title: Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
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.
authors.affiliation: 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.
authors.forename: Deepak
authors.initials: D
authors.lastname: Bhasin
authors.forename: Somsundaram N
authors.initials: SN
authors.lastname: Chettiar
authors.forename: Jonathan P
authors.initials: JP
authors.lastname: Etter
authors.forename: May
authors.initials: M
authors.lastname: Mok
authors.forename: Pui-Kai
authors.initials: PK
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D006801:Humans; D008958:Models, Molecular; D009285:Naphthoquinones / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009285:Naphthoquinones; C035342:1,4-naphthoquinone