1-Aryl-3-(2-chloroethyl) ureas: synthesis and in vitro assay as potential anticancer agents.
1-Aryl-3-(2-chloroethyl) ureas and 1-aryl-3-nitroso-3-(2-chloroethyl) ureas, derived from 4-phenylbutyric acid and alkylanilines, were synthesized and their cytotoxicity was evaluated on human adenocarcinoma cells in vitro. Methyl 4-[p-[3-(2-chloroethyl)ureido]-phenyl]butyrate, 4-methyl [3-(2-chloroethyl)ureido]benzene, and 4-butyl[3-(2-chloroethyl)ureido]benzene were found to be at least as cytotoxic as 4-[p-[bis-(2-chloroethyl)amino]phenyl]butyric acid (chlorambucil), while their N-nitroso derivatives were inactive.
Gaudreault
R C
RC
Department of Pharmacology, Faculty of Medicine, Université Laval, Ste-Foy, Québec, Canada.
Lacroix
J
J
Pagé
M
M
Joly
L P
LP
D000230:Adenocarcinoma / Q000188:drug therapy; D000970:Antineoplastic Agents / Q000138:chemical synthesis; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009607:Nitrosourea Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects*
D000970:Antineoplastic Agents; D009607:Nitrosourea Compounds