Synthesis of 2-(thienyl-2-yl or-3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

Title
Synthesis of 2-(thienyl-2-yl or-3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
Author(s)
이응석프리텀다빠[프리텀다빠]라다깔끼[라다깔끼]최호영[최호영]최재훈[최재훈]윤민호[윤민호]정병선정미자[정미자]남정민[남정민]나영화[나영화]조원제[조원제]권영주[권영주]
Keywords
DNA
Issue Date
201003
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.6, pp.2245 - 2254
Abstract
A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their topoisomerase I and II inhibition and cytotoxic activity against several human cancer cell lines. Compounds 10-19 showed moderate topoisomerase I and II inhibitory activity and 20-29 showed significant topoisomerase II inhibitory activity. Structure-activity relationship study revealed that 4-(5-chlorofuran-2-yl)-2-(thiophen-3-yl) moiety has an important role in displaying topoisomerase II inhibition. (C) 2010 Elsevier Ltd. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/22767http://dx.doi.org/10.1016/j.bmc.2010.01.065
ISSN
0968-0896
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약학대학 > 약학부 > Articles
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