Next Article in Journal
Anti-Helicobacter pylori Activity of Isocoumarin Paepalantine: Morphological and Molecular Docking Analysis
Next Article in Special Issue
Targeted Magnetic Nanotheranostics of Cancer
Previous Article in Journal
11C-Labeling of Aryl Ketones as Candidate Histamine Subtype-3 Receptor PET Radioligands through Pd(0)-Mediated 11C-Carbonylative Coupling
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(5), 794; doi:10.3390/molecules22050794

Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems

1
Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
2
Department of Comparative Endocrinology, Medical University of Lodz, 7/9 Zeligowskiego Street, 90-752 Lodz, Poland
3
Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
4
Laboratory of Cell Cultures and Genomic Analysis, Medical University of Lodz, 7/9 Zeligowskiego Street, Lodz 90-752, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 20 March 2017 / Revised: 28 April 2017 / Accepted: 9 May 2017 / Published: 12 May 2017
View Full-Text   |   Download PDF [1580 KB, uploaded 12 May 2017]   |  

Abstract

Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC–3, DU–145 and MCF–7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds–DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs. View Full-Text
Keywords: polyamine conjugates; anticancer activity; DNA binding studies; in silico ADMET screening polyamine conjugates; anticancer activity; DNA binding studies; in silico ADMET screening
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).

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

Szumilak, M.; Galdyszynska, M.; Dominska, K.; Bak-Sypien, I.I.; Merecz-Sadowska, A.; Stanczak, A.; Karwowski, B.T.; Piastowska-Ciesielska, A.W. Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems. Molecules 2017, 22, 794.

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