Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 9, Pages 3066-3077Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.03.051
Keywords
Hydroxylated 2,4-diphenyl-6-aryl pyridines; Topoisomerase I and II inhibitor; Cytotoxicity; Anticancer agents
Funding
- Ministry of Education, Science and Technology [20100007620]
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A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group( s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity. (c) 2010 Elsevier Ltd. All rights reserved.
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