Cytostatic effect of homo-aza-steroidal esters in vivo and in vitro. Structure-activity relationships.
The p-[N,N-bis (2-chloroethyl)amino]phenylacetate esters of 3 beta-hydroxy-N-methyl-17 alpha-aza-D-homo-5 alpha-androstan-17-one and 3 beta-hydroxy-17 alpha-aza-D-homo-5 alpha-androstane have been prepared and their antitumor activity evaluated against L1210 leukemia, P388 leukemia, Ehrlich ascites tumor (EAT) and Lewis Lung Carcinoma (LLC). The results are compared with those of the p-[N,N-bis (2-chloroethyl)amino]phenylacetate of 3 beta-hydroxy-17 alpha-aza-D-homo- 5 alpha-androstan-17-one. The above compounds were also tested in vitro against L1210, P 388, EAT and BHX cell cultures. All compounds were found to be active and their structure-activity relationship is discussed.
Catsoulacos
P
P
University of Patras, School of Health Sciences, Greece.
Camoutsis
C
C
Papageorgiou
A
A
Adamiak-Margariti
E
E
D000731:Androstanes / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D001378:Azasteroids / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D007939:Leukemia L1210 / Q000188:drug therapy*; D007941:Leukemia P388 / Q000188:drug therapy*; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000731:Androstanes; D000970:Antineoplastic Agents; D001378:Azasteroids; D009588:Nitrogen Mustard Compounds; C077967:3-hydroxy-17-aza-D-homoandrostan-4-N,N-bis(2-chloroethyl)aminophenylacetate; C077969:3-hydroxy-N-methyl-17-aza-D-homoandrostan-17-one-4-N,N-bis(2-chloroethyl)aminophenylacetate; C017888:NSC 290205