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, including congeners containing an aminoxyl moiety, were synthesized and evaluated 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 attempt was made to rationalize the results on the basis of the lipophilic properties of the compounds. The most active compound (8) possessed the most balanced lipophilic properties, corresponding to a log P value near zero.
Sosnovsky
G
G
Department of Chemistry, University of Wisconsin, Milwaukee 53201.
Lukszo
J
J
Konieczny
M
M
Purgstaller
K
K
Laib
F
F
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001384:Azetidines / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004354:Drug Screening Assays, Antitumor; D007941:Leukemia P388 / Q000188:drug therapy; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D016566:Organoselenium Compounds / Q000494:pharmacology; D013852:Thiotepa / Q000494:pharmacology; D013721:Triethylenephosphoramide / Q000031:analogs & derivatives* / Q000494:pharmacology
D000970:Antineoplastic Agents; D001384:Azetidines; D016566:Organoselenium Compounds; D013852:Thiotepa; D013721:Triethylenephosphoramide