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Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells
Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic s...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076013/ https://www.ncbi.nlm.nih.gov/pubmed/32179835 http://dx.doi.org/10.1038/s41598-020-59059-3 |
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author | Buzharevski, Antonio Paskaš, Svetlana Sárosi, Menyhárt-Botond Laube, Markus Lönnecke, Peter Neumann, Wilma Murganić, Blagoje Mijatović, Sanja Maksimović-Ivanić, Danijelа Pietzsch, Jens Hey-Hawkins, Evamarie |
author_facet | Buzharevski, Antonio Paskaš, Svetlana Sárosi, Menyhárt-Botond Laube, Markus Lönnecke, Peter Neumann, Wilma Murganić, Blagoje Mijatović, Sanja Maksimović-Ivanić, Danijelа Pietzsch, Jens Hey-Hawkins, Evamarie |
author_sort | Buzharevski, Antonio |
collection | PubMed |
description | Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytotoxic or cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib showed different modes of action that were dependent on the cell type. |
format | Online Article Text |
id | pubmed-7076013 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
spelling | pubmed-70760132020-03-23 Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells Buzharevski, Antonio Paskaš, Svetlana Sárosi, Menyhárt-Botond Laube, Markus Lönnecke, Peter Neumann, Wilma Murganić, Blagoje Mijatović, Sanja Maksimović-Ivanić, Danijelа Pietzsch, Jens Hey-Hawkins, Evamarie Sci Rep Article Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytotoxic or cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib showed different modes of action that were dependent on the cell type. Nature Publishing Group UK 2020-03-16 /pmc/articles/PMC7076013/ /pubmed/32179835 http://dx.doi.org/10.1038/s41598-020-59059-3 Text en © The Author(s) 2020 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/. |
spellingShingle | Article Buzharevski, Antonio Paskaš, Svetlana Sárosi, Menyhárt-Botond Laube, Markus Lönnecke, Peter Neumann, Wilma Murganić, Blagoje Mijatović, Sanja Maksimović-Ivanić, Danijelа Pietzsch, Jens Hey-Hawkins, Evamarie Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title | Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title_full | Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title_fullStr | Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title_full_unstemmed | Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title_short | Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells |
title_sort | carboranyl derivatives of rofecoxib with cytostatic activity against human melanoma and colon cancer cells |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076013/ https://www.ncbi.nlm.nih.gov/pubmed/32179835 http://dx.doi.org/10.1038/s41598-020-59059-3 |
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