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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...

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Autores principales: Alsayari, Abdulrhman, Asiri, Yahya I., Muhsinah, Abdullatif Bin, Hassan, Mohd. Zaheen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi 2021
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.
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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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