Cytostatic activity of an estradiol-linked nitrosourea in MXT mammary carcinoma and L 5222 leukemia.
Investigation of 1-(2-chloroethyl)-1-nitrosocarbamoyl-L-alanine-estradiol-17-ester (CNC-ala-17-E2) and of the unlinked single agents 1-(2-chloroethyl)-1-nitrosocarbamoyl-L-alanine (CNC-ala) and estradiol in the MXT mammary carcinoma in vivo uncovered a significant antitumor activity only for CNC-ala-17-E2 at a non-toxic dose level (growth inhibition greater than 70%). In vitro investigations using the clonogenic assay had a comparable result: Here, too, CNC-ala-17-E2 was superior to the unlinked single agents. No difference in therapeutic activity between CNC-ala-17-E2 and CNC-ala could be observed in a transplanted rat leukemia (L 5222).
Zeller
W J
WJ
Institute of Toxicology and Chemotherapy, German Cancer Research Center, Heidelberg, Fed. Rep. of Germany.
Schreiber
J
J
Petru
E
E
Eisenbrand
G
G
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001667:Binding, Competitive; D003600:Cytosol / Q000378:metabolism; D004054:Diethylstilbestrol / Q000378:metabolism; D004958:Estradiol / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D005260:Female; D007942:Leukemia, Experimental / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D051379:Mice; D008815:Mice, Inbred Strains; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000473:pathology
D000970:Antineoplastic Agents; D009588:Nitrogen Mustard Compounds; D011960:Receptors, Estrogen; D004958:Estradiol; D004054:Diethylstilbestrol; C056364:1-(2-chloroethyl)-1-nitrosocarbamoylalanine estradiol-17-ester