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http://dx.doi.org/10.5012/bkcs.2011.32.10.3566

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

Jeong, Byeong-Seon (College of Pharmacy, Yeungnam University)
Choi, Ho-Young (College of Pharmacy, Yeungnam University)
Kwak, Young-Shin (Bio-Therapeutics Research Institute, Korea Research Institute for Bioscience and Biotechnology)
Lee, Eung-Seok (College of Pharmacy, Yeungnam University)
Publication Information
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.
Keywords
Terpyridine; 2,4,6-Tripyridyl pyridine; Topoisomerase inhibition; Cytotoxicity; SAR study;
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