Three heterobimetallic gold(I)-ruthenium(II) complexes containing heteroditopic bipyridine-N-heterocyclic carbene (NHC) ligands were synthesized and fully characterized by spectroscopic methods and in one case by single-crystal X-ray diffraction. In addition, the in vitro cytotoxic, antileishmanial, and antimalarial activities of these new heterobimetallic complexes were assessed. Moreover, the photophysical properties of two compounds have been used to localize them in tumor cells by confocal microscopy.