In this article, we report the design, synthesis, photodynamic properties, and in vitro\nevaluation of photoactivatable prodrug for the poly (ADP-ribose) polymerase 1 (PARP-1) inhibitor\nTalazoparib. In order to yield a photoactivatable, inactive prodrug, photoactivatable protecting groups\n(PPGs) were employed to mask the key pharmacophore of Talazoparib. Our study confirmed the\ngood stability and photolytic effect of prodrugs. A PARP-1 enzyme inhibition assay and PARylation\nexperiment showed that the inhibitory activity of the prodrug was reduced 380 times and more\nthan 658 times, respectively, which proved that the prodrugâ??s expected activity was lost after PPG\nprotection. In BRCA1- and BRCA2-deficient cell lines, the inhibitory activity of the compound was\nsignificantly restored after ultraviolet (UV) irradiation. The results indicate that the photoactivatable\nprodrug strategy is an interesting approach for studying PARP inhibitors. Meanwhile, the described\nphotoactivatable prodrug also provided a new biological tool for the mechanism research of PARP
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