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InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Aug 01; Vol. 22 (15), pp. 5063-6. Date of Electronic Publication: 2012 Jun 13. - Publication Year :
- 2012
-
Abstract
- A convenient and practical methodology for the synthesis of 2-aryl quinazolin-4(3H)-ones by the condensation of o-aminobenzamides with aromatic aldehydes under mild conditions using catalytic InCl(3) with good yields and high selectivities. This method has been extended for the synthesis of 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones which have potential applications in medicinal chemistry. Many of these compounds were evaluated for their anti-proliferative properties in vitro against four cancer cell lines and several compounds were found to be active. Further in vitro studies indicated that inhibition of sirtuins could be the possible mechanism of action of these molecules.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Apoptosis drug effects
Binding Sites
Catalysis
Catalytic Domain
Cell Line, Tumor
Computer Simulation
Drug Screening Assays, Antitumor
Humans
K562 Cells
Pyrimidinones chemical synthesis
Pyrimidinones toxicity
Quinazolinones chemical synthesis
Quinazolinones toxicity
Sirtuin 1 chemistry
Sirtuin 1 metabolism
Antineoplastic Agents chemical synthesis
Indium chemistry
Pyrimidinones chemistry
Quinazolinones chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22749421
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.06.003