, Volume 21, Issue 11, pp 3598-3606
Date: 25 Nov 2011

Synthesis and biological evaluation of novel pyrimidine-2(1H)-ones/thiones as potent anti-inflammatory and anticancer agents

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Abstract

Recently there has been an increased interest in the synthesis of pyrimidinone and their applications in medicinal chemistry. Pyrimidinone derivatives represent one of the active classes of the compounds possessing a wide spectrum of biological activities such as anti-tumour, anti-fungal, anti-inflammatory, anti-bacterial, etc. This study utilises chalcones as starting compounds that are obtained by Claisen-Schmidt condensation. These chalcones underwent cyclisation upon treatment with urea and thiourea in the presence of sodium hydroxide to obtain the corresponding pyrimidinones and pyrimidinethiones. The structures of the synthesized compounds were investigated by means of UV, IR, 1H NMR and Mass spectral analysis. The anti-oxidant activity of the compounds was measured by standard free radical scavenging assays (DPPH, Nitric oxide radicals). The compounds with significant anti-oxidant activity were then screened for the in vivo anti-inflammatory activity and it showed that the compounds ETT and DMT possess good activity as comparable to the standard. All the synthesized compounds were evaluated for their in vitro anti-cancer activity by MTT assay among which compounds CLU and ETU showed significant activity against HeLa and HepG2 cell lines, respectively.