Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-γ

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This article reports the synthesis and related biological activity of novel dihydropyrimidones.

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4 p.

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Bharathkumar, Hanumantharayappa; Paricharak, Shardul; Dinesh, K. R.; Siveen, Kodappully Sivaraman; Fuchs, Julian E.; Rangappa, Shobith et al. September 2, 2014.

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This article reports the synthesis and related biological activity of novel dihydropyrimidones.

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4 p.

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Abstract: Hepatocellular carcinoma, a fatal liver cancer, affects 600 000 people annually and ranks third in cancer-related lethality. In this work we report the synthesis and related biological activity of novel dihydropyrimidones. Among the tested compounds, 5-acetyl-4-(1Hindol-3-yl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one (4g) was found to bemost active towards the HepG2 cell line (IC50¼ 17.9 mM), being at the same time 7.6-fold selective over normal (LO2) liver cells (IC50 ¼ 136.9 mM). Subsequently, we identified peroxisome proliferator-activated receptor g as a target of compound 4g using an in silico approach, and confirmed this mode-of-action experimentally.

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  • RSC Advances, 2014. London, UK: Royal Society of Chemistry

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  • Publication Title: RSC Advances
  • Volume: 4
  • Pages: 1-4
  • Peer Reviewed: Yes

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UNT Scholarly Works

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  • August 15, 2014

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  • September 2, 2014

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  • September 2, 2014

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  • Aug. 29, 2017, 9:38 a.m.

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Bharathkumar, Hanumantharayappa; Paricharak, Shardul; Dinesh, K. R.; Siveen, Kodappully Sivaraman; Fuchs, Julian E.; Rangappa, Shobith et al. Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-γ, article, September 2, 2014; London, United Kingdom. (digital.library.unt.edu/ark:/67531/metadc990950/: accessed October 16, 2018), University of North Texas Libraries, Digital Library, digital.library.unt.edu; crediting UNT College of Arts and Sciences.