关键词: anticancer apoptosis cytotoxicity inhibitor pyrazole

Mesh : Antineoplastic Agents / pharmacology Pyrazoles / pharmacology Cell Line Structure-Activity Relationship Tubulin

来  源:   DOI:10.3390/ijms241612724   PDF(Pubmed)

Abstract:
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.
摘要:
吡唑衍生物,作为一类杂环化合物,具有独特的化学结构,赋予它们广谱的药理活性。它们已被广泛探索用于设计有效和选择性的抗癌剂。近年来,已经合成了许多吡唑衍生物,并评估了它们对各种癌细胞系的抗癌潜力。构效关系研究表明,在吡唑环的不同位置上进行适当的取代可以显着增强抗癌功效和肿瘤选择性。值得注意的是,许多吡唑衍生物通过与包括微管蛋白在内的各种靶标相互作用而表现出多种抗癌作用机制。EGFR,CDK,BTK,和DNA。因此,本文综述了目前对吡唑衍生物的结构特征及其与不同靶标的构效关系的认识,旨在促进潜在的吡唑类抗癌药物的开发。我们关注2018年至今报道的吡唑类化合物抗癌活性的最新研究进展。
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