IN THE SEARCH FOR NEW ANTICANCER DRUGS .26. A COMPARISON OF ANTICANCER ACTIVITIES OF SEVERAL TEPA, THIO-TEPA, SELENO-TEPA, AND AZETIDINE ANALOGS, INCLUDING CONGENERS CONTAINING AN AMINOXYL MOIETY

A series of TEPA, Thio-TEPA, Seleno-TEPA, and azetidine analogs, inclu ding congeners containing an aminoxyl moiety, were synthesized and eva luated In vivo for anticancer activity against the murine lymphocytic leukemia P388. All aziridine derivatives were found to be active with an increase in life span ranging from 42 % to 272 %, and all azetidine analogs were rated as inactive with one marginal exception. An attemp t was made to rationalize the results on the basis of the lipophilic p roperties of the compounds. The most active compound (8) possessed the most balanced lipophilic properties, corresponding to a log P value n ear zero.