Abstract
An extended series of substituted 1-phenylaziridines has been prepared and the activity as inhibitors of the transplanted Walker carcinoma 256 has been examined. Highest tumour-growth inhibitory activity is shown by the 2,4-dinitrophenyl derivatives and one of these, 5-aziridino-2,4-dinitrobenzamide (CB 1954), has exhibited outstanding selectivity of action. In a series of N-substituted derivatives of this carcinostatic amide it has been demonstrated that there is a correlation between the water/lipoid partition coefficient of the compound and also between the expected sensitivity of the amide linkage towards hydrolysis on the one hand and the chemotherapeutic index in the Walker tumour assay on the other. Highest activity is shown by the more hydrophilic and the more easily hydrolysed amide derivatives. The chemical reactivity of a selection of the new compounds towards a typical nucleophile, the iodide ion, has been determined. It has been established that the presence of an effective alkylating centre in the molecule is essential for tumour-growth inhibitory activity.
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