2-Haloethylating Agents for Cancer Chemoterapy. 2-Haloethyl Sulfonates

Article abstract of DOI:10.1021/jm00362a016

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.