The formation and isolation of the antitumor drug cisplatin analogue cis- The reactivity of the complex to model nucleobases 9-ethylguanine (9-EtGH) and 1-methylcytosine (1-MeC) has been investigated by 1 H NMR spectroscopy at 45°C in aqueous media. The results show that 1 reacts slowly with 9-EtGH (t 1/2 ≈ 5 days) by displacement of Cl -, producing cis- ) 2 (9-EtGH-N 7 ) 2 ], which is similar to the major cross-link adduct of cisplatin with DNA. However, 1 gives no reaction with 1-MeC. This appears to be due to the lesser reactivity of 1-MeC and to competition between the cross-link reaction and dimerization of 1 to [Pt 2 (µ-mtpo-N 3 ,N 4 ) 4 ]. Circular dichroism studies of DNA in the presence of 1 show that the platinum complex reacts efficiently after 48 h at a optimum ratio of 0.25 Pt atom/mol of DNA nucleotide. These results and those obtained from reaction of 1 with 9-EtGH suggest that the platinum compound binds the N7 atoms of two guanines of the same strand, forming intrastrand cross-linked adducts. Chelation of DNA bases by 1 causes important conformational changes, bringing the guanines close together. The anticancer activity of complex 1 has been tested against the human cancer cell lines MCF-7 breast carcinoma and A121 ovarian carcinoma. Results indicate a moderate antitumor activity against breast carcinoma and a marked and selective cytotoxic effect against ovarian carcinoma.