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PubMed1990

Evaluation of the cytotoxicity of some Mannich bases of acetophenone against the EMT6 tumour.

1-Phenyl-3-(4-morpholinyl)propan-1-one hydrochloride 1 and the related piperidino derivative 2 were shown to have activity against the EMT6 tumour in vitro. Modification of the structures of these compounds by introducing a glucosyloxy group onto the aryl rings lowered cytotoxicity but conversion of 1 and 2 into the corresponding bis-Mannich bases increased bioactivity considerably.

Acetophenones↗
PubMed1989

[Selenazoles. XII. (1) Reaction of 4-(p-tolyl)-selenosemi-carbazides of acetic, benzoic, isonicotinic, nicotinic and picolinic acid with omega-acetophenone].

The cyclization of 4-(p-tolyl)-selenosemicarbazides of acetic, benzoic, isonicotinic, nicotinic and picolinic acids (Ia-e) with omega-bromoacetophenone was investigated in the medium of methanol (Method A) or in methanol in the presence of anhydrous sodium acetate (Method B). Acid hydrolysis of compounds IIf-i and IVa-c, e was studied. Results of UV and IR spectrometric measurements and of the in vitro microbiological studies are presented. In contradistinction to corresponding thiosemicarbazides, the change in N4 nitrogen atom basicity of the parent selenosemicarbazide I (pKa of p-toluidine = 5.1), in comparison to that of 4-phenyl-selenosemicarbazide (pKa of aniline = 4.63), proved to influence the equilibrium of the reaction with omega-bromoacetophenone only in the methanol medium without addition of anhydrous sodium acetate (Method A).

Acetates↗