邵利辉,甘宜远,张丽琼,王贞超,欧阳贵平.化学通报,2019,82(9):779-788. |
6-取代喹唑啉衍生物的合成及抗肿瘤活性研究进展 |
Progress in Synthesis and Antitumor Activity of 6-Substituted Quinazoline Derivatives |
投稿时间:2019-05-29 修订日期:2019-06-24 |
DOI: |
中文关键词: 6-取代喹唑啉, 抗肿瘤活性, 合成, 酪氨酸激酶抑制剂, 作用机制 |
英文关键词:6-Substituted quinazoline, Antitumor activity, Synthesis, Tyrosine kinase inhibitor Mechanism of action |
基金项目:国家自然科学基金(21867004),药用植物功效与利用国家重点实验室(FAMP201801K),贵州省科技计划平台项目(黔科合平台人才20185781)和贵州省科技计划(黔科合基础20181051)资助。 |
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中文摘要: |
喹唑啉及其衍生物作为重要的药效团,具有广谱的抗肿瘤生物活性,一直是药物化学研究的热点。本文围绕近年来6-酰胺类、卤代类、醚类、与7位成环类、杂环类等喹唑啉衍生物的合成,及其抗肿瘤活性作用机制研究进行概述,以期为活性更高、毒性更小的新型抗肿瘤化合物的设计合成提供参考。 |
英文摘要: |
Quinazoline and its derivatives, as an important pharmacophore, have a broad spectrum of anti-tumor biological activity, and have been the focus of medicinal chemistry research. In this paper, the synthesis of quinazoline derivatives with different substituents such as amides, halogens, ethers, 7-rings, heterocyclics derivatives, as well as their anti-tumor biological activity were reviewed. It is expected to provide a reference for the design and synthesis of new anticancer compounds with higher activity and less toxicity. |
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