State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.
Teaching and Research Section of Natural Medicinal Chemistry, School of Pharmacy, Guizhou Medical University, Guiyang, China.
J Enzyme Inhib Med Chem. 2022 Dec;37(1):9-38. 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.
微管在细胞有丝分裂过程中起着重要作用，可以在细胞有丝分裂前期形成纺锤体，将染色体拉到细胞的两端，然后分裂成两个子细胞，完成有丝分裂过程。微管抑制剂通过抑制微管动力学和破坏微管内稳态来抑制细胞增殖。从而诱导细胞周期在 G2/M 期停滞，并干扰有丝分裂过程。已经发现，多种查尔酮衍生物可以与微管蛋白结合并破坏微管的动态平衡，抑制肿瘤细胞的增殖，发挥抗肿瘤作用。因此，针对微管蛋白的查尔酮衍生物进行了大量的研究。本综述描述了近年来合成或天然的查尔酮微管抑制剂及其对癌细胞活性的构效关系（SAR）。
