The modified steroidal alkylating agents, 17β-hydroxy-3-aza-A-homo-4α-androsten-4-one{p-[bis(2-chloroethyl)amino]phenyl}butyrate(1),3α-hydroxy-13,17-seco-5α-androstan-17-oic-13,17-lactam{p-[bis(2-chloroethyl)amino]phenyl butyrate(2),3β-hydroxy-13,17-seco-5-androsten-17-oic-13,17-lactam{p-[bis-(2-chloroethyl)amino]phenyl}butyrate(3) 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.

Keywords:
Homo-aza-steroidal esters, Antitumor activity
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© 1986 S. Karger AG, Basel
1986
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