科研成果详情

题名Design, synthesis and biological evaluation of indoline-maleimide conjugates as potential antitumor agents for the treatment of colorectal cancer
作者
发表日期2024-06-15
发表期刊Bioorganic and Medicinal Chemistry   影响因子和分区
语种英语
原始文献类型Article
关键词AKT/GSK-3β Antitumor Colorectal cancer Efficient synthesis Indoline-maleimide conjugates
其他关键词INHIBITORS ; PATHWAY ; BREAST
摘要An efficient protocol for direct coupling of maleimides and indolines at the C7-position was achieved under Rh(III) catalysis. Thirty four novel indoline-maleimide conjugates were prepared in good to excellent yields using this method. All compounds were evaluated for their anti-proliferative effect against colorectal cell lines. Among them, compound 3ab showed the most potent anti-proliferative activity against the CRC cells, and displayed low toxicity in the normal cell. Further investigation indicated that 3ab could effectively suppress the proliferation and migration of CRC cells, along with inducing cell cycle arrest and apoptosis. Mechanistic studies revealed that compound 3ab inhibited the proliferation of CRC cells via suppressing the AKT/GSK-3β pathway. In vivo evaluation demonstrated remarkable antitumor effect of 3ab (10 mg/kg) in the HCT116 xenograft model with no obvious toxicity, which is superior to that of 5-Fluorouracil (20 mg/kg). Therefore, conjugate 3ab could be considered as a potential CRC therapy agent for further development.
资助项目National Natural Science Foundation of China[22077096];Natural Science Foundation of Zhejiang Province[LY23B020006];Wenzhou Municipal Science & Technology Bureau[Y20220128]
出版者Elsevier Ltd
ISSN0968-0896
EISSN1464-3391
卷号108
DOI10.1016/j.bmc.2024.117786
页数14
WOS类目Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS记录号WOS:001257481000001
收录类别SCOPUS ; PUBMED ; SCIE
URL查看原文
PubMed ID38843656
SCOPUSEID2-s2.0-85195071049
通讯作者地址[Wu, Jianmin]Institute of Genomic Medicine,Wenzhou Medical University,Zhejiang,Wenzhou,325035,China
Scopus学科分类Biochemistry;Molecular Medicine;Molecular Biology;Pharmaceutical Science;Drug Discovery;Clinical Biochemistry;Organic Chemistry
引用统计
文献类型期刊论文
条目标识符https://kms.wmu.edu.cn/handle/3ETUA0LF/214957
专题附属第一医院
检验医学院(生命科学学院、生物学实验教学中心)
药学院(分析测试中心)
基因组医学研究院
通讯作者Wu, Jianmin; Song, Zengqiang; Zhan, Lingling
作者单位
1.Department of Laboratory Medicine,The First Affiliated Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,325035,China;
2.School of Pharmaceutical Sciences,Wenzhou Medical University,Zhejiang,Wenzhou,325035,China;
3.Institute of Genomic Medicine,Wenzhou Medical University,Zhejiang,Wenzhou,325035,China;
4.School of Laboratory Medicine and Life Sciences,Wenzhou Medical University,Zhejiang,Wenzhou,325035,China
第一作者单位药学院(分析测试中心)
通讯作者单位基因组医学研究院
第一作者的第一单位药学院(分析测试中心)
推荐引用方式
GB/T 7714
Tang, Jielin,Zhang, Yuxin,Zhou, Lingling,et al. Design, synthesis and biological evaluation of indoline-maleimide conjugates as potential antitumor agents for the treatment of colorectal cancer[J]. Bioorganic and Medicinal Chemistry,2024,108.
APA Tang, Jielin., Zhang, Yuxin., Zhou, Lingling., Song, Xiangrui., Wei, Yusi., ... & Zhan, Lingling. (2024). Design, synthesis and biological evaluation of indoline-maleimide conjugates as potential antitumor agents for the treatment of colorectal cancer. Bioorganic and Medicinal Chemistry, 108.
MLA Tang, Jielin,et al."Design, synthesis and biological evaluation of indoline-maleimide conjugates as potential antitumor agents for the treatment of colorectal cancer".Bioorganic and Medicinal Chemistry 108(2024).

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