Gold(III) complexes, isostructural and isoelectronic with platinum(II) comp
lexes, are of potential interest as antitumor drugs. We prepared four repre
sentative square planar gold(III) complexes - [AuCl3(Hpm)], [AuCl2(esal)],
[AuCl(dien)]Cl-2 and [Au(en)(2)]Cl-3 - and characterized them both in the s
olid state and in solution. Thereafter, the cytotoxicity of these compounds
was evaluated in vitro against the A2780 human ovarian tumor cell line tha
t was used as the reference cell line. Remarkably, all these gold(III) comp
lexes 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 t
o overcome resistance to cisplatin to a large extent. The implications of t
hese findings for the development of new gold(III) complexes to be tested a
s antitumor agents are discussed.