Identification of 2,3,6-trisubstituted quinoxaline derivatives as a Wnt2/β-catenin pathway inhibitor in non-small-cell lung cancer cell lines

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 19, 2010, Pages 5900-5904

  Lee, Sang Bum ^a   Park, Young In ^a   Dong, Mi Sook ^a   Gong, Young Dae ^b  

^a Korea University   (South Korea)

^b Dongguk University   (South Korea)

Author keywords

Anticancer agents; Drug like library; Small molecule inhibitors; Wnt protein

Indexed keywords

ANTINEOPLASTIC AGENT; BETA CATENIN; ETHYLENE; QUINOXALINE DERIVATIVE; WNT2 PROTEIN;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL CULTURE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG SCREENING; DRUG STRUCTURE; LUNG NON SMALL CELL CANCER;

ANTINEOPLASTIC AGENTS; BETA CATENIN; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; HUMANS; LUNG NEOPLASMS; QUINOXALINES; SIGNAL TRANSDUCTION; WNT PROTEINS;

EID: 77957596003     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.088     Document Type: Article

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27. 2 incubator for 30 min and the absorbance was measured on a molecular dynamic plate reader (Bio-Rad, Germany) at 490 nm.
28. 4) were transfected using the Transfast transfection reagent (Promega, USA) with 1 μg reporter construct and 15 ng pRL-TK plasmid and incubated with various concentrations of selected compounds at 37 °C. After 24 h, the cells were lysed in 50 μl passive lysis buffer (Promega, USA). Firefly luciferase and Renilla luciferase activity were determined using the Dual-Glo Luciferase Assay System (promega, USA). Results are expressed as the mean ± SEM of normalized ratios of firefly luciferase activity and renilla luciferase activity measurements for each triplicate set.
29. 4 supplemented with a complete protease inhibitor cocktail (Roche, USA). The protein content was determined using the Bradford assay (Bio-Rad, Germany). Protein samples (20-30 μg of protein) were subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis and transferred to nitrile cellulose membranes (Whatman, Germany) for western blotting. The primary antibodies used were β-catenin and GAPDH (Santa Cruz Biotechnology, Santa Cruz, USA). Immunoreactive proteins were visualized with ECL (Amersham Biosciences, USA) according to the manufacturer's protocol. The densities of the bands were quantitatively analyzed using the TINA 2.0 software (Raytest, Straubenhardt, Germany).