cis-bis(pyridine)platinum(II) organoamides with unexpected growth inhibition properties and antitumor activity

Lorraine K. Webster, Glen B. Deacon, David P Buxton, Brian L Hillcoat, Alison James, Ian A G Roos, Robin J. Thomson, Laurence P G Wakelin, Tracey L Williams

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The platinum(II) organoamides [Pt(NRCH 2) 2L 2] (L = pyridine (py), R = p-HC 6F 4, C 6F 5, p-IC 6F 4, p-ClC 6F 4, p-C 6F 5C 6F 4; L = 4-methylpyridine, R = p-HC 6F 4) and [Pt(NRCH 2CH 2NR′)(py) 2] (R = P-HC 6F 4, R′ = C 6F 5, p-BrC 6F 4, or p-MeC 6F 4) inhibit the growth of murine L1210 leukemia cells in culture with ID 50 values for continuous exposure in the range 0.6-2.7 μM. Representative complexes are also active against L1210 cells in 2-h pulse exposures, as well as against the cisplatin-resistant variant L1210/DDP and human colonic carcinoma cell lines HT 29 and BE. Three complexes [Pt(NRCH 2) 2L 2] (R = p-HC 6F 4, C 6F 5, or p-IC 6F 4) have good activity (T/C ≥ 180%) against P388 leukemia in mice, and all other compounds tested are active except when R = p-C 6F 5C 6F 4, L = py. Although the molecular basis of the biological activity of these complexes is not known, the observation of good activity for amineplatinum(II) compounds with no hydrogen substitutents on the nitrogen donor atoms introduces a new factor in the anticancer behavior of platinum(II) complexes.

Original languageEnglish
Pages (from-to)3349-3353
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number18
Publication statusPublished - 1992

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