The biological activity of four cisplatin-like Pt-phosphane complexes, namely, cis-[PtCl 2 (L) 2 ], L = PPh 3 , P(Ph) 2 (p-C 6 H 4 -COOH), P(Ph) 2 (-CH 2 CH 2 -COOH) and its succinimidyl ester derivative, has been tested on monolayer cultures of three tumour cell lines (namely, A2780 human ovarian carcinoma and its cisplatin-resistant form A2780Cp8, and human colon adenocarcinoma HCT116). These complexes can undergo intramolecular rearrangements by virtue of their functionalized phosphanes, thereby existing as fully opened (O) or fully closed (C) forms. Our results show that only the opened forms exhibit moderate activity, which, although inferior to the ac-[a]