Cargando…

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

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Szumilak, Marta, Galdyszynska, Malgorzata, Dominska, Kamila, Bak-Sypien, Irena I., Merecz-Sadowska, Anna, Stanczak, Andrzej, Karwowski, Boleslaw T., Piastowska-Ciesielska, Agnieszka W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6153941/
https://www.ncbi.nlm.nih.gov/pubmed/28498338
http://dx.doi.org/10.3390/molecules22050794
_version_ 1783357597746724864
author Szumilak, Marta
Galdyszynska, Malgorzata
Dominska, Kamila
Bak-Sypien, Irena I.
Merecz-Sadowska, Anna
Stanczak, Andrzej
Karwowski, Boleslaw T.
Piastowska-Ciesielska, Agnieszka W.
author_facet Szumilak, Marta
Galdyszynska, Malgorzata
Dominska, Kamila
Bak-Sypien, Irena I.
Merecz-Sadowska, Anna
Stanczak, Andrzej
Karwowski, Boleslaw T.
Piastowska-Ciesielska, Agnieszka W.
author_sort Szumilak, Marta
collection PubMed
description 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.
format Online
Article
Text
id pubmed-6153941
institution National Center for Biotechnology Information
language English
publishDate 2017
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-61539412018-11-13 Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems Szumilak, Marta Galdyszynska, Malgorzata Dominska, Kamila Bak-Sypien, Irena I. Merecz-Sadowska, Anna Stanczak, Andrzej Karwowski, Boleslaw T. Piastowska-Ciesielska, Agnieszka W. Molecules Article 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. MDPI 2017-05-12 /pmc/articles/PMC6153941/ /pubmed/28498338 http://dx.doi.org/10.3390/molecules22050794 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Szumilak, Marta
Galdyszynska, Malgorzata
Dominska, Kamila
Bak-Sypien, Irena I.
Merecz-Sadowska, Anna
Stanczak, Andrzej
Karwowski, Boleslaw T.
Piastowska-Ciesielska, Agnieszka W.
Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title_full Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title_fullStr Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title_full_unstemmed Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title_short Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
title_sort synthesis, biological activity and preliminary in silico admet screening of polyamine conjugates with bicyclic systems
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6153941/
https://www.ncbi.nlm.nih.gov/pubmed/28498338
http://dx.doi.org/10.3390/molecules22050794
work_keys_str_mv AT szumilakmarta synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT galdyszynskamalgorzata synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT dominskakamila synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT baksypienirenai synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT mereczsadowskaanna synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT stanczakandrzej synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT karwowskiboleslawt synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems
AT piastowskaciesielskaagnieszkaw synthesisbiologicalactivityandpreliminaryinsilicoadmetscreeningofpolyamineconjugateswithbicyclicsystems