Unknown

Dataset Information

0

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 IC? value of 1-3 ?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.

SUBMITTER: Bhasin D 

PROVIDER: S-EPMC4304211 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

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

Bhasin Deepak D   Chettiar Somsundaram N SN   Etter Jonathan P JP   Mok May M   Li Pui-Kai PK  

Bioorganic & medicinal chemistry 20130518 15

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  ...[more]

Similar Datasets

Unknown Synthesis, SAR, and Docking Studies Disclose 2-Arylfuran-1,4-naphthoquinones as In Vitro Antiplasmodial Hits.
| S-EPMC5684547 | biostudies-literature
Unknown Synthesis and SAR studies of novel 6,7,8-substituted 4-substituted benzyloxyquinolin-2(1H)-one derivatives for anticancer activity.
| S-EPMC4337696 | biostudies-literature
Unknown Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25.
| S-EPMC6925601 | biostudies-literature
Unknown Synthesis, leishmanicidal activity and theoretical evaluations of a series of substituted bis-2-hydroxy-1,4-naphthoquinones.
| S-EPMC6271274 | biostudies-literature
Unknown Synthesis and Evaluation of Antimicrobial and Cytotoxic Activity of Oxathiine-Fused Quinone-Thioglucoside Conjugates of Substituted 1,4-Naphthoquinones.
| S-EPMC7463537 | biostudies-literature
Unknown Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.
| S-EPMC4755333 | biostudies-literature
Unknown Generation of Aryl Radicals from Aryl Hydrazines via Catalytic Iodine in Air: Arylation of Substituted 1,4-Naphthoquinones.
| S-EPMC7057683 | biostudies-literature
Unknown Synthesis, Cytotoxic Activity Evaluation and Quantitative Structure-Activity Analysis of Substituted 5,8-Dihydroxy-1,4-Naphthoquinones and their O- and S-Glycoside Derivatives Tested Against Neuro-2a Cancer Cells.
| S-EPMC7761386 | biostudies-literature
Unknown Anticancer activity of methyl-substituted oxaliplatin analogs.
| S-EPMC3375001 | biostudies-literature
Unknown Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones.
| S-EPMC8314044 | biostudies-literature