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Design, synthesis, and structure-activity relationships of new benzofuro [3,2-b]pyridin-7-ols as DNA topoisomerase II inhibitors

Title
Design, synthesis, and structure-activity relationships of new benzofuro [3,2-b]pyridin-7-ols as DNA topoisomerase II inhibitors
Authors
Shrestha, AarajanaJo, HyunjiKwon, YoungjooLee, Eung-Seok
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2018
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN
0960-894XJCR Link

1464-3405JCR Link
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS vol. 28, no. 4, pp. 566 - 571
Keywords
Fused heterocyclesBenzofuro[3,2-b]pyridin-7-olHydroxyl-substituentTopoisomerase inhibitionAntiproliferative activityStructure-activity relationship
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Human DNA topoisomerases have become attractive targets for developing more effective anticancer drugs. In this study, a series of new benzofuro[3,2-b] pyridin-7-ols were designed and synthesized for the first time and screened for their topoisomerase I and II inhibitory and antiproliferative activity. Structure-activity relationships revealed the position of ortho-and para-hydroxyl group at 2-phenyl ring, and meta-hydroxyl group at 4-phenyl ring of benzofuro[3,2-b] pyridin-7-ol are important for potent and selective topo II inhibitory activity. Compound 11 showed the most selective and potent topo II inhibition (100% inhibition at 100 mM) and strongest antiproliferative activity (IC50 = 0.86 mu M) than all the positive controls in HeLa cell line. (C) 2018 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2018.01.048
Appears in Collections:
약학대학 > 약학과 > Journal papers
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