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基于靶点的抗癌药物研发中的三唑并嘧啶。

Triazole-fused pyrimidines in target-based anticancer drug discovery.

机构信息

Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, China; State Key Laboratory of Esophageal Cancer Prevention & Treatment, Key Laboratory of Henan Province for Drug Quality and Evaluation, Institute of Drug Discovery and Development, School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, 450001, Henan Province, China.

Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, China; State Key Laboratory of Esophageal Cancer Prevention & Treatment, Key Laboratory of Henan Province for Drug Quality and Evaluation, Institute of Drug Discovery and Development, School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, 450001, Henan Province, China.

出版信息

Eur J Med Chem. 2023 Mar 5;249:115101. doi: 10.1016/j.ejmech.2023.115101. Epub 2023 Jan 11.

Abstract

In recent decades, the development of targeted drugs has featured prominently in the treatment of cancer, which is among the major causes of mortality globally. Triazole-fused pyrimidines, a widely-used class of heterocycles in medicinal chemistry, have attracted considerable interest as potential anticancer agents that target various cancer-associated targets in recent years, demonstrating them as valuable templates for discovering novel anticancer candidates. The current review concentrates on the latest advancements of triazole-pyrimidines as target-based anticancer agents, including works published between 2007 and the present (2007-2022). The structure-activity relationships (SARs) and multiple pathways are also reviewed to shed light on the development of more effective and biotargeted anticancer candidates.

摘要

近几十年来,靶向药物的发展在癌症治疗中尤为突出,癌症是全球主要死亡原因之一。三唑并嘧啶类化合物是药物化学中广泛应用的一类杂环化合物,近年来作为针对各种癌症相关靶标的潜在抗癌药物引起了相当大的关注,它们被证明是发现新型抗癌候选药物的有价值的模板。本综述重点介绍了三唑嘧啶作为基于靶标的抗癌药物的最新进展,包括 2007 年至今(2007-2022 年)发表的研究工作。还综述了结构-活性关系(SAR)和多种途径,以阐明开发更有效和生物靶向性的抗癌候选药物的方向。

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