期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 15, 页码 4662-4669出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.05.017
关键词
1,4-Naphthoquinone; Plumbagin; Juglone; LLL12.1; Menadione; STAT3
资金
- NCI NIH HHS [P30 CA016058] Funding Source: Medline
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 IC50 value of 1-3 mu M 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. (C) 2013 Published by Elsevier Ltd.
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