Branching tryptamines as a tool to tune their antiproliferative activity

Abstract

The influence of a series of tryptamine derivatives on the viability of normal (HEK293) and tumor (HepG2, Jurkat and SH-SY5Y) cells has been evaluated. All tryptamines tested were three different substitution types: C- and N-branching, and indole benzylation. All the derivations enhance the activity of compounds separately, although the effects of different substitutions were not additive. Thus, combinations of C- and N-branchings as well as C-branching and indole benzylation gave little or no increase in activity.

Keywords: Branching amines; Cyclopropylketone arylhydrazones; Cytotoxicity; MAO degradation; Rearrangement; Tryptamine derivatives.