A dinuclear gold(I) pyrrolidinedithiocarbamato complex (1) with a bidentate carbene ligand has been constructed and shows potent in vitro cytotoxic activities towards cisplatin‐resistant ovarian cancer cells A2780cis. Its rigid scaffold enables a zinc(II)‐based metal–organic framework (Zn‐MOF) to be used as a carrier in facilitating the uptake and release of 1 in solutions. Instead of using a conventional dialysis approach for the drug‐release testing, in this study, a set of transwell assay‐based experiments have been designed and employed to examine the cytotoxic and antimigratory activities of 1@Zn‐MOF towards A2780cis. Gold medicine: A dinuclear gold(I) pyrrolidinedithiocarbamato complex with a bidentate carbene ligand has been constructed and shows potent in vitro cytotoxic and antimigratory activities towards cisplatin‐resistant ovarian carcinoma A2780cis. Its rigid scaffold enables a zinc(II)‐based metal–organic framework (Zn‐MOF) to be used in facilitating its uptake and release in solutions.