Arylpyridines, arylpyrimidines and related compounds as potential modulator agents of the VEGF, hTERT and c-Myc oncogenes
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Other documents of the author: Martín Beltrán, Celia; Sanchez Peris, Maria; Conesa Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Alberto Marco, J.
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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https://doi.org/10.1016/j.bmc.2019.01.039 |
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Title
Arylpyridines, arylpyrimidines and related compounds as potential modulator agents of the VEGF, hTERT and c-Myc oncogenesAuthor (s)
Date
2019-03-01Publisher
ElsevierISSN
0968-0896; 1464-3391Bibliographic citation
MARTÍN-BELTRÁN, Celia, et al. Arylpyridines, arylpyrimidines and related compounds as potential modulator agents of the VEGF, hTERT and c-Myc oncogenes. Bioorganic & medicinal chemistry, 2019, vol. 27, no 5, p. 880-887Type
info:eu-repo/semantics/articlePublisher version
https://www.sciencedirect.com/science/article/pii/S0968089618318881Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
Twenty-four derivatives structurally related to honokiol have been synthesized and biologically evaluated. IC50 values were determined towards the HT-29, MCF-7 and HEK-293 cell lines. Some of these derivatives exhibited ... [+]
Twenty-four derivatives structurally related to honokiol have been synthesized and biologically evaluated. IC50 values were determined towards the HT-29, MCF-7 and HEK-293 cell lines. Some of these derivatives exhibited comparable or lower IC50 values than honokiol towards the HT-29 and MCF-7 cell lines or else higher selectivity indexes than the natural product. Twelve selected derivatives were evaluated for their ability to inhibit the expression of the VEGFA, hTERT and c-Myc genes and also to inhibit the production of total c-Myc protein and the secretion of the VEGF protein. One of the most promising compounds, 3-(2,4-dimethoxyphenyl)pyridine, may be a good candidate for further studies as an anticancer agent as it is able to improve the effect shown by honokiol in downregulating all gene expression and protein production at a safe concentration for non-tumor cells. [-]
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Bioorganic & medicinal chemistry, 2019, vol. 27, noInvestigation project
Ministerio de Economia y Competitividad of Spain: CTQ2014-52949-P; Conselleria dEmpresa, Universitat i Ciencia de la Generalitat Valenciana: PROMETEO/2013/027, ACOMP/2014/274; University Jaume I: PI-1B2011-37Rights
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