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  • Title: Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
    Author: Bhasin D, Chettiar SN, Etter JP, Mok M, Li PK.
    Journal: Bioorg Med Chem; 2013 Aug 01; 21(15):4662-9. PubMed ID: 23791367.
    Abstract:
    In this paper, we report the structure-activity relationship studies of substituted 1,4-naphthoquinones for its anticancer properties. 1,4-Naphthoquinone, Juglone, Menadione, Plumbagin and LLL12.1 were used as lead molecules to design PD compounds. Most of the PD compounds showed improved antiproliferative activity in comparison to the lead molecule in prostate (DU-145), breast (MDA-MB-231) and colon (HT-29) cancer cell lines. PD9, PD10, PD11, PD13, PD14 and PD15 were found to be the most potent compound with an IC₀ value of 1-3 μM in all cancer cell lines. Fluorescent polarization assay was employed to study the inhibition of STAT3 dimerization by PD compounds. PD9 and PD18 were found to be potent STAT3 dimerization inhibitors.
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