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Discovery of 3,4,6-Triaryl-2-pyridones as Potential Anticancer Agents that Promote ROS-Independent Mitochondrial-Mediated Apoptosis in Human Breast Carcinoma Cells

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dc.contributor.author Ansari, M I
dc.contributor.author Arun, Ashutosh
dc.contributor.author Hussain, M K
dc.contributor.author Konwar, Rituraj
dc.contributor.author Hajela, K
dc.date.accessioned 2017-04-18T11:05:17Z
dc.date.available 2017-04-18T11:05:17Z
dc.date.issued 2016
dc.identifier.citation ChemistrySelect, 2016, 1, 4255 – 4264 en
dc.identifier.uri http://hdl.handle.net/123456789/1666
dc.description.abstract A library of 3,4,6-triaryl-2-pyridones has been synthesized using multicomponent reaction (MCR) of substituted acetophenones, benzaldehydes and phenyl acetamides. All the synthesized compounds were evaluated for their anti-breast cancer activity, in vitro in ER+ and ER- cancer cell lines, wherein, compounds (4-(3,4-dimethoxyphenyl)-6-(4-methoxyphenyl)-3-phenylpyridin-2(1H)–one) (11) and (3,6-bis(4-methoxyphenyl)-4-(4-(2-(piperidin-1-yl)ethoxy)phenyl)pyridin-2(1H)-one) (35) were found to be the most active with best safety profile towards non-cancer originated HEK-293 cells. Cell cycle analysis showed that the compounds 11 and 35 induced statistically significant arrest of cells in G1 phase and reduction in S-phase cells in a dose-dependent manner. Compound 11, unlike compound 35 exerts breast cancer cell membrane specific action as observed with LDH assay, whereas compound 35 induced ROS-independent mitochondrial-mediated apoptosis in breast cancer cell line, MDA-MB-231. Apoptotic activity of compound 35 was also confirmed by DNA fragmentation and by expression of pro-apoptotic genes, BAD, BAK, and BimL. Compound 35 is about five times safer than its effective IC50 values in MDA-MB-231 cell line, which makes it a non-toxic breast cancer therapeutic agent. en
dc.format.extent 1287729 bytes
dc.format.mimetype application/pdf
dc.language.iso en en
dc.relation.ispartofseries CSIR-CDRI Communication no.is 9312. en
dc.subject Apoptosis en
dc.subject Breast Cancer en
dc.subject DNA Fragmentation en
dc.subject Reactive oxygen species en
dc.subject 3,4,6-Triaryl-2-pyridones en
dc.title Discovery of 3,4,6-Triaryl-2-pyridones as Potential Anticancer Agents that Promote ROS-Independent Mitochondrial-Mediated Apoptosis in Human Breast Carcinoma Cells en
dc.type Article en


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