School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China.
Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Hangzhou Normal University, Hangzhou 311121, China.
Int J Mol Sci. 2023 Aug 12;24(16):12724. doi: 10.3390/ijms241612724.
Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical structures that confer them with a broad spectrum of pharmacological activities. They have been extensively explored for designing potent and selective anticancer agents. In recent years, numerous pyrazole derivatives have been synthesized and evaluated for their anticancer potential against various cancer cell lines. Structure-activity relationship studies have shown that appropriate substitution on different positions of the pyrazole ring can significantly enhance anticancer efficacy and tumor selectivity. It is noteworthy that many pyrazole derivatives have demonstrated multiple mechanisms of anticancer action by interacting with various targets including tubulin, EGFR, CDK, BTK, and DNA. Therefore, this review summarizes the current understanding on the structural features of pyrazole derivatives and their structure-activity relationships with different targets, aiming to facilitate the development of potential pyrazole-based anticancer drugs. We focus on the latest research advances in anticancer activities of pyrazole compounds reported from 2018 to present.
吡唑衍生物作为一类杂环化合物,具有独特的化学结构,赋予它们广泛的药理活性。它们已被广泛探索用于设计高效和选择性的抗癌药物。近年来,已经合成了许多吡唑衍生物,并对它们对各种癌细胞系的抗癌潜力进行了评估。构效关系研究表明,在吡唑环的不同位置进行适当的取代可以显著提高抗癌疗效和肿瘤选择性。值得注意的是,许多吡唑衍生物通过与包括微管蛋白、EGFR、CDK、BTK 和 DNA 在内的各种靶标相互作用,表现出多种抗癌作用机制。因此,本综述总结了目前对吡唑衍生物结构特征及其与不同靶标的构效关系的理解,旨在促进基于吡唑的潜在抗癌药物的开发。我们重点介绍了 2018 年至今报道的吡唑化合物在抗癌活性方面的最新研究进展。