Wang Chao, Shi Lingyu, Yang Shanbo, Chang Jing, Liu Wenjing, Zeng Jun, Meng Jingsen, Zhang Renshuai, Xing Dongming
Cancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, China.
School of Basic Medicine, Qingdao University, Qingdao, China.
Front Chem. 2023 Mar 1;11:1096666. doi: 10.3389/fchem.2023.1096666. eCollection 2023.
Cancer threatens human health and life. Therefore, it is particularly important to develop safe and effective antitumor drugs. Microtubules, the main component of cytoskeleton, play an important role in maintaining cell morphology, mitosis, and signal transduction, which are one of important targets of antitumor drug research and development. Colchicine binding site inhibitors have dual effects of inhibiting proliferation and destroying blood vessels. In recent years, a series of inhibitors targeting this target have been studied and some progress has been made. XRP44X has a novel structure and overcomes some disadvantages of traditional inhibitors. It is also a multifunctional molecule that regulates not only the function of tubulin but also a variety of biological pathways. Therefore, the structure, synthesis, structure-activity relationship, and biological activity of XRP44X analogues reported in recent years were summarized in this paper, to provide a useful reference for the rational design of efficient colchicine binding site inhibitors.
癌症威胁着人类的健康和生命。因此，开发安全有效的抗肿瘤药物尤为重要。微管作为细胞骨架的主要成分，在维持细胞形态、有丝分裂和信号转导中发挥着重要作用，是抗肿瘤药物研发的重要靶点之一。秋水仙碱结合位点抑制剂具有抑制增殖和破坏血管的双重作用。近年来，针对这一靶点的一系列抑制剂已被研究并取得了一些进展。XRP44X具有新颖的结构，克服了传统抑制剂的一些缺点。它也是一种多功能分子，不仅调节微管蛋白的功能，还调节多种生物途径。因此，本文总结了近年来报道的XRP44X类似物的结构、合成、构效关系及生物活性，为高效秋水仙碱结合位点抑制剂的合理设计提供有益参考。
