In addition to showing antiproliferative effects against human cancer cells, the compound potently and selectively inhibits PARP1 with respect to the seleno‐enzyme thioredoxin reductase.[154] Preliminary studies of this Au(III) PARPi indicated promising anti‐proliferative activity towards several cancer cell lines and an additive relationship when explored in combination with cisplatin. Here, PARP1 is linked to cancer.