Structure and activity relationships of platinum complexes with anti-tumour activity. |
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Authors: | P D Braddock T A Connors M Jones A R Khokhar D H Melzack M L Tobe |
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Affiliation: | 1. William Ramsay and Ralph Forster Laboratories, University College, Gower Street, London, WC1 UK;2. The Chester Beatty Research Institute, Institute of Cancer Research; Royal Cancer Hospital, Fulham Road, London, SW3 6JB Great Britain |
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Abstract: | 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. |
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Keywords: | DMSO dimethylsulphoxide TI therapeutic index |
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