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S E Northcott

Publications and source records attributed to S E Northcott.

2 recordsLinked to original sources

Solution chemistry and analytical characterization of ormaplatin.

Ormaplatin is a racemic, platinum(IV), anti-cancer drug which is currently involved in phase 1 clinical trials. Characterizing the purity of ormaplatin represents an analytical challenge for several reasons. These include the lack of solution stability of ormaplatin, its process impurities and solution decomposition products, the strong concentration and pH dependence of various decomposition pathways and solution equilibria and the absence of chromatographic reproducibility. Two independent types of aqueous decomposition pathways have been observed. The first pathway involves the generation of soluble PtIV containing species which remain in equilibrium with the parent material in solution. The second pathway involves the generation of PtII containing materials which tend to be less soluble. The most interesting material in this latter class is probably the chloride bridged mixed valence material which has been characterized structurally by X-ray diffraction. Liquid chromatography and sample handling procedures have been developed which allow for the accurate determination of bulk drug purity, as well as, an understanding of numerous reversible equilibria.

Antineoplastic Agents↗

Cytotoxicity of tetraplatin and cisplatin for human and rodent cell lines cultured as monolayers and multicellular spheroids.

The cytotoxicity of tetraplatin (dl-trans), its d- and l-isomers, and cisplatin for four human tumor cell lines (myeloma 8226, ovarian 2008, A2780, and OVCAR-3), their cisplatin-resistant variants, and three rodent cell lines (V79, EMT6/Ro, and L1210) were compared. Tetraplatin was more, or equally as, potent as cisplatin for the human cell lines and for L1210 but was clearly less potent for V79 and EMT6/Ro. The d-trans tetraplatin was more potent than the l-trans. Cisplatin resistant human tumor cells were less resistant to tetraplatin. On comparing sensitivity of V79 and EMT6/Ro cells in two growth models, we observed that all of the platinum compounds were more cytotoxic to cells in multicellular spheroids than in exponentially growing monolayers. Uptake studies, however, showed that tetraplatin was more cytotoxic to spheroids because spheroids accumulated more drug than monolayers.

Animals↗