A novel 3-arylethynyl-substituted pyrido[2,3,-b]pyrazine derivatives and pharmacophore model as Wnt2/β-catenin pathway inhibitors in non-small-cell lung cancer cell lines
ANTINEOPLASTIC ACTIVITY;
ARTICLE;
CANCER CELL CULTURE;
CELL PROLIFERATION;
CONTROLLED STUDY;
DRUG CYTOTOXICITY;
DRUG DESIGN;
DRUG STRUCTURE;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
HUMAN TISSUE;
HYDROGEN BOND;
HYDROPHOBICITY;
IC 50;
LUNG NON SMALL CELL CANCER;
SIGNAL TRANSDUCTION;
J.M. William, C.K. Jeffrey, B. Ramesh, V.N.B. Peter, S. Fukuyama, G. Krishnamurthy, L.M. Ronald, P. Keith, S. Barb, and J.T. Eugene Bioorg. Med. Chem. 18 2010 190
15 more than 20,000 small molecules by combinatorial synthetic technology. In the first stage, we selected 1434 representative compounds by virtual screening based on drug-like property considering with known Wnt pathway inhibiters
15 more than 20,000 small molecules by combinatorial synthetic technology. In the first stage, we selected 1434 representative compounds by virtual screening based on drug-like property considering with known Wnt pathway inhibiters.
Gong, Y.-D.; Jeon, M. K.; Hwang, S. H.; Dong, M. S.; Lee, S. B.; Kang, K. H.; Oh, C. H. Novel 2-Sustituted Aminoalkylenyloxy-3-Substituted Phenyl Ethynyl Quinoxaline Derivatives, Korea Pat. No. 0889389.
Gong, Y.-D.; Dong, M. S.; Hwang, S. H.; Lee, T. I.; Lee, S. B. 2-Sustituted Aminoalkylenyloxy-3-Substituted Phenylethynyl-6-Amino Quinoxaline, Korea Pat. Appl. No. 2008-0076221.
Cell proliferation assay: Cell proliferation was determined by using a CellTiter 96 non-radioactive cell proliferation assay kit according to the manufacturer's protocol (Promega, USA). The detail procedure was mentioned in biological experimental part
Cell proliferation assay: Cell proliferation was determined by using a CellTiter 96 non-radioactive cell proliferation assay kit according to the manufacturer's protocol (Promega, USA). The detail procedure was mentioned in biological experimental part.
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Korea Pat. App. No. 2006-0063214
Lee, S. J.; Gong, Y.-D.; Jeon, M. K.; Moon, S. H.; Jun, K. H.; Kim, J. M.; Lee, S. H.; Lee, H. H.; Kang, M. J. 2-Arylalkylenyloxy-3-Ethynylpyrido[2,3- b] Pyrazine Derivatives, Korea Pat. App. No. 2006-0063214.
We checked cytotoxicity of the 13 compounds in human lung fibroblast cell line (LL47) and were over 0.5-1.0 μM higher than those in A549 cells
We checked cytotoxicity of the 13 compounds in human lung fibroblast cell line (LL47) and were over 0.5-1.0 μM higher than those in A549 cells.
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In the early stage of our research, we used Calphostin C as positive control since we could not obtain other known comparison inhibitors from commercial market. And then we have synthesized and used the Pfizer lead compound (Data Monitor Research Store: preclinical stage, pyrinium pamoate) as positive control
In the early stage of our research, we used Calphostin C as positive control since we could not obtain other known comparison inhibitors from commercial market. And then we have synthesized and used the Pfizer lead compound (Data Monitor Research Store: preclinical stage, pyrinium pamoate) as positive control.
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0037468255
B.C.Y. Wong, X.H. Jiang, X.M. Fan, M.C.M. Lin, S.H. Jiang, S.K. Lam, and H.F. Kung Oncogene 22 2003 1189
T. Chalet, G.N. Rita, J.R. Anthony, P. Beata, K. Fatima, Z. Zhaobin, Z. Huanchun, T. Quincy, C.N. Ainsley, G. Paraskevi, Z. Wei, J.O. Jeffrey, M.P. Manuela, K.C. Nicolaou, and G.V.M. Erwin Cancer Res. 65 2005 605