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Design, synthesis and anticancer activity of novel dihydrobenzofuro[4,5-b] [1,8]naphthyridin-6-one derivatives

Title
Design, synthesis and anticancer activity of novel dihydrobenzofuro[4,5-b] [1,8]naphthyridin-6-one derivatives
Authors
Kang J.-A.Yang Z.Lee J.Y.De U.Kim T.H.Park J.Y.Lee H.J.Park Y.J.Chun P.Kim H.S.Jeong L.S.Moon H.R.
Ewha Authors
정낙신
Issue Date
2011
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 21, no. 19, pp. 5730 - 5734
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
On the basis of the chemical structures of psorospermin with a xanthone template and acronycine derivatives with an acridone template, rac-1 and rac-2 constructed on an 1,2-dihydrobenzofuro[4,5-b][1,8]naphthyridin-6(11H)-one scaffold were designed and synthesized as potential anticancer agents. Their anticancer activities were evaluated against five human cancer cell lines. Rac-2 showed similar anticancer activity to doxorubicin and rac-1 exhibited even higher anticancer activity against LNCaP (IC 50 = 0.14 μM), DU145 (IC 50 = 0.15 μM), PC3 (IC 50 = 0.30 μM) and MCF-7 (IC 50 = 0.26 μM) cancer lines than doxorubicin and rac-2. Also, rac-1 revealed very potent anticancer activity (IC 50 = 0.15 μM) against MCF-7/ADR cell (doxorubicin-resistant breast cancer cell) lines and induced G2/M phase arrest of the cell cycle in MCF-7/ADR cells. © 2011 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2011.08.016
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약학대학 > 약학과 > Journal papers
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