Abstract
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-kappaB 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.
2010 Elsevier Masson SAS. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology
-
Base Sequence
-
Cell Line
-
Eukaryotic Initiation Factor-4E / metabolism*
-
Humans
-
Inhibitory Concentration 50
-
Models, Molecular
-
NF-kappa B / antagonists & inhibitors
-
NF-kappa B / chemistry
-
NF-kappa B / metabolism*
-
Neoplasms / genetics
-
Neoplasms / metabolism*
-
Protein Biosynthesis / drug effects*
-
Protein Conformation
-
Quinazolinones / chemical synthesis
-
Quinazolinones / chemistry
-
Quinazolinones / pharmacology*
-
Transcription Factor AP-1 / antagonists & inhibitors
-
Transcription Factor AP-1 / metabolism*
-
Transcription, Genetic / drug effects*
Substances
-
Antineoplastic Agents
-
Eukaryotic Initiation Factor-4E
-
NF-kappa B
-
Quinazolinones
-
Transcription Factor AP-1