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利用微波、超声和机械化学技术合成抗癌吡唑衍生物的最新进展。

Recent advances in the synthesis of anticancer pyrazole derivatives using microwave, ultrasound, and mechanochemical techniques.

作者信息

Becerra Diana, Castillo Juan-Carlos

机构信息

Escuela de Ciencias Químicas, Universidad Pedagógica y Tecnológica de Colombia Avenida Central del Norte 39-115 Tunja Colombia

出版信息

RSC Adv. 2025 Mar 4;15(9):7018-7038. doi: 10.1039/d4ra08866b. eCollection 2025 Feb 26.

Abstract

Pyrazole and its derivatives have attracted considerable attention in pharmaceutical and medicinal chemistry, as reflected in their presence in numerous FDA-approved drugs and clinical candidates. This review presents a comprehensive analysis of articles published between 2014 and 2024, focusing on the microwave-, ultrasound-, and mechanochemical-assisted synthesis of pyrazole derivatives with anticancer activity. It explores synthetic methodologies, anticancer efficacy, and molecular docking studies, underscoring the significance of pyrazole derivatives in drug discovery and medicinal chemistry. Notably, microwave irradiation stands out as the most widely employed technique, providing high efficiency by significantly reducing reaction times while maintaining moderate temperatures. Ultrasound irradiation serves as a valuable alternative, particularly for processes that require milder conditions, whereas mechanochemical activation, though less frequently employed, offers distinct advantages in terms of sustainability.

摘要

吡唑及其衍生物在药物化学和医药化学领域引起了广泛关注,这体现在众多已获美国食品药品监督管理局(FDA)批准的药物和临床候选药物中。本综述对2014年至2024年间发表的文章进行了全面分析,重点关注微波、超声和机械化学辅助合成具有抗癌活性的吡唑衍生物。它探讨了合成方法、抗癌功效和分子对接研究,强调了吡唑衍生物在药物发现和医药化学中的重要性。值得注意的是,微波辐射是应用最广泛的技术,通过显著缩短反应时间并保持适度温度来提供高效率。超声辐射是一种有价值的替代方法,尤其适用于需要更温和条件的过程,而机械化学活化虽然使用频率较低,但在可持续性方面具有明显优势。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b246/11878059/0e2a037d51d8/d4ra08866b-f1.jpg

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