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Synthesis, anticancer activity, toxicity evaluation and molecular docking studies of novel phenylaminopyrimidine-(thio)urea hybrids as potential kinase inhibitors.
Date
2019-02-01
Author
Ture, Asli
Kahraman, Deniz Cansen
Atalay, Rengül
Helvacioglu, Sinem
Charehsaz, Mohammad
KÜÇÜKGÜZEL, İLKAY
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Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License
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Thirty-two novel urea/thiourea compounds as potential kinase inhibitor were designed, synthesized and evaluated for their cytotoxic activity on breast (MCF7), colon (HCT116) and liver (Huh7) cancer cell lines. Compounds 10, 19 and 30 possessing anticancer activity with IC50 values of 0.9, 0.8 and 1.6 mu M respectively on Huh7 cells were selected for further studies. These hit compounds were tested against liver carcinoma panel. Real time cell electronic sensing assay was used to evaluate the effects of the compounds 10, 19 and 30 on the growth pattern of liver cancer cells. Apoptotic cell death and cell cycle analysis upon treatment of liver carcinoma cells with hit compounds were determined. A significant apoptotic cell death was detected upon treatment of Huh7 and Mahlavu cells with compound 30 after 48 h of treatment. Additionally, compound 10 caused cell cycle arrest at G0/G1 phase. Mutagenicity of hit compounds was evaluated. Assertively, these compounds were not found to be mutagenic on Salmonella typhimurium strains TA98 and TA100. To understand the binding modes of the synthesized compounds, molecular docking studies were performed using the crystal data of VEGFR and Src-kinase enzymes in correlation with anticancer activities.
Subject Keywords
Phenylaminopyrimidines
,
Ureas
,
Thioureas
,
Cancer
,
Molecular docking
,
Src-kinase
,
VEGFR
URI
https://hdl.handle.net/11511/32513
Journal
Computational biology and chemistry
DOI
https://doi.org/10.1016/j.compbiolchem.2018.12.003
Collections
Graduate School of Informatics, Article
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A. Ture, D. C. Kahraman, R. Atalay, S. Helvacioglu, M. Charehsaz, and İ. KÜÇÜKGÜZEL, “Synthesis, anticancer activity, toxicity evaluation and molecular docking studies of novel phenylaminopyrimidine-(thio)urea hybrids as potential kinase inhibitors.,”
Computational biology and chemistry
, pp. 227–241, 2019, Accessed: 00, 2020. [Online]. Available: https://hdl.handle.net/11511/32513.