[Synthesis and antitumor properties of 3'-desamino- dimethylformamidine doxorubicin].
Interaction of doxorubicin hydrochloride with dimethylformamide diethylacetal yielded hydrochloride of 3'-desamino-3'-dimethylformamidine doxorubicin (DFD). It was shown that with single intravenous administration to tumor-free mice DFD was 2.5 times less toxic than the initial doxorubicin. Antitumor activity of DFD was studied with respect to 6 transplantable murine tumors: lymphosarcoma LIO-1, sarcoma 180, lymphadenosis NK-Ly, Ehrlich carcinoma, hemocytoblastosis La and leukemia P-388. Selectivity of the DFD activity against all the above tumors was shown to be high and practically equal to that of doxorubicin. DFD had the highest inhibitory effect on development of Ehrlich carcinoma and lymphosarcoma LIO-1.
Ul'ianova
L A
LA
Tarasova
V E
VE
Shepelevtseva
N G
NG
Bychkkova
E N
EN
Povarov
L S
LS
D000578:Amidines / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D004317:Doxorubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D007928:Lethal Dose 50; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy*
D000578:Amidines; C059890:3'-desamino-3'-dimethylformamidinedoxorubicin; D004317:Doxorubicin
Sintez i protivoopukholevye svoĭstva 3'-dezamino- 3'-dimethylformamidinodoksorubitsina.