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A series of novel hybrid compounds between aza-brazilin and imidazole have been prepared from 3-(3,4-dimethoxyphenyl)propanoic acid. Their structures were confirmed by 1 H NMR, 13 C NMR, HR-ESI-MS and X-ray crystallographic analysis. These compounds have been evaluated in vitro against a panel of human tumor cell lines. 2-Methyl-3-(naphthalen-2-ylmethyl)-1-(2-oxo-2-(4,9,10-trimethoxy-6,6a,7,11b-tetrahydro-5H-indeno[2,1-c]quinolin-5-yl)ethyl)-1H-benzo[d]imidazol-3-ium bromide (26) was found todoi:10.6023/cjoc201412055 fatcat:pdlllknpynejfflrdrqnaqvrie