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  • Title: Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action.
    Author: Kim K, Kim SJ, Han YT, Hong SJ, An H, Chang DJ, Kim T, Lim B, Lee J, Surh YJ, Suh YG.
    Journal: Bioorg Med Chem Lett; 2015 Nov 15; 25(22):5444-8. PubMed ID: 26392052.
    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.
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