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Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line
A series of [1,2]oxazolo[5,4‐e]isoindole derivatives was evaluated against HL‐60 cell line and its multidrug resistance (MDR) variant, HL‐60R, resistant to doxorubicin and to other P‐gp substrates by overexpressing the efflux pump. They displayed antiproliferative activities, with IC(50) values rang...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9540667/ https://www.ncbi.nlm.nih.gov/pubmed/35749723 http://dx.doi.org/10.1002/ddr.21962 |
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author | Labbozzetta, Manuela Barreca, Marilia Spanò, Virginia Raimondi, Maria Valeria Poma, Paola Notarbartolo, Monica Barraja, Paola Montalbano, Alessandra |
author_facet | Labbozzetta, Manuela Barreca, Marilia Spanò, Virginia Raimondi, Maria Valeria Poma, Paola Notarbartolo, Monica Barraja, Paola Montalbano, Alessandra |
author_sort | Labbozzetta, Manuela |
collection | PubMed |
description | A series of [1,2]oxazolo[5,4‐e]isoindole derivatives was evaluated against HL‐60 cell line and its multidrug resistance (MDR) variant, HL‐60R, resistant to doxorubicin and to other P‐gp substrates by overexpressing the efflux pump. They displayed antiproliferative activities, with IC(50) values ranging from 0.02 to 5.5 µM. In particular, the newly synthesized compound 4k produced synergistic effects in terms of cell growth inhibition and cell death induction either in combination with a Vinca alkaloid, Vinblastine, and a Taxane, Paclitaxel in HL‐60R cells. The study of the mechanism of action indicated that all compounds showed antimitotic activity through inhibition of tubulin polymerization. Thus, [1,2]oxazoles could represent a valuable tool to overcome MDR mechanism, confirming the potential use of this class of compounds. |
format | Online Article Text |
id | pubmed-9540667 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-95406672022-10-14 Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line Labbozzetta, Manuela Barreca, Marilia Spanò, Virginia Raimondi, Maria Valeria Poma, Paola Notarbartolo, Monica Barraja, Paola Montalbano, Alessandra Drug Dev Res Research Articles A series of [1,2]oxazolo[5,4‐e]isoindole derivatives was evaluated against HL‐60 cell line and its multidrug resistance (MDR) variant, HL‐60R, resistant to doxorubicin and to other P‐gp substrates by overexpressing the efflux pump. They displayed antiproliferative activities, with IC(50) values ranging from 0.02 to 5.5 µM. In particular, the newly synthesized compound 4k produced synergistic effects in terms of cell growth inhibition and cell death induction either in combination with a Vinca alkaloid, Vinblastine, and a Taxane, Paclitaxel in HL‐60R cells. The study of the mechanism of action indicated that all compounds showed antimitotic activity through inhibition of tubulin polymerization. Thus, [1,2]oxazoles could represent a valuable tool to overcome MDR mechanism, confirming the potential use of this class of compounds. John Wiley and Sons Inc. 2022-06-24 2022-09 /pmc/articles/PMC9540667/ /pubmed/35749723 http://dx.doi.org/10.1002/ddr.21962 Text en © 2022 The Authors. Drug Development Research published by Wiley Periodicals LLC. https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Articles Labbozzetta, Manuela Barreca, Marilia Spanò, Virginia Raimondi, Maria Valeria Poma, Paola Notarbartolo, Monica Barraja, Paola Montalbano, Alessandra Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title | Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title_full | Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title_fullStr | Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title_full_unstemmed | Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title_short | Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
title_sort | novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line |
topic | Research Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9540667/ https://www.ncbi.nlm.nih.gov/pubmed/35749723 http://dx.doi.org/10.1002/ddr.21962 |
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