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Phenylethynyl-substituted Heterocycles Inhibit Cyclin D1 and Induce the Expression of Cyclin-dependent Kinase Inhibitor p21Wif1/Cip1 in Colorectal Cancer Cells

Abstract

Fluorinated, phenylethynyl-substituted heterocycles that possessed either an N-methylamino or N,N-dimethylamino group attached to heterocycles including pyridines, indoles, 1H-indazoles, quinolines, and isoquinolines inhibited the proliferation of LS174T colon cancer cells in which the inhibition of cyclin D1 and induction of the cyclin-dependent kinase inhibitor-1 (i.e., p21Wif1/Cip1) served as a readout for antineoplastic activity at a cellular level. On a molecular level, these agents, particularly 4-((2,6-difluorophenyl)ethynyl)-N-methylisoquinolin-1-amine and 4-((2,6-difluorophenyl)ethynyl)-N,N-dimethylisoquinolin-1-amine, bound and inhibited the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A).

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Publication details

The article was received on 31 Jul 2017, accepted on 30 Oct 2017 and first published on 03 Nov 2017


Article type: Research Article
DOI: 10.1039/C7MD00393E
Citation: Med. Chem. Commun., 2017, Accepted Manuscript
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    Phenylethynyl-substituted Heterocycles Inhibit Cyclin D1 and Induce the Expression of Cyclin-dependent Kinase Inhibitor p21Wif1/Cip1 in Colorectal Cancer Cells

    V. M. Sviripa, L. Kril, W. Zhang, Y. Xie, P. Wyrebek, L. Ponomareva, X. Liu, Y. Yuan, C. Zhang, D. Watt and C. Liu, Med. Chem. Commun., 2017, Accepted Manuscript , DOI: 10.1039/C7MD00393E

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