A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

• Published in: Journal of enzyme inhibition and medicinal chemistry Vol. 37; no. 1; pp. 9 - 38
• Main Authors: Liu, Wenjing, He, Min, Li, Yongjun, Peng, Zhiyun, Wang, Guangcheng
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 01.12.2022; Taylor & Francis Ltd; Taylor & Francis Group
• Subjects: anticancer; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antitumor activity; Binding sites; Breast cancer; Cell cycle; Cell division; Cell growth; Cell proliferation; Cell Proliferation - drug effects; Chalcones; Chalcones - chemistry; Chalcones - pharmacology; Chromosomes; Cytotoxicity; Dose-Response Relationship, Drug; Food science; Herbal medicine; Homeostasis; Humans; Laboratories; microtubule; Microtubules; Mitosis; Molecular Structure; Neoplasms - drug therapy; Neoplasms - metabolism; Neoplasms - pathology; Pharmaceutical sciences; Polymerization - drug effects; Prophase; Proteins; Review; Structure-Activity Relationship; Tubulin; Tubulin - metabolism; Tubulin Modulators - chemistry; Tubulin Modulators - pharmacology; tubulin polymerisation inhibitors; Tumors; microtubule; tubulin polymerisation inhibitors; Chalcones; anticancer
• ISSN: 1475-6366; 1475-6374; 1475-6374
• DOI: 10.1080/14756366.2021.1976772

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.