Evaluation of in vitro toxicity of N,N-dimethyl-2-propen-1-amines isomers

The trypanocidal activities of cis-3-(4'-bromo[1,1'-biphenyl]-4-yl)-3-(phen yl)-N,N-dimethyl-2-propen-1-amine (Vb) and cis-3-(4'-bromo[1,1'-biphenyl]-4 -yl)-3-(4-bromophenyl)-N,N-dimethyl-2-propen-1-anine (Vg) appeared 6.3 and 3.5 fold more active than the trans-isomers, respectively Multi-endpoints f or toxicity were also applied. Neutral red uptake (NRU), tetrazolium salt r eduction (MTT), DNA content on V79 fibroblast cell culture and acute toxici ty von E. coli were measured. The IC50 through DNA contents was lower for t he cis-isomers in both series of compounds 5b: 7.8 mu M and 5g: 5.2 mu M). NRU values for derivative 5b in isomeric mixture shows the same value as th e isolated isomers however, in the case of 5g a more significant toxicity o f the cis-isomer was found. MTT values show that 5g is more toxic than 5b. In both cases, the acute toxicity of the trans-isomers was higher than that of the cis-isomers.