Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 9, Pages 3558-3563Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.04.038
Keywords
Transcription factors; NF-kappa B; AP-1; Translational factor; eIF-4E; Quinazolinone derivatives; Molecular modeling; Thiazole derivatives
Categories
Funding
- Feist-Weiller Cancer Center
- Industrial Commissionerate of Gujarat
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In our effort to discover and develop small molecule multi-pathway inhibitors which may be useful as tools for treating cancerous conditions, we have synthesized a small library of 2-thiazole-5-yl-3H-quinazolin-4-one derivatives. Synthesized compounds were evaluated as inhibitors of NF-kappa B and AP-1 mediated transcriptional and eIF-4E mediated translational activation as these transcription and translation factors are known to play a pivotal role in initiation and progression of cancer. The results from the study suggest the utility of the 2-thiazole-5-yl-3H-quinazolin-4-one scaffold as a promising scaffold for the design of novel multi-pathway inhibitors, which can be explored as anti-cancer agents. (C) 2010 Elsevier Masson SAS. All rights reserved.
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