Antileukemic effect of homo-aza-steroidal ester of [p-[bis(2-chloroethyl)amino]phenyl]acetic acid.

The homo-aza-steroidal ester of [p-[bis(2-chloroethyl)amino]phenyl]acetic acid, 3beta-hydroxy-13alpha-amino-13,17-seco-5alpha-androstan-17-oic-13,17,-lactam p-bis(2-chloroethyl)aminophenylacetate (ASE), gives a greater than 50% increased lifespan over controls in the treatment of L1210 leukemia by the ip, sc, and oral routes of administration and a greater than 150% increased lifespan in the treatment of P388 leukemia by the ip route (the only route tested). Both a daily and a Day 1, 5, and 9 treatment schedule are essentially equally effective. In this study, ASE is compared to the parent compound phenesterin which is inactive in both of these tumor lines. To our knowledge ASE is the first steroidal alkylating agent to show activity in the L1210 leukemia.