Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents
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Other documents of the author: Pla López, Alberto; Castillo, Raquel; Cejudo Marín, Rocío; García Pedrero, Olaya; Bakir Laso, Mariam; Falomir, Eva; Miguel Carda
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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Title
Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget AgentsAuthor (s)
Date
2022-06-24Publisher
MDPIBibliographic citation
Pla-López, A.; Castillo, R.; Cejudo-Marín, R.; García-Pedrero, O.; Bakir-Laso, M.; Falomir, E.; Carda, M. Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents. Int. J. Mol. Sci. 2022, 23, 7049. https://doi.org/10.3390/ ijms23137049Type
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Abstract
Twenty-six triazole-based derivatives were designed for targeting both PD-L1 (programmed death receptor ligand 1) and VEGFR-2 (vascular endothelial growth factor receptor 2). These compounds were synthetized and ... [+]
Twenty-six triazole-based derivatives were designed for targeting both PD-L1 (programmed death receptor ligand 1) and VEGFR-2 (vascular endothelial growth factor receptor 2). These compounds were synthetized and biologically evaluated as multitarget inhibitors of VEGFR-2, PD-L1 and c-Myc proteins. The antiproliferative activity of these molecules on several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was determined. The effects on the abovementioned biological targets were evaluated for some selected compounds. Compound 23, bearing a p-chlorophenyl group, showed better results than sorafenib in regard to the downregulation of VEGFR-2 and a similar effect to BMS-8 on both PD-L1 and c-Myc proteins. The antiangiogenic and antivascular activities of chloro derivatives were also established by endothelial microtube formation assay on Matrigel®. [-]
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Int. J. Mol. Sci. 2022, 23(13)Funder Name
Ministerio de Economía y Competitividad, España | Universitat Jaume I | Generalitat Valenciana
Project code
RTI2018-097345-B-I00 | UJI-B2018-38 | UJI-B2021-46 | GACUJI/2022/05 | ACIF/2020/341
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© 2022 by the authors.
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info:eu-repo/semantics/openAccess
info:eu-repo/semantics/openAccess
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- QUIO_Articles [694]