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Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action

Cited 5 time in Web of Science Cited 5 time in Scopus
Authors
Kim, Kyeojin; Kim, Su-Jung; Han, Young Taek; Hong, Sung-Jun; An, Hongchan; Chang, Dong-Jo; Kim, Taewoo; Lim, Bumhee; Lee, Jeeyeon; Surh, Young-Joon; Suh, Young-Ger
Issue Date
2015-11
Citation
Bioorganic and Medicinal Chemistry Letters, Vol.25 No.22, pp.5444-5448
Keywords
STAT3Small molecule inhibitorsApoptosisAntitumorBreast cancer
Abstract
A series of novel STAT3 inhibitors consisting of Michael acceptor has been identified through assays of the focused in-house library. In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In particular, analog 6 revealed promising STAT3 inhibitory activity in HeLa cell lines. The analog also exhibited selective inhibition of STAT3 phosphorylation without affecting STAT1 phosphorylation and cytostatic effect in human breast epithelial cells (MCF10A-ras), which supports cancer cell-specific inhibitory properties. (C) 2015 Elsevier Ltd. All rights reserved.
ISSN
0960-894X
URI
https://hdl.handle.net/10371/172649
DOI
https://doi.org/10.1016/j.bmcl.2015.07.063
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Graduate School of Convergence Science and Technology (융합과학기술대학원)Dept. of Molecular and Biopharmaceutical Sciences (분자의학 및 바이오제약학과)Journal Papers (저널논문_분자의학 및 바이오제약학과)
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