In vitro antiproliferative effect of β-phenylethylamine derivatives and doxorubicin combinations on MCF/ADR cell lines

A series of 3,4-dimethoxyphenylethylamine derivatives was prepared from Baylis–Hillman (BH) adducts. The effect of these compounds on the proliferation of breast cancer cell lines (MCF-7) and the corresponding Doxorubicin (Dox) resistant cell lines (MCF-7/ADR) was studied. Aminoalcohols 1a – d were obtained from the Michael addition reaction of 3,4-dimethoxyphenylethylamine and BH adducts. For the preparation of unsaturated amines 2a – d , BH adducts were converted into allylic bromides by treatment with HBr in acidic solution. N -nucleophile introduction could be controlled by the choice of solvent furnishing the corresponding amines 2a – d . A third class of amines ( 3a – c ) was prepared by hydrogenation reaction of amines 2a – d . In respect of the biological evaluation, some of the synthesized compounds exhibited moderate inhibitory effect on the cell growth. In addition, in MCF-7/ADR cell lines, the antiproliferative effect of Dox shifted from 5 to 88 % when co-administrated with compound 2b .