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
G. Sosnovsky et al., 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, Journal of pharmaceutical sciences, 83(7), 1994, pp. 982-988
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.