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


Vol. 32,  No. 10, pp. 3566-3570, Oct.  2011
10.5012/bkcs.2011.32.10.3566


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  Abstract

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.

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  Cite this article

[IEEE Style]

B. Jeong, H. Choi, Y. Kwak, null, E. Lee, "Synthesis of 2,4,6-Tripyridyl Pyridines, and Evaluation of Their Antitumor Cytotoxicity, Topoisomerase I and II Inhibitory Activity, and Structure-activity Relationship," Bulletin of the Korean Chemical Society, vol. 32, no. 10, pp. 3566-3570, 2011. DOI: 10.5012/bkcs.2011.32.10.3566.

[ACM Style]

Byeong-Seon Jeong, Hoyoung Choi, Young-Shin Kwak, null, and Eung-Seok Lee. 2011. Synthesis of 2,4,6-Tripyridyl Pyridines, and Evaluation of Their Antitumor Cytotoxicity, Topoisomerase I and II Inhibitory Activity, and Structure-activity Relationship. Bulletin of the Korean Chemical Society, 32, 10, (2011), 3566-3570. DOI: 10.5012/bkcs.2011.32.10.3566.