Synthesis, antitumor,activity, and structure-activity relationship study of trihydroxylated 2,4,6-triphenyl pyridines as potent and selective topoisomerase II inhibitors

Title
Synthesis, antitumor,activity, and structure-activity relationship study of trihydroxylated 2,4,6-triphenyl pyridines as potent and selective topoisomerase II inhibitors
Author(s)
이응석라다깔끼박찬미[박찬미]전규연[전규연]지준구[지준구]이준호[이준호]프리텀다빠권영주[권영주]타라만카다얏
Keywords
DNA TOPOISOMERASES; CANCER-CHEMOTHERAPY; DERIVATIVES; ALPHA; CYTOTOXICITY; POISONS; MECHANISMS; EXPRESSION; CLEAVAGE; GENES
Issue Date
201409
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.84, pp.555 - 565
Abstract
A series of eighteen trihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of each phenyl rings attached to the central pyridine. They were evaluated for topoisomerase I and II inhibitory activity, and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Most of the compounds exhibited strong and selective topoisomerase II inhibitory activity compared to the positive control, etoposide, and also displayed significant cytotoxicity in low micromolar range. Trihydroxylated 2,4,6-triphenyl pyridines were more potent than mono- and di-hydroxylated 2,4,6-triphenyl pyridines, which have been previously studied in our research group. Positive correlation between topoisomerase II inhibitory activity and cytotoxicity was observed for the most compounds. Molecular docking study shows qualitatively consistent with the results of biological assays. (c) 2014 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/30883http://dx.doi.org/10.1016/j.ejmech.2014.07.058
ISSN
0223-5234
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약학대학 > 약학부 > Articles
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