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A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors
Microtubules play an important role in the process of cell mitosis and can form a spindle in the mitotic prophase of the cell, which can pull chromosomes to the ends of the cell and then divide into two daughter cells to complete the process of mitosis. Tubulin inhibitors suppress cell proliferation...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8667932/ https://www.ncbi.nlm.nih.gov/pubmed/34894980 http://dx.doi.org/10.1080/14756366.2021.1976772 |
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author | Liu, Wenjing He, Min Li, Yongjun Peng, Zhiyun Wang, Guangcheng |
author_facet | Liu, Wenjing He, Min Li, Yongjun Peng, Zhiyun Wang, Guangcheng |
author_sort | Liu, Wenjing |
collection | PubMed |
description | Microtubules play an important role in the process of cell mitosis and can form a spindle in the mitotic prophase of the cell, which can pull chromosomes to the ends of the cell and then divide into two daughter cells to complete the process of mitosis. Tubulin inhibitors suppress cell proliferation by inhibiting microtubule dynamics and disrupting microtubule homeostasis. Thereby inducing a cell cycle arrest at the G2/M phase and interfering with the mitotic process. It has been found that a variety of chalcone derivatives can bind to microtubule proteins and disrupt the dynamic balance of microtubules, inhibit the proliferation of tumour cells, and exert anti-tumour effects. Consequently, a great number of studies have been conducted on chalcone derivatives targeting microtubule proteins. In this review, synthetic or natural chalcone microtubule inhibitors in recent years are described, along with their structure-activity relationship (SAR) for anticancer activity. |
format | Online Article Text |
id | pubmed-8667932 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-86679322021-12-14 A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors Liu, Wenjing He, Min Li, Yongjun Peng, Zhiyun Wang, Guangcheng J Enzyme Inhib Med Chem Review Microtubules play an important role in the process of cell mitosis and can form a spindle in the mitotic prophase of the cell, which can pull chromosomes to the ends of the cell and then divide into two daughter cells to complete the process of mitosis. Tubulin inhibitors suppress cell proliferation by inhibiting microtubule dynamics and disrupting microtubule homeostasis. Thereby inducing a cell cycle arrest at the G2/M phase and interfering with the mitotic process. It has been found that a variety of chalcone derivatives can bind to microtubule proteins and disrupt the dynamic balance of microtubules, inhibit the proliferation of tumour cells, and exert anti-tumour effects. Consequently, a great number of studies have been conducted on chalcone derivatives targeting microtubule proteins. In this review, synthetic or natural chalcone microtubule inhibitors in recent years are described, along with their structure-activity relationship (SAR) for anticancer activity. Taylor & Francis 2021-12-11 /pmc/articles/PMC8667932/ /pubmed/34894980 http://dx.doi.org/10.1080/14756366.2021.1976772 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by-nc/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial License (http://creativecommons.org/licenses/by-nc/4.0/ (https://creativecommons.org/licenses/by-nc/4.0/) ), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Review Liu, Wenjing He, Min Li, Yongjun Peng, Zhiyun Wang, Guangcheng A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title | A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title_full | A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title_fullStr | A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title_full_unstemmed | A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title_short | A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
title_sort | review on synthetic chalcone derivatives as tubulin polymerisation inhibitors |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8667932/ https://www.ncbi.nlm.nih.gov/pubmed/34894980 http://dx.doi.org/10.1080/14756366.2021.1976772 |
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