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Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition
BACKGROUND: Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead mo...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Hindawi
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8277517/ https://www.ncbi.nlm.nih.gov/pubmed/34326873 http://dx.doi.org/10.1155/2021/5691982 |
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author | Alsayari, Abdulrhman Asiri, Yahya I. Muhsinah, Abdullatif Bin Hassan, Mohd. Zaheen |
author_facet | Alsayari, Abdulrhman Asiri, Yahya I. Muhsinah, Abdullatif Bin Hassan, Mohd. Zaheen |
author_sort | Alsayari, Abdulrhman |
collection | PubMed |
description | BACKGROUND: Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. METHODS: The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. RESULTS: One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC(50) 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC(50) 0.83 μM). CONCLUSION: In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents. |
format | Online Article Text |
id | pubmed-8277517 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Hindawi |
record_format | MEDLINE/PubMed |
spelling | pubmed-82775172021-07-28 Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition Alsayari, Abdulrhman Asiri, Yahya I. Muhsinah, Abdullatif Bin Hassan, Mohd. Zaheen J Oncol Research Article BACKGROUND: Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. METHODS: The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. RESULTS: One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC(50) 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC(50) 0.83 μM). CONCLUSION: In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents. Hindawi 2021-07-05 /pmc/articles/PMC8277517/ /pubmed/34326873 http://dx.doi.org/10.1155/2021/5691982 Text en Copyright © 2021 Abdulrhman Alsayari et al. https://creativecommons.org/licenses/by/4.0/This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Alsayari, Abdulrhman Asiri, Yahya I. Muhsinah, Abdullatif Bin Hassan, Mohd. Zaheen Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title | Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title_full | Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title_fullStr | Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title_full_unstemmed | Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title_short | Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition |
title_sort | anticolon cancer properties of pyrazole derivatives acting through xanthine oxidase inhibition |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8277517/ https://www.ncbi.nlm.nih.gov/pubmed/34326873 http://dx.doi.org/10.1155/2021/5691982 |
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