Synthesis and biological evaluation of cytotoxic properties of stilbene-based resveratrol analogs

This work deals with the preparation of stilbene-based resveratrol analogs by employing the Perkin reaction, aiming at synthesizing potential antitumor lead compounds and evaluating their pharmacological activities. The proliferation inhibitor test against tumor cell lines identified analogs 9 and 11 as the most active among all synthesized derivatives, presenting IC50 in micromolar range for certain cell lines. For study on the embryonic development, compounds 8 and 9 at the lowest tested concentration (41.7 μM) that inhibited sea urchin egg development, but only after third cleavage were used. Both the compounds inhibited 100% of normal development since first cleavage. These data partially corroborated the results obtained with MTT assay using tumor cell lines. None of the tested compounds revealed hemolytic action in assay with mouse erythrocytes.

Graphical abstract By employing Perkin reaction, seven stilbene-based resveratrol analogs have been prepared in order to examine their in vitro activity against tumor cell lines and embryonic development of sea urchin egg.Figure optionsDownload full-size imageDownload as PowerPoint slide