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三唑类化合物在抗癌药物研发中的结构修饰策略。

Structural modification strategies of triazoles in anticancer drug development.

机构信息

School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China.

出版信息

Eur J Med Chem. 2024 Sep 5;275:116578. doi: 10.1016/j.ejmech.2024.116578. Epub 2024 Jun 13.

Abstract

The triazole functional group plays a pivotal role in the composition of biomolecules with potent anticancer activities, including numerous clinically approved drugs. The strategic utilization of the triazole fragment in the rational modification of lead compounds has demonstrated its ability to improve anticancer activities, enhance selectivity, optimize pharmacokinetic properties, and overcome resistance. There has been significant interest in triazole-containing hybrids in recent years due to their remarkable anticancer potential. However, previous reviews on triazoles in cancer treatment have failed to provide tailored design strategies specific to these compounds. Herein, we present an overview of design strategies encompassing a structure-modification approach for incorporating triazoles into hybrid molecules. This review offers valuable references and briefly introduces the synthesis of triazole derivatives, thereby paving the way for further research and advancements in the field of effective and targeted anticancer therapies.

摘要

三氮唑官能团在具有强大抗癌活性的生物分子组成中起着关键作用,包括许多临床批准的药物。在先导化合物的合理修饰中,三氮唑片段的战略性利用已经证明了它能够提高抗癌活性、增强选择性、优化药代动力学性质和克服耐药性。近年来,含三氮唑的杂合物因其显著的抗癌潜力而受到极大关注。然而,之前关于三唑类化合物在癌症治疗中的综述未能提供针对这些化合物的特定设计策略。在此,我们介绍了一种将三唑引入杂合物中的结构修饰方法的设计策略概述。本综述提供了有价值的参考文献,并简要介绍了三唑衍生物的合成,为有效和靶向抗癌疗法领域的进一步研究和进展铺平了道路。

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