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https://doi.org/10.1039/c4ra08713e
| Title: | Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-γ | Authors: | Bharathkumar, H Paricharak, S Dinesh, K.R Siveen, K.S Fuchs, J.E Rangappa, S Mohan, C.D Mohandas, N Kumar, A.P Sethi, G Bender, A Basappa, Laboratory of Chemical Biology, Department of Chemistry, Bangalore University, Palace Road, Bangalore, 560001, India Rangappa, K.S |
Keywords: | Biological evaluation In-silico In-vitro |
Issue Date: | 2014 | Citation: | Bharathkumar, H, Paricharak, S, Dinesh, K.R, Siveen, K.S, Fuchs, J.E, Rangappa, S, Mohan, C.D, Mohandas, N, Kumar, A.P, Sethi, G, Bender, A, Basappa, Laboratory of Chemical Biology, Department of Chemistry, Bangalore University, Palace Road, Bangalore, 560001, India, Rangappa, K.S (2014). Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-γ. RSC Advances 4 (85) : 45143-45146. ScholarBank@NUS Repository. https://doi.org/10.1039/c4ra08713e | Abstract: | Hepatocellular carcinoma, a fatal liver cancer, affects 600000 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-(1H-indol-3-yl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one (4g) was found to be most active towards the HepG2 cell line (IC50= 17.9 μM), being at the same time 7.6-fold selective over normal (LO2) liver cells (IC50= 136.9 μM). Subsequently, we identified peroxisome proliferator-activated receptor γ as a target of compound 4g using an in silico approach, and confirmed this mode-of-action experimentally. © 2014 the Partner Organisations. | Source Title: | RSC Advances | URI: | https://scholarbank.nus.edu.sg/handle/10635/176019 | ISSN: | 2046-2069 | DOI: | 10.1039/c4ra08713e |
| Appears in Collections: | Elements Staff Publications |
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