Six dibutyl‐1,3,2‐dioxastannolanes, including two enantiomeric pairs, exhibited greater in vitro antitumour activity towards a variety of human tumour cell lines than cisplatin but with little discrimination, suggesting hydrolysis to a common cytotoxic intermediate. A cell line hypersensitive to mitochondrial inhibitors (CI80–13S) was not sensitive to any of the test compounds, suggesting that cell mechanisms other than, or in addition to, mitochondrial function are targeted by tin antitumour agents. A pigmented melanoma cell line (MM418c5) was resistant to the test compounds, which were found to be sequestered by melanin. This resistance was not observed with triphenyltin hydroxide.