Synthesis and anti-proliferation activity of mogrol derivatives bearing quinoline and triazole moieties

[Display omitted] A series of novel derivatives based on mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening resul...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2021-06, Vol.42, p.128090-128090, Article 128090
Main Authors: Song, Jing-Ru, Li, Na, Li, Dian-Peng
Format: Article
Language:English
Subjects:
Lung cancer
Mogrol
Quinoline
Structural modification
Triazole
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] A series of novel derivatives based on mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47 μM against A549 cell, and could induce the cell apoptosis in a dose-dependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with morgol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13 μM. The research stimulated the development of potential therapeutic agent for lung cancer from the natural mogrol.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.128090