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Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives

Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds 1 and 7 single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytoto...

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Autores principales: Szulczyk, Daniel, Bielenica, Anna, Roszkowski, Piotr, Dobrowolski, Michał A., Olejarz, Wioletta, Napiórkowska, Mariola, Struga, Marta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355942/
https://www.ncbi.nlm.nih.gov/pubmed/32570862
http://dx.doi.org/10.3390/molecules25122816
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author Szulczyk, Daniel
Bielenica, Anna
Roszkowski, Piotr
Dobrowolski, Michał A.
Olejarz, Wioletta
Napiórkowska, Mariola
Struga, Marta
author_facet Szulczyk, Daniel
Bielenica, Anna
Roszkowski, Piotr
Dobrowolski, Michał A.
Olejarz, Wioletta
Napiórkowska, Mariola
Struga, Marta
author_sort Szulczyk, Daniel
collection PubMed
description Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds 1 and 7 single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytotoxic activity against a panel of human cancer cell lines, which is contrary to normal (HaCaT) cell lines, by using the MTT method. Studies were followed by lactate dehydrogenase assay, apoptotic activity, and interleukin-6 assay. Within the studied group, compound 6 showed the most promising results in all biological studies. The strongest influence in A549 cells was denoted for derivative 4, which inhibited interleukin release almost tenfold, as compared to the control.
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spelling pubmed-73559422020-07-22 Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives Szulczyk, Daniel Bielenica, Anna Roszkowski, Piotr Dobrowolski, Michał A. Olejarz, Wioletta Napiórkowska, Mariola Struga, Marta Molecules Article Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds 1 and 7 single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytotoxic activity against a panel of human cancer cell lines, which is contrary to normal (HaCaT) cell lines, by using the MTT method. Studies were followed by lactate dehydrogenase assay, apoptotic activity, and interleukin-6 assay. Within the studied group, compound 6 showed the most promising results in all biological studies. The strongest influence in A549 cells was denoted for derivative 4, which inhibited interleukin release almost tenfold, as compared to the control. MDPI 2020-06-18 /pmc/articles/PMC7355942/ /pubmed/32570862 http://dx.doi.org/10.3390/molecules25122816 Text en © 2020 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
Szulczyk, Daniel
Bielenica, Anna
Roszkowski, Piotr
Dobrowolski, Michał A.
Olejarz, Wioletta
Napiórkowska, Mariola
Struga, Marta
Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title_full Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title_fullStr Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title_full_unstemmed Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title_short Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives
title_sort cytotoxicity evaluation of novel bis(2-aminoethyl)amine derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355942/
https://www.ncbi.nlm.nih.gov/pubmed/32570862
http://dx.doi.org/10.3390/molecules25122816
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