In vitro and in silico biological evaluation of phthalimide derivatives as antiproliferative agents
Fuente:
Redalyc
Enregistré dans:
| Auteur principal: | |
|---|---|
| Format: | Artículo científico |
| Langue: | en |
| Publié: |
Universidad Nacional Autónoma de México
2021
|
| Sujets: | |
| Accès en ligne: | |
| Tags: |
Ajouter un tag
Pas de tags, Soyez le premier à ajouter un tag!
|
| _version_ | 1876463309748699136 |
|---|---|
| author | Crystel A. Sierra-Rivera |
| author_facet | Crystel A. Sierra-Rivera |
| contents | In vitro and in silico biological evaluation of phthalimide derivatives as antiproliferative agents Crystel A. Sierra-Rivera Muhammad Kashif Lenci K. Vázquez-Jiménez Alejandro Zugasti-Cruz Alfredo Juárez-Saldivar Alma D. Paz-González Gildardo Rivera Biología phthalimide Antiproliferative molecular docking DNA methyltransferase 1 Phthalimide is considered a scaffold for the development of new anticancer agents. In this work, the antiproliferative activity of forty-three phthalimide derivatives was evaluated against cervical (HeLa), liver (HepG2), breast (4T1) cancer cell lines, and a normal cell line of murine fibroblasts (3T3). Finally, a molecular docking analysis of phthalimide derivatives on the active site of the enzymes DNA methyltransferase 1 (DNMT1) and vascular endothelial growth factor receptor 2 (VEGR2) as potential drug targets was performed. The compounds, C16, E11, and E16 showed the best antiproliferative activity against the cell lines HeLa and 4T1. Only, the compound H16 decreased 32% cell proliferation against HepG2 cell line. The compounds H5, H16, E2, E16, and C1 did not affect the proliferation of the 3T3 cell line. The molecular docking analysis showed that phthalimide derivatives have a greater affinity for DNMT1 than S-adenosyl-l-homocysteine, a potent DNMT1 inhibitor. However, molecular docking results do not correlate with their antiproliferative effects, suggesting another potential mechanism of action for the active compounds. 2021 artículo científico 1405-888X https://www.redalyc.org/articulo.oa?id=43271644010 https://www.redalyc.org/journal/432/43271644010/ https://www.redalyc.org/journal/432/43271644010/html/ https://www.redalyc.org/journal/432/43271644010/43271644010.epub https://www.redalyc.org/journal/432/43271644010/movil 10.22201/fesz.23958723e.2021.314 en http://www.redalyc.org/revista.oa?id=432 Tip Revista Especializada en Ciencias Químico-Biológicas application/pdf Universidad Nacional Autónoma de México Tip Revista Especializada en Ciencias Químico-Biológicas (México) Vol.24 |
| format | Artículo científico |
| id | redalyc_43271644010 |
| institution | Redalyc |
| language | en |
| publishDate | 2021 |
| publisher | Universidad Nacional Autónoma de México |
| spellingShingle | In vitro and in silico biological evaluation of phthalimide derivatives as antiproliferative agents Crystel A. Sierra-Rivera Biología phthalimide Antiproliferative molecular docking DNA methyltransferase 1 In vitro and in silico biological evaluation of phthalimide derivatives as antiproliferative agents Crystel A. Sierra-Rivera Muhammad Kashif Lenci K. Vázquez-Jiménez Alejandro Zugasti-Cruz Alfredo Juárez-Saldivar Alma D. Paz-González Gildardo Rivera Biología phthalimide Antiproliferative molecular docking DNA methyltransferase 1 Phthalimide is considered a scaffold for the development of new anticancer agents. In this work, the antiproliferative activity of forty-three phthalimide derivatives was evaluated against cervical (HeLa), liver (HepG2), breast (4T1) cancer cell lines, and a normal cell line of murine fibroblasts (3T3). Finally, a molecular docking analysis of phthalimide derivatives on the active site of the enzymes DNA methyltransferase 1 (DNMT1) and vascular endothelial growth factor receptor 2 (VEGR2) as potential drug targets was performed. The compounds, C16, E11, and E16 showed the best antiproliferative activity against the cell lines HeLa and 4T1. Only, the compound H16 decreased 32% cell proliferation against HepG2 cell line. The compounds H5, H16, E2, E16, and C1 did not affect the proliferation of the 3T3 cell line. The molecular docking analysis showed that phthalimide derivatives have a greater affinity for DNMT1 than S-adenosyl-l-homocysteine, a potent DNMT1 inhibitor. However, molecular docking results do not correlate with their antiproliferative effects, suggesting another potential mechanism of action for the active compounds. 2021 artículo científico 1405-888X https://www.redalyc.org/articulo.oa?id=43271644010 https://www.redalyc.org/journal/432/43271644010/ https://www.redalyc.org/journal/432/43271644010/html/ https://www.redalyc.org/journal/432/43271644010/43271644010.epub https://www.redalyc.org/journal/432/43271644010/movil 10.22201/fesz.23958723e.2021.314 en http://www.redalyc.org/revista.oa?id=432 Tip Revista Especializada en Ciencias Químico-Biológicas application/pdf Universidad Nacional Autónoma de México Tip Revista Especializada en Ciencias Químico-Biológicas (México) Vol.24 |
| title | In vitro and in silico biological evaluation of phthalimide derivatives as antiproliferative agents |
| topic | Biología phthalimide Antiproliferative molecular docking DNA methyltransferase 1 |
| url | https://www.redalyc.org/articulo.oa?id=43271644010 https://www.redalyc.org/journal/432/43271644010/ https://www.redalyc.org/journal/432/43271644010/html/ https://www.redalyc.org/journal/432/43271644010/43271644010.epub https://www.redalyc.org/journal/432/43271644010/movil |