Structure and activity relationships of platinum complexes with anti-tumour activity

• Published in: Chemico-biological interactions Vol. 11; no. 3; p. 145
• Main Authors: Braddock, P D, Connors, T A, Jones, M, Khokhar, A R, Melzack, D H, Tobe, M L
• Format: Journal Article
• Language: English
• Published: Ireland 01-09-1975
• Subjects: Animals; Cisplatin - chemical synthesis; Cisplatin - therapeutic use; Female; Isomerism; Lethal Dose 50; Mice; Mice, Inbred BALB C; Neoplasms, Experimental - drug therapy; Plasmacytoma - drug therapy; Solubility; Stereoisomerism; Structure-Activity Relationship
• ISSN: 0009-2797
• DOI: 10.1016/0009-2797(75)90095-2

A number of complexes of platinum(II) and platinum(IV) have been prepared, characterised and tested for their ability to cause regression of a mouse plasma cell tumour. All active compounds possess two cis amine ligands but the oxidation state of the platinum is not critical. Relatively minor structural and substituent changes in the amine can lead to major and dramatic changes in the therapeutic index, generally, but not necessarily, associated with changes in toxicity. Some preliminary results on the relationship between structure and solubility are also reported.