Abstract
Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.
Original language | English |
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Pages (from-to) | 3201-3209 |
Number of pages | 9 |
Journal | European Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 8 |
DOIs | |
State | Published - Aug 2011 |
Bibliographical note
Funding Information:This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0001661 , 2009-0066925 , 2010-0005506 and 2010-0002646 ).
Keywords
- 4-chromanone
- Cytotoxicity
- Terpyridine
- Terthiophene
- Topoisomerase I and II