Further studies on the antineoplastic activity of homo-aza-steroidal esters.
The modified steroidal alkylating agents, 17 beta-hydroxy-3-aza-A-homo-4 alpha-androsten-4- one(p-[bis(2-chloroethyl)amino]phenyl)butyrate(1),3 alpha-hydroxy- 13,17-seco-5 alpha- butyrate(2),3 beta-hydroxy-13,17-seco-5-androsten-17-oic- 13,17-lactam(p-[bis-(2-chloroethyl)amino]phenyl)butyrate(3) and and (p-[bis(2-chloroethyl)amino]phenyl)butyric acid(4) have been tested against L1210, P388, Ehrlich ascites tumors (EAT), Lewis lung (LL) carcinoma and adenocarcinoma CA-755. Of four compounds evaluated in L1210 leukemia, none displayed antileukemic activity. Almost all of the four compounds were more or less active against P388 leukemia. Compound 2 possesses a slight antitumor activity in EAT, while only compound 1 appears to be active in LL carcinoma. The antitumor activity of the three modified steroidal esters on adenocarcinoma CA-755 seems to be interesting.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D001378:Azasteroids / Q000627:therapeutic use*; D002699:Chlorambucil / Q000031:analogs & derivatives* / Q000627:therapeutic use; D005260:Female; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D013260:Steroids, Heterocyclic / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D001378:Azasteroids; D013260:Steroids, Heterocyclic; C051251:3-hydroxy-13,17-seco-5-androsten-17-oic-13,17-lactam (4-(bis(2-chloroethyl)amino)phenyl)butyrate; D002699:Chlorambucil; C051250:3-hydroxy-13,17-secoandrostan-17-oic-13,17-lactam (4-(bis(2-chloroethyl)amino)phenyl)butyrate; C051249:17-hydroxy-3-aza-A-homo-4-androsten-4-one (4-(bis(2-chloroethyl)amino)phenyl)butyrate