In the Search for New Anticancer Drugs. 17. Linear and Cyclic Polyether Analogues of N,N:N,'N':N'',N''-Tri-1,2-ethanediylphosphoric Triamide and N,N:N',N':N'',N''-Tri-1,2-ethanediylphosphorothioic Triamide

Article abstract of DOI:10.1021/jm00157a023

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.