Syntheses and evaluation of some mannich bases derived from acetophenones against P388 lymphocytic leukemia and toxicological assessment of 3-dimethyl-amino-2-dimethylaminomethyl-1-(4-methoxyphenyl)-1-propanone dihydrochloride in rats.

A number of analogues of 3-dimethylamino-2-dimethylaminomethyl-1-(4-methoxyphenyl)-1-propanone dihydrochloride (IIa) and related compounds which showed activity against P388 lymphocytic leukemia were prepared, and of the 16 analogues, three met the criterion for activity in this screen. The toxicity of IIa was examined in rats and either a single dose of 25 mg/kg or nine daily doses of 12.5 mg/kg administered by the intraperitoneal route produced marked irritation and damage to the tissue with which it came into contact. Compound IIa did not show significant activity against eight other tumor systems.