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

Author:

Kong Yuanfang1,Liu Shuanglin123,Wang Shaopei123,Xu Jindan123,Hu Yulong123,Jiang Shiqing1,Dong Chunhong123ORCID

Affiliation:

1. Henan University of Chinese Medicine Zhengzhou 450046 P. R. China

2. Henan Polysaccharide Research Center Zhengzhou 450046 P. R. China

3. Henan Key Laboratory of Chinese Medicine for Polysaccharides and Drugs Research Zhengzhou 450046 P. R. China

Abstract

AbstractA series of C10‐position imidazole‐modified catalpol derivatives are specifically designed and synthesized for serving as potential pancreatic cancer inhibitors, which are characterized by 1H NMR, 13C 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.

Funder

Henan Provincial Science and Technology Research Project

Publisher

Wiley

Subject

General Chemistry,Biochemistry,Organic Chemistry

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3