We prepared four representative square planar gold(III) complexes - [AuCl3(Hpm)], [AuCl2(esal)], [AuCl(dien)]Cl2 and [Au(en)2]Cl3 -and characterized them both in the solid state and in solution. Thereafter, the cytotoxicity of these compounds was evaluated in vitro against the A2780 human ovarian tumor cell line that was used as the reference cell line. Remarkably, ali these gold(III) complexes showed significant cytotoxic effects, [AuCl2(esal)] showing a potency comparable to cisplatin. The present gold(III) complexes were also tested on the corresponding cisplatin-resistant line and revealed they were able to overcome resistance to cisplatin to a large extent. The implications of these findings for the development of new gold(III) complexes to be tested as antitumor agents are discussed