Academic Journal
Synthesis of Combretastatin A-4 and 3 0 -Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression
| العنوان: | Synthesis of Combretastatin A-4 and 3 0 -Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression |
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| المؤلفون: | Agut, Raúl, Falomir, Eva, Murga, Juan, Martín Beltrán, Celia, Gil Edo, Raquel, Pla, Alberto, Carda, Miguel, Marco, J. Alberto |
| بيانات النشر: | MDPI |
| سنة النشر: | 2020 |
| المجموعة: | Repositori Universitat Jaume I (Repositorio UJI) |
| مصطلحات موضوعية: | combretastatin A-4, 30 -aminocombretastatin A-4, cytotoxicity, tubulin, microtubules, cell cycle, VEGF, hTERT, c-Myc |
| الوصف: | Natural product combretastatin A-4 (CA-4) and its nitrogenated analogue 3 0 -aminocombretastatin A-4 (AmCA-4) have shown promising antitumor activities. In this study, a range of CA-4 and AmCA-4 derivatives containing amino acid pendants have been synthesized in order to compare their biological actions with those of their parent compounds. Thus, inhibition of cell proliferation on tumor cell lines HT-29, MCF-7 and A-549, as well as on the nontumor cell line HEK-273; in vitro tubulin polymerization; mitotic cell arrest; action on the microtubule cell network and inhibition of VEGF, hTERT, and c-Myc genes have been evaluated. Some AmCA-4 derivatives bearing L-amino acids exhibited inhibition of cell proliferation at low nanomolar levels exceeding the values shown by AmCA-4. Furthermore, while CA-4 and AmCA-4 derivatives do not show significant effects on the in vitro tubulin polymerization and cell cycle arrest, some selected CA-4 and AmCA-4 derivatives are able to cause total depolymerization of the microtubule network on A-549 cells. The best results were obtained in the inhibition of gene expression, particularly on the VEGF gene, in which some AmCA-4 derivatives greatly exceeded the inhibition values achieved by the parent compound. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1420-3049 |
| Relation: | Molecules 2020, 25, 660; project CTQ2014-52949-P, project RTI2018-097345-B-I00, project UJI-B2018-38; https://www.mdpi.com/1420-3049/25/3/660; Agut, R.; Falomir, E.; Murga, J.; Martín-Beltrán, C.; Gil-Edo, R.; Pla, A.; Carda, M.; Marco, J.A. Synthesis of Combretastatin A-4 and 3′-Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression. Molecules 2020, 25, 660.; http://hdl.handle.net/10234/187517; http://dx.doi.org/10.3390/molecules25030660 |
| DOI: | 10.3390/molecules25030660 |
| الاتاحة: | http://hdl.handle.net/10234/187517 https://doi.org/10.3390/molecules25030660 |
| Rights: | © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). ; Atribución 4.0 Internacional ; http://creativecommons.org/licenses/by-sa/4.0/ ; info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.24E007DE |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 14203049 |
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| DOI: | 10.3390/molecules25030660 |