Abstract
Some bifunctional alkylating agents having groups reactive to both myeloid and lymphatic tissue have been prepared in an attempt to produce a truly “radiomimetic” compound with respect to its effect on the blood cells. 4-bromobutyl methanesulphonate, a compound possessing a therapeutic index on the Walker carcinoma three times as great as that of the clinically active 1,4-dimethanesulphonoxybutane (busulphan), satisfied this criterion. In most cases the anti-tumour activity of the compounds was greater than the corresponding derivatives in which the two alkylating functions were the same. Structure-activity relationships, using the rate of reaction with nucleophiles and the ether-water partition coefficients as parameters, are discussed.
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