Biphenyl-gold(III) complexes: a promising scaffold in the fight against cancer. Organometallic gold(III) complexes have attracted a large attention as potential anticancer agents in the last decades. The main advantage of organometallic complexes is their high redox stability in physiological media due to the presence of Au-C bounds. In this respect, bis-cyclometalated [(C^N^C)AuL]+ complexes have demonstrated great potential. However, their main limitations are the large number of coordination site occupied by the pincer ligands, leaving only one or no coordination sites available for other ligands. To enlarge the scope of structures that can be evaluated and potentially explore new modes of actions while preserving the high redox stability of bis-cyclometalated complexes, a reorganization of their coordination sphere appeared highly promising. Using a biphenyl ligand giving two Au-C bounds would preserve the high redox stability of bis-cyclometalated complexes while offering two coordination sites available for various ligands to optimize the anticancer properties of the complexes. Thus, this scaffold led to structures ranging from very labile which activity is due to one decoordinated ligand to hemilabile complexes and up to highly stable complexes in cellulo for which the active principle is the native cationic complex.