Design, Synthesis, and Preliminary Antitumor Activity Evaluation of Novel Alkaloid Derivatives-Reference-Cited by-同舟云学术

Design, Synthesis, and Preliminary Antitumor Activity Evaluation of Novel Alkaloid Derivatives

Published:2020-02 Issue:2 Volume:15 Page:1934578X2090353
ISSN:1934-578X
Container-title:Natural Product Communications
language:en
Short-container-title:Natural Product Communications

Author:

Wang Li-Jiao¹²,Cao Zhi-Xing¹,Guo Li¹^ORCID

Affiliation:

1. The Ministry of Education Key Laboratory of Standardization of Chinese Herbal Medicine, Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province-Key Laboratory Breeding Base of Co-founded by Sichuan Province and MOST, Pharmacy College, Chengdu University of Traditional Chinese Medicine, China

2. School of Food and Bioengineering, Xihua University, Chengdu, China

Abstract

A novel alkaloid scaffold was designed through scaffold-hopping strategy based on the active pyrazines alkaloid isolated previously. A total of 25 derivatives were synthesized based on this scaffold and evaluated for their antitumor activities. Among all these tested compounds, 9f exhibited most excellent antitumor activities toward H460 cells, TMD-8 cells, and MV4-11 cells in vitro by 3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2 H-tetrazolium bromide assay with IC50 values of 29.8, 14.9, and 18.8 μM, respectively.

Funder

Open Research Subject of Key Laboratory of Food Biotechnology of Sichuan province of China

Chun-Hui Project from Ministry of Education of China

Center of Comprehensive Health Management

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

Link

http://journals.sagepub.com/doi/pdf/10.1177/1934578X20903534

Reference9 articles.

1. Diterpenoid Alkaloids from the Lateral Root of Aconitum carmichaelii

2. Isolation and structural characterization of an immunostimulating polysaccharide from fuzi, Aconitum carmichaeli

3. Two New C20-Diterpenoid Alkaloids from Aconitum carmichaelii

4. Two new pyrazines from the parent roots of Aconitum carmichaelii