Next Article in Journal
Lectin Engineering, a Molecular Evolutionary Approach to Expanding the Lectin Utilities
Next Article in Special Issue
Novel All Trans-Retinoic Acid Derivatives: Cytotoxicity, Inhibition of Cell Cycle Progression and Induction of Apoptosis in Human Cancer Cell Lines
Previous Article in Journal
Modulation of the RNA Interference Activity Using Central Mismatched siRNAs and Acyclic Threoninol Nucleic Acids (aTNA) Units
Previous Article in Special Issue
A Survey of Marine Natural Compounds and Their Derivatives with Anti-Cancer Activity Reported in 2012
Article Menu

Export Article

Open AccessArticle
Molecules 2015, 20(5), 7620-7636; doi:10.3390/molecules20057620

5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors

1
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China
2
West China School of Pharmacy, Sichuan University, Chengdu 610041, China
3
The Second Division of Hepatobiliary Surgery, Center of PLA, Center of General Surgery of PLA, General Hospital of Chengdu Military Region, Chengdu 610083, China
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 15 January 2015 / Revised: 16 April 2015 / Accepted: 20 April 2015 / Published: 27 April 2015
View Full-Text   |   Download PDF [1297 KB, uploaded 27 April 2015]   |  

Abstract

A series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also showed good anti-viability activities against two tumor cell lines. Due to the low molecular weight and the fact that no quinoline derivative has been reported as an EZH2 inhibitor, this compound could serve as a lead compound for further optimization. View Full-Text
Keywords: histone methyltransferase; Enhancer of Zeste Homologue 2 (EZH2); quinolines; anticancer activity histone methyltransferase; Enhancer of Zeste Homologue 2 (EZH2); quinolines; anticancer activity
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Xiang, P.; Jie, H.; Zhou, Y.; Yang, B.; Wang, H.-J.; Hu, J.; Hu, J.; Yang, S.-Y.; Zhao, Y.-L. 5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors. Molecules 2015, 20, 7620-7636.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top