Design, Synthesis and Biological Evaluation of Novel Catalpol Derivatives as Potential Pancreatic Cancer Inhibitors

被引：1

作者：

Kong, Yuanfang ^{[1
]}

Liu, Shuanglin ^{[1
,2
,3
]}

Wang, Shaopei ^{[1
,2
,3
]}

Xu, Jindan ^{[1
,2
,3
]}

Hu, Yulong ^{[1
,2
,3
]}

Jiang, Shiqing ^{[1
]}

Dong, Chunhong ^{[1
,2
,3
]}

机构：

[1] Henan Univ Chinese Med, Zhengzhou 450046, Peoples R China

[2] Henan Polysaccharide Res Ctr, Zhengzhou 450046, Peoples R China

[3] Henan Key Lab Chinese Med Polysaccharides & Drugs, Zhengzhou 450046, Peoples R China

来源：

CHEMISTRY-AN ASIAN JOURNAL | 2023年 / 18卷 / 12期

关键词：

Anti-pancreatic cancer; Catalpol derivatives; Evaluation; Synthesis; PROLIFERATION; APOPTOSIS; CELLS;

D O I：

10.1002/asia.202300185

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of C10-position imidazole-modified catalpol derivatives are specifically designed and synthesized for serving as potential pancreatic cancer inhibitors, which are characterized by H-1 NMR, C-13 NMR and high-resolution mass spectrometry (HRMS). They were evaluated by the 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) test on two human pancreatic cancer cells PANC-1, BxPC-3 and normal pancreatic cell HPDE6-C7, which showed the significant inhibitory effected on the growth of human pancreatic cancer cells of PANC-1 and BxPC-3, especially 91.6% efficacy on BxPC-3, and 73.1% on PANC-1. Simulation studies like molecular docking supported strong binding of vascular endothelial growth factor receptor 2 (VEGFR-2) protein tyrosine kinase (PDB ID: 4AGD), a target of pancreatic cancer. A novel imidazol-modified catalpol compound 3i with strong inhibitory effect on pancreatic cancer cells, which could potentially develop into anti-pancreatic cancer drug candidates in the future.

引用

页数：10

共 35 条

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