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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 10
BKCSDE 32(10)
October 20, 2011 

Synthesis of 2,4,6-Tripyridyl Pyridines, and Evaluation of Their Antitumor Cytotoxicity, Topoisomerase I and II Inhibitory Activity, and Structure-activity Relationship
Byeong-Seon Jeong, Hoyoung Choi, Young-Shin Kwak,*, Eung-Seok Lee*
Terpyridine, 2,4,6-Tripyridyl pyridine, Topoisomerase inhibition, Cytotoxicity, SAR study
A 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 have shown 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 than positive controls. Structure-activity relationship study indicated that 2,2':6',2''-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.
3566 - 3570
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