Journal of Medicinal Chemistry p. 1250 - 1256 (1986)
Update date:2022-08-02
Topics:
Sosnovsky, George
Lukszo, Jan
Rao, N. Uma Maheswara
Linear and cyclic polyether derivatives 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) are synthesized and evaluated for their antineoplastic activity against the murine lymphocytic leukemia P388.All compounds, except for 7d, were active ranging from 42percent to 287percent increase in life span (percent ILS).All CD2F1 male mice treated with the most active compound (7a) at 90 mg/kg per day for 9 days were alive after 30 days, whereas all mice treated with the clinical drug thio-TEPA were dead.The percent ILS for compound 7a on day 60 was 525.A correlation is presented between the structural features of compounds and their lipophilicities and antineoplastic activities.
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