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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7355942 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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