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Synthesis and biological evaluation of novel GSK-3β inhibitors as anticancer agents

Title
Synthesis and biological evaluation of novel GSK-3β inhibitors as anticancer agents
Authors
Choi M.J.Oh D.W.Jang J.W.Cho Y.S.Seo S.H.Jeong K.S.Ko S.Y.Pae A.N.
Ewha Authors
고수영
SCOPUS Author ID
고수영scopus
Issue Date
2011
Journal Title
Bulletin of the Korean Chemical Society
ISSN
0253-2964JCR Link
Citation
vol. 32, no. 6, pp. 2015 - 2020
Indexed
SCI; SCIE; SCOPUS; KCI WOS scopus
Abstract
A series of isoxazol-indolin-2-one was designed for GSK-3β inhibitors as novel anticancer agents based on their binding mode analysis in GSK-3β crystal structure. Total 21 compounds were synthesized and evaluated for their inhibitory activity against two tumor cell lines (DU145 and HT29). Most of the synthesized compounds were potent with above 80% inhibitory activity at 100 μM, and several compounds were examined for inhibitory activity against GSK-3β. Among them, 15(Z) (R 1=H, R 2=3-Cl-phenyl) was most active with 78% inhibition of tumor cell line (HT29) at 20 μM and 72% inhibition of GSK-3β at 20 μM.
DOI
10.5012/bkcs.2011.32.6.2015
Appears in Collections:
자연과학대학 > 화학·나노과학전공 > Journal papers
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