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

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.

• Authors: Sang-Bum Lee, Young In Park, Mi-Sook Dong, Young-Dae Gong
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 19 Pg. 5900-4 (Oct 01 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20729080 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Quinoxalines
• Wnt Proteins
• beta Catenin

Topics

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