Journal of Medicinal Chemistry p. 1168 - 1173 (1983)
Update date:2022-08-03
Topics:
Shealy, Y. Fulmer
Krauth, Charles A.
Struck, Robert F.
Montgomery, John A.
Because certain (2-chloroethyl)triazenes and (2-haloethyl)nitrosoureas have high antineoplastic activity, 2-chloroethyl and 2-fluoroethyl sulfonates were prepared to try to develop additional types of 2-haloethylating agents.In this initial study, it was demonstrated that antineoplastic activity much superior to that of the prototype, 2-chloroethyl methanesulfonate, could be found among 2-chloroethyl sulfonates.Among a variety of 2-chloroethyl alkane- and arenesulfonates, several substituted methanesulfonates displayed significant activity agains P388 leukemia in mice; the chloromethanesulfonat e showed high activity (T/C = 218percent).None of the arenesulfonates were active in this test.
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