PROCESS FOR THE PREPARATION OF CHLORAMBUCIL DERIVATIVES

摘要

Anti-tumor estradiol-chlorambucil conjugates I (R=H, acyl; n=1,2) were prepd. Thus, treatment of estradiol 17-(Br-acetate) with chlorambucilAg-salt in Me2SO gave I (R=H; n=1). I (R=Bz; n=a) at 15mg/kg inhibited tumor growth in mice 98% compared to 70% inhibition using chlorambucil.