condensation products with antitumoraktivitet, erhallna by condensation of alpha aminoisopropylfenylketon, via karbonylgruppens c = o bonding.with substituted amines or hydrazines or with funktionssubstituerade

摘要

Cpds. of formula Ph-C(=NR)-C(Me)2-NH2 (I) are new (where R is NHCSNH2, NHCOOC(Me)3, NHCH2COOEt, CH(Me)CH2CH2CH(Et)2 or CH(R')CONH2; R' is H, Me, i-Pr, CH2Ph, 3-indolyl, CH2CH2SMe or CH2OH). - (I) are antitumour agents, e.g. active against Lewis carcinoma at doses of 138-229 mg/kg, adenocarcinoma 755 at 30 mg/kg, sarcoma 37 at 30-83 mg/kg and Ehrlich carcinoma at 45-138 mg/kg (i.p., mouse). - (I) is prepd. by reacting cpd. of formula (II) with cpd. of formula RNH2 in stoichiometric amts. The reaction is carried out in methanol at 17-20 deg.C. Cpd. (II) may be prepd. by alkaline decomposition of a quaternised salt of isopropyl phenyl ketone N,N-dimethylhydrazone.