In the search for new anticancer drugs. 17. Linear and cyclic polyether analogs of N,N:N',N':N",N"-tri-1,2-ethanediylphosphoric triamide and N,N:N',N':N",N"-tri-1,2-ethanediylphosphorothioic triamide
- 1 July 1986
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 29 (7) , 1250-1256
- https://doi.org/10.1021/jm00157a023
Abstract
Linear and cyclic polyether derivatives of 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 42% to 287% increase in life span (% 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 % 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.This publication has 2 references indexed in Scilit:
- In the search for new anticancer drugs. 9. Synthesis and anticancer activity of spin-labeled analogs of N,N:N',N':N",N"-tris(1,2-ethanediyl)phosphoric triamide and N,N:N',N':N",N"-tris(1,2-ethanediyl)phosphorothioic triamideJournal of Medicinal Chemistry, 1984
- One-day vath (vinblastine, adriamycin, thiotepa, and halotestin) therapy for advanced breast cancer refractory to chemotherapyCancer, 1981