含异吲哚酮的吡啶并[2,3-d]嘧啶衍生物的合成及生物活性研究

doi:10.6023/cjoc202510010

研究论文

含异吲哚酮的吡啶并[2,3-d]嘧啶衍生物的合成及生物活性研究

曹瑞霞^*,a, 贾玉萍^b, 张文婷^a, 谭淑文^a, 徐亚馨^a, 焦善善^a, 李笑笑^a, 赵俊宏^*,c

^a齐鲁师范学院化学与化工学院济南 250200
^b山东省药学科学院济南 250101
^c河南省科学院化学研究所有限公司郑州 450002

收稿日期:2025-10-16 修回日期:2025-11-26
基金资助:
齐鲁师范学院青年博士支持计划(No QBJH19-0038); 国家自然科学基金面上项目(82372242); 山东省科技型中小企业创新能力提升工程项目(2023TSGC0921)

Synthesis and Biological Activity of Novel Pyrido[2,3-d]pyrimidin Containing Isoindolin-1-One

Cao Ruixia^*,a, Jia Yuping^b, Zhang Wenting^a, Tan Shuwen^a, Xu Yaxin^a, Jiao Shanshan^a, Li Xiaoxiao^a, Zhao Junhong^*,c

^aCollege of Chemistry and Chemical Engineering, Qilu Normal University, Jinan, 250200
^bShandong Academy of pharmaceutical Sciences, Jinan, 250101
^cInstitute of Chemistry Co. Ltd, Henan Academy of science, Zhengzhou, 450002

Received:2025-10-16 Revised:2025-11-26
Contact: *E-mail: crx0510@163.com; zhaopassion@126.com
Supported by:
Young Doctor Support Program of Qilu Normal University (No.QBJH19-0038). National Natural Science Foundation of China (82372242); Shandong Province Science and Technology-based Small and Medium-sized Enterprises Innovation Capacity Enhancement Project (2023TSGC0921)

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摘要/Abstract

为了寻找结构新颖,活性较强的抗肿瘤化合物,设计并合成了一系列新型的含异吲哚酮的吡啶并[2,3-d]嘧啶衍生物,并用核磁共振波谱(NMR)和高分辨质谱(HRMS)等方法对化合物结构进行表征。采用噻唑兰(MTT)法测定目标化合物对肿瘤细胞(MCF-7)的抑制活性。结果显示,7c、7d、7i和7l具有较强的抑制活性,其中化合物7i的抑制活性最强,IC₅₀为15.85 μmol/L, 优于阳性对照药帕博西尼.

关键词: 帕博西尼, 乳腺癌, 抗肿瘤

In order to find novel strucuture anti-tumor drugs, a series of novel pyrido[2,3-d]pyrimidin derivatives containing Isoindolin-1-one were synthesized and evaluated for their inhibitory activities against human breast cancer cells(MCF-7), by using MTT assay. These chemical structures were well characterized by NMR and HRMS spectroscopic methods. Compounds 7c, 7d, 7i and 7l had better inhibitory activity against MCF-7 cells than Palbociclib, compound 7i showed the most potent inhibitory activity against MCF-7 cells with the IC₅₀ values of 15.85 μmol/L.

Key words: Palbociclib, human breast cancer, Anticancer

引用此文

曹瑞霞, 贾玉萍, 张文婷, 谭淑文, 徐亚馨, 焦善善, 李笑笑, 赵俊宏. 含异吲哚酮的吡啶并[2,3-d]嘧啶衍生物的合成及生物活性研究[J]. 有机化学, doi: 10.6023/cjoc202510010.

Cao Ruixia, Jia Yuping, Zhang Wenting, Tan Shuwen, Xu Yaxin, Jiao Shanshan, Li Xiaoxiao, Zhao Junhong. Synthesis and Biological Activity of Novel Pyrido[2,3-d]pyrimidin Containing Isoindolin-1-One[J]. Chinese Journal of Organic Chemistry, doi: 10.6023/cjoc202510010.

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