Next Article in Journal
The Impact of Halloysite on the Thermo-Mechanical Properties of Polymer Composites
Next Article in Special Issue
Microwave-Assisted Facile Synthesis, Anticancer Evaluation and Docking Study of N-((5-(Substituted methylene amino)-1,3,4-thiadiazol-2-yl)methyl) Benzamide Derivatives
Previous Article in Journal
Antidiabetic Effects of Tea
Previous Article in Special Issue
Evaluation of Tanshinone IIA Developmental Toxicity in Zebrafish Embryos
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(5), 829; doi:10.3390/molecules22050829

Microwave-Assisted Synthesis of Imidazo[4,5-f][1,10]phenanthroline Derivatives as Apoptosis Inducers in Chemotherapy by Stabilizing Bcl-2 G-quadruplex DNA

1
The First Affiliation Hospital, Guangdong Pharmaceutical University, Guangzhou 510006, China
2
School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China
3
Department of Chemistry, Jinan University, Guangzhou 510006, China
4
Department of Laboratory Medicine, Shanghai Children’s Medical Center, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China
5
School of Nursing, Guangdong Pharmaceutical University, Guangzhou 510006, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Julio A. Seijas Vázquez
Received: 23 March 2017 / Revised: 11 May 2017 / Accepted: 14 May 2017 / Published: 20 May 2017
(This article belongs to the Special Issue ECSOC-20)
View Full-Text   |   Download PDF [2350 KB, uploaded 20 May 2017]   |  

Abstract

Herein, a series of imidazo[4,5-f][1,10] phenanthroline derivatives RPIP (PIP = imidazo [4,5-f][1,10] phenanthroline, R = NO2, 1; CF3, 2; Cl, 3; OH, 4) have been synthesized in yields of 82.3–94.7% at 100 °C under the irradiation of microwave. MTT assay has been utilized to evaluate the inhibitory activity (IC50) of these compounds against the growth of various tumor cells, and the results revealed that these compounds, especially 1, exhibited excellent inhibitory activity against the growth of A549 cells with IC50 of 15.03 μM. Moreover, it’s also confirmed that 1 can penetrate into the membrane of tumor cells and distribute in mitochondria when observed under microscopy, resulting apoptosis of tumor cells. The further studies showed that 1 can bind to bcl-2 G-quadruplex DNA, which demonstrated by the increase of melting point of bcl-2 G4 DNA in the presence of 1, as well as electronic titration and emission spectra. In a word, this kind of compound may develop as a potential apoptosis inducer in cancer chemotherapy via binding and stabilizing to the bcl-2 G-quadruplex DNA. View Full-Text
Keywords: microwave-assisted synthesis; imidazo[4,5-f][1,10]phenanthroline derivatives; apoptosis inducers; bcl-2 G-quadruplex DNA microwave-assisted synthesis; imidazo[4,5-f][1,10]phenanthroline derivatives; apoptosis inducers; bcl-2 G-quadruplex DNA
Figures

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).

Supplementary material

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

Li, L.; Cao, J.-Q.; Liu, H.-M.; Wu, Q.; Pan, Q.-H.; Zeng, Z.-P.; Lan, Y.-T.; Li, Y.-M.; Mei, W.-J.; Wang, X.-C.; Zheng, W.-J. Microwave-Assisted Synthesis of Imidazo[4,5-f][1,10]phenanthroline Derivatives as Apoptosis Inducers in Chemotherapy by Stabilizing Bcl-2 G-quadruplex DNA. Molecules 2017, 22, 829.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

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