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E-mail: yskwak@kribb.re.krReceived June 1, 2011, Accepted August 2, 2011A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity,topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 haveshown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2':6',2''-terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better thanpositive controls. Structure-activity relationship study indicated that 2,2':6',2''-terpyridine skeleton has animportant role in displaying significant cytotoxicity against several human cancer cell lines. Key Words : Terpyridine, 2,4,6-Tripyridyl pyridine, Topoisomerase inhibition, Cytotoxicity, SAR studyIntroductionIn the past several years, our research group has beenstudying terpyridine derivatives for their topoisomeraseinhibitory activity and cytotoxicity against several humancancer cell lines for the development of novel anticanceragents. As a result, it has been reported that various ter-pyridine derivatives, as bioisosteres of α-terthiophene (potentprotein kinase C inhibitor),

bulletin of the korean chemical society

Synthesis of 2,4,6-Tripyridyl Pyridines, and Evaluation of Their Antitumor Cytotoxicity, Topoisomerase I and II Inhibitory Activity, and Structure-activity Relationship