Next Article in Journal
4,6,8-Triarylquinoline-3-carbaldehyde Derivatives: Synthesis and Photophysical Properties
Previous Article in Journal
Crystal Structures and Antifungal Activities of Fluorine-Containing Thioureido Complexes with Nickel(II)
Article Menu

Export Article

Open AccessArticle
Molecules 2013, 18(12), 15750-15768; doi:10.3390/molecules181215750

Design, Synthesis and Evaluation of N13-Substituted Evodiamine Derivatives against Human Cancer Cell Lines

1
School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China
2
College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China
*
Authors to whom correspondence should be addressed.
Received: 23 October 2013 / Revised: 7 November 2013 / Accepted: 12 November 2013 / Published: 17 December 2013
View Full-Text   |   Download PDF [402 KB, uploaded 18 June 2014]   |  

Abstract

Attempting to improve the anticancer activity and solubility of evodiamine in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) solutions, thirty-eight N13-substituted evodiamine derivatives were designed, synthesized and tested for antitumor activities against six kinds of human cancer cell lines, namely prostate cancer (DU-145 and PC-3), lung cancer (H460), breast cancer (MCF-7), colon cancer (HCT-5) and glioblastoma (SF-268). The solubility of these compounds in SGF and SIF solutions was evaluated, and apoptosis induced by 2-2, 2-3, 2-16 and 3-2 was determined. The results showed: (1) among all compounds examined, 2-16 showed the highest antitumor activity and a broader spectrum of activity, with IC50 values ranging from 1–2 µM; (2) their solubility was obviously improved; (3) 2-3, 2-16 and 3-2 had a significant impact inducing apoptosis in some cancer cell lines. The preliminary structure-activity relationships of these derivatives were discussed. View Full-Text
Keywords: N13-substituted evodiamine derivatives; antitumor activity; apoptosis; solubility N13-substituted evodiamine derivatives; antitumor activity; apoptosis; solubility
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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

Song, S.; Chen, Z.; Li, S.; Huang, Y.; Wan, Y.; Song, H. Design, Synthesis and Evaluation of N13-Substituted Evodiamine Derivatives against Human Cancer Cell Lines. Molecules 2013, 18, 15750-15768.

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