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Synfacts 2007(9): 0921-0921  
DOI: 10.1055/s-2007-968907
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York

The Synthesis of Trisubstituted Pyridines via Kröhnke Reaction

Contributor(s): Victor Snieckus, Jignesh J. Patel
A. Basnet, P. Thapa, R. Karki, Y. Na, Y. Jahng, B.-S. Jeong, T. C. Jeong, C.-S. Lee, E.-S. Lee*
Yeungnam University and Catholic Universtiy of Daegu, Kyongsan, Korea
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Publication History

Publication Date:
23 August 2007 (online)

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Significance

Various 2,4,6-trisubstituted pyridine derivatives have been synthesized using modified Kröhnke reaction conditions. These compounds were evaluated for their Topo I and II inhibitory activity and antitumor cytotoxicity against several human cancer cell lines and found that heterocyclic moieties are important at 2- and 4-positions on the central pyridine ring system to display these activities. There was no direct correlation between antitumor cytotoxicity and topo­isomerase inhibitory activity.