Phosphorus-nitrogen compounds. 24. Phosphoramide mustard carrier derivatives.
Diethylstilbestrol, psoralen, and propranolol were used as potential carrier molecules for selective concentrations of a nitrogen mustard moiety in breast, skin, and lung tissues, respectively. The propranolol derivative gave two racemic mixtures, which were tested to ascertain any differences in anticancer activity. The insertion of a P = O group between the carrier and oncolytic portions offsets the excess lipophilic contribution of the latter and possibly provides for latentiation of alkylating activity. Murine tumor testing of the phosphoramide mustard derivatives and two intermediates indicated that two compounds possessed marginal activity against mammary carcinoma and lymphocytic leukemia.
D000818:Animals; D004054:Diethylstilbestrol / Q000378:metabolism; D004304:Dosage Forms; D005363:Ficusin / Q000378:metabolism; D007942:Leukemia, Experimental / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D008958:Models, Molecular; D009588:Nitrogen Mustard Compounds / Q000008:administration & dosage*; D011433:Propranolol / Q000378:metabolism; D014961:X-Ray Diffraction
D004304:Dosage Forms; D009588:Nitrogen Mustard Compounds; D004054:Diethylstilbestrol; D011433:Propranolol; D005363:Ficusin