Dimethanesulphonate esters in receptor mapping studies. 1. Benzene 1,2-, 1,3- and 1,4-diol, dimethanol and diethanol dimethanesulphonates and anti-tumour activity.

The anti-tumour activities of nine aromatic dimethanesulphonate esters were examined. Their biological effects have been related to both their chemical reactivity and to the computer-modelled vectorial positions of the centres of alkylation of the compounds. One compound (19) has shown activity between sensitive and resistant Yoshida tumours in vivo and also shows the highest activity between these two cell lines in vitro. In its minimal energy form, this compound would require to interact with converging nucleophilic centres about 6 A apart, and it is tentatively suggested that this may be an appropriate dimension for a receptor which is required to be alkylated in order to show anti-tumour activity.