Anticancer activity and SAR studies of substituted 1,4-naphthoquinones

  • Bioorg Med Chem. 2013 Aug 1;21(15):4662-9. doi: 10.1016/j.bmc.2013.05.017.
Deepak Bhasin  1 ,  Somsundaram N Chettiar ,  Jonathan P Etter ,  May Mok ,  Pui-Kai Li
Affiliations
  • 1. Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Rm 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210-1291, United States.
PMID: 23791367 DOI: 10.1016/j.bmc.2013.05.017
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.