Synthesis and antitumor evaluation of 4-ethoxycarbonyl cyclophosphamide analogs

Article abstract of DOI:10.1002/jps.2600670539

4 Ethoxycarbonyl analogs of cyclophosphamide and its five-membered ring homolog were synthesized utilizing the cyclization method previously described. N,N Bis(2 chloroethyl) 4 ethoxycarbonyl 1,3,2 oxazaphospholidin 2 amine 2 oxide demonstrated activity against L 1210 lymphoid leukemia whereas N,N bis(2 chloroethyl) 4 (ethoxycarbonyl)tetrahydro 2H 1,3,2 oxazaphosphorin 2 amine 2 oxide did not. The oxazaphosphorin 2 amine was evaluated against human epidermoid carcinoma of the nasopharynx (cell culture). The results again were negative: ED₅₀=2.8x10.