Journal of Medicinal Chemistry p. 782 - 788 (1984)
Update date:2022-09-26
Topics:
Sosnovsky, George
Paul, Buddha D.
A number of N,N:N',N':N'',N''-tri-1,2-ethanediylphosphoric triamide (TEPA) and N,N:N',N':N'',N''-tri-1,2-ethanediylphosphorothioic triamide (thio-TEPA) derivatives containing either two aziridine moieties (1a) or two (2-chloroethyl)amino functions (1b) and either a 2,2,6,6-tetramethylpiperidine, 1-oxy-2,2,6,6-tetramethylpiperidine or 1-hydroxy-2,2,6,6-tetramethylpiperidine component were synthesized and tested against lymphocytic leukemia P388 in mice.In a structure-activity comparison it was found that at optimum dose all compounds containing the nitroxyl radical were more active than the corresponding hydroxylamine derivatives.The open-chain compounds (1b) were less active than the corresponding aziridine ring compounds (1a).The replacement of the X = bridge in 1a with the X = N(CH3) group resulted in lowering of the anticancer activity.
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