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Aryl azoles based scaffolds for disrupting tumor microenvironment
dc.contributor.author | Pla López, Alberto | |
dc.contributor.author | Martinez-Colomina, Paula | |
dc.contributor.author | Cañada-García, Laura | |
dc.contributor.author | Fuertes-Monge, Laura | |
dc.contributor.author | Orellana-Palacios, Jose C. | |
dc.contributor.author | Valderrama-Martínez, Alejandro | |
dc.contributor.author | Pérez Sosa, Marikena | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Falomir, Eva | |
dc.date.accessioned | 2023-12-15T08:53:08Z | |
dc.date.available | 2023-12-15T08:53:08Z | |
dc.date.issued | 2023-11-15 | |
dc.identifier.citation | A. Pla-López, P. Martínez-Colomina, L. Cañada-García, L. Fuertes-Monge, J. C. Orellana-Palacios, A. Valderrama-Martínez, M. Pérez-Sosa, M. Carda, E. Falomir E. Aryl azoles based scaffolds for disrupting tumor microenvironment. Bioorg Med Chem. 2023; 95:117490. https://doi.org/10.1016/j.bmc.2023.117490 | ca_CA |
dc.identifier.issn | 0968-0896 | |
dc.identifier.uri | http://hdl.handle.net/10234/205194 | |
dc.description.abstract | Thirty-nine aryl azoles, thirteen triazoles and twenty-seven tetrazoles, have been synthetized and biologically evaluated to determine their activity as tumor microenvironment disruptors. Antiproliferative studies have been performed on tumor cell lines HT-29, A-549 and MCF-7 and on non-tumor cell line HEK-293. It has been studied in HT-29 the expression levels of biological targets which are involved in tumor microenvironment processes, such as PD-L1, CD-47, c-Myc and VEGFR-2. In addition, antiproliferative activity was evaluated when HT-29 were co-cultured with THP-1 monocytes and the secretion levels of IL-6 were also determined in these co-cultures. The angiogenesis effect of some selected compounds on HMEC-1 was also evaluated as well as their action against vasculogenic mimicry on HEK-293. Compounds bearing an amino group in the phenyl ring and a halogen atom in the benzyl ring showed promising results as tumor microenvironment disrupting agents. The most outstanding compound decrease dramatically the population of HT-29 cells when co-cultured with THP-1 monocytes and the levels of IL-6 secreted, as well as it showed moderate effects over PD-L1, CD-47 and c-Myc. | ca_CA |
dc.description.sponsorShip | Funding for open access charge: CRUE-Universitat Jaume I | |
dc.format.extent | 14 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | Elsevier | ca_CA |
dc.relation.isPartOf | Bioorganic & Medicinal Chemistry, 2023, vol. 95 | ca_CA |
dc.rights.uri | http://creativecommons.org/licenses/by-nc/4.0/ | ca_CA |
dc.subject | triazole | ca_CA |
dc.subject | tetrazole | ca_CA |
dc.subject | PD-L1 | ca_CA |
dc.subject | VEGFR-2 | ca_CA |
dc.subject | c-Myc | ca_CA |
dc.subject | CD-47 | ca_CA |
dc.subject | IL-6 | ca_CA |
dc.subject | tumor microenvironment | ca_CA |
dc.subject | antiproliferative activity | ca_CA |
dc.subject | angiogenesis | ca_CA |
dc.title | Aryl azoles based scaffolds for disrupting tumor microenvironment | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | https://doi.org/10.1016/j.bmc.2023.117490 | |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | ca_CA |
dc.relation.publisherVersion | https://www.sciencedirect.com/science/article/pii/S0968089623003383?casa_token=j1XlLf85WzMAAAAA:hxPIB9PKD4gOOyz5k68nE4A_tp6baO-4DiayAu_pzJgDTXqLbfWEHeRngM3T2UkMapRsw4sNHA | ca_CA |
dc.description.sponsorship | This work was supported by the Grant PID2021-126277OB-100 funded by MCIN/AEI/ https://doi.org/10.13039/501100011033 and by “ERDF A way of making Europe” and by Universitat Jaume I (project UJI-B2021-46). A.P-L. appreciates the FPI contract from Generalitat Valenciana (ACIF/2020/341). P.M–C. thanks Universitat Jaume I for the Juan Murga Clausell in memoriam fellowship (UJI-2022). | |
dc.type.version | info:eu-repo/semantics/publishedVersion | ca_CA |
project.funder.identifier | https://doi.org/10.13039/501100011033 | ca_CA |
project.funder.name | Ministerio de Ciencia e Innovación | ca_CA |
project.funder.name | Universitat Jaume I | ca_CA |
project.funder.name | Generalitat Valenciana | ca_CA |
oaire.awardNumber | MCIN/PEICTI2021-2023/PID2021-126277OB-100 | ca_CA |
oaire.awardNumber | UJI-B2021-46 | ca_CA |
oaire.awardNumber | ACIF/2020/341 | ca_CA |
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