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

Sang-Bum Lee; Young In Park; Mi-Sook Dong; Young-Dae Gong

doi:10.1016/j.bmcl.2010.07.088

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

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5900-4. doi: 10.1016/j.bmcl.2010.07.088. Epub 2010 Jul 29.

Authors

Sang-Bum Lee¹, Young In Park, Mi-Sook Dong, Young-Dae Gong

Affiliation

¹ Graduate School of Biotechnology, Korea University, Seoul 136701, Republic of Korea.

PMID: 20729080
DOI: 10.1016/j.bmcl.2010.07.088

Abstract

We screened 1434 small heterocyclic molecules and identified thirteen 2,3,6-trisubstituted quinoxaline derivatives that were able to inhibit the Wnt/β-catenin signal pathway and cell proliferation. In the screen, some of the hit compounds such as the ethylene group-coupled quinoxaline derivatives were shown to hold promise for use as potential small-molecule inhibitors of the Wnt/β-catenin signal pathway in non-small-cell lung cancer cell lines.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Antineoplastic Agents / therapeutic use
Carcinoma, Non-Small-Cell Lung / drug therapy*
Carcinoma, Non-Small-Cell Lung / genetics
Carcinoma, Non-Small-Cell Lung / metabolism
Cell Line, Tumor
Humans
Lung Neoplasms / drug therapy*
Lung Neoplasms / genetics
Lung Neoplasms / metabolism
Quinoxalines / chemical synthesis
Quinoxalines / chemistry*
Quinoxalines / therapeutic use
Signal Transduction / drug effects*
Wnt Proteins / antagonists & inhibitors
Wnt Proteins / metabolism*
beta Catenin / antagonists & inhibitors
beta Catenin / metabolism*

Substances

Antineoplastic Agents
Quinoxalines
Wnt Proteins
beta Catenin