Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety

We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase I inhibitory activity. Compounds 19, 20, 26–28, and 47–50 especially showed stronger topo II inhibitory activity than etoposide.

2,4,6-Triaryl pyridine derivatives with chlorophenyl and phenolic moeity at 2,- and 4- position of the central pyridine were synthesized and evaluated their antitumor activities.Figure optionsDownload as PowerPoint slideHighlights
► Forty-two 2,4,6-triaryl pyridines, containing chlorophenyl and phenol, were synthesized.
► Prepared compounds were evaluated for topo I and II inhibitory activity, and cytotoxicity.
► Most compounds showed better topo II inhibitory activity compared to topo I inhibitory activity.
► Several compounds have shown stronger topo II inhibitory activity than etoposide.