prodrugs produce singlet oxygen and are capable of a rapid cisplatin release in the presence of sodium ascorbate. Investigation of antiproliferative activity demonstrated excellent biosafety of these prodrugs, as well as outstanding phototoxicity under 530 nm low-dose green light.