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Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

In our present research, we synthesised new thiazolidine-2,4-diones (12–28). All the newly synthesised compounds were evaluated for antiproliferative and antibacterial activity. Antiproliferative evaluation was carried out using normal human skin fibroblasts and tumour cell lines: A549, HepG2, and M...

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Autores principales: Trotsko, Nazar, Przekora, Agata, Zalewska, Justyna, Ginalska, Grażyna, Paneth, Agata, Wujec, Monika
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010082/
https://www.ncbi.nlm.nih.gov/pubmed/29098896
http://dx.doi.org/10.1080/14756366.2017.1387543
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author Trotsko, Nazar
Przekora, Agata
Zalewska, Justyna
Ginalska, Grażyna
Paneth, Agata
Wujec, Monika
author_facet Trotsko, Nazar
Przekora, Agata
Zalewska, Justyna
Ginalska, Grażyna
Paneth, Agata
Wujec, Monika
author_sort Trotsko, Nazar
collection PubMed
description In our present research, we synthesised new thiazolidine-2,4-diones (12–28). All the newly synthesised compounds were evaluated for antiproliferative and antibacterial activity. Antiproliferative evaluation was carried out using normal human skin fibroblasts and tumour cell lines: A549, HepG2, and MCF-7. The IC(50) values were determined for tested compounds revealing antiproliferative activity. Moreover, safety index (SI) was calculated. Among all tested derivatives, the compound 18 revealed the highest antiproliferative activity against human lung, breast, and liver cancer cells. More importantly, the derivative 18 showed meaningfully lower IC(50) values when compared to the reference substance, irinotecan, and relatively high SI values. Moreover, newly synthesised compounds were screened for the bacteria growth inhibition in vitro. According to our screening results, most active compound was the derivative 18 against Gram-positive bacteria. Therefore, it may be implied that the novel compound 18 appears to be a very promising agent for anticancer treatment.
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spelling pubmed-60100822018-07-11 Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives Trotsko, Nazar Przekora, Agata Zalewska, Justyna Ginalska, Grażyna Paneth, Agata Wujec, Monika J Enzyme Inhib Med Chem Research Paper In our present research, we synthesised new thiazolidine-2,4-diones (12–28). All the newly synthesised compounds were evaluated for antiproliferative and antibacterial activity. Antiproliferative evaluation was carried out using normal human skin fibroblasts and tumour cell lines: A549, HepG2, and MCF-7. The IC(50) values were determined for tested compounds revealing antiproliferative activity. Moreover, safety index (SI) was calculated. Among all tested derivatives, the compound 18 revealed the highest antiproliferative activity against human lung, breast, and liver cancer cells. More importantly, the derivative 18 showed meaningfully lower IC(50) values when compared to the reference substance, irinotecan, and relatively high SI values. Moreover, newly synthesised compounds were screened for the bacteria growth inhibition in vitro. According to our screening results, most active compound was the derivative 18 against Gram-positive bacteria. Therefore, it may be implied that the novel compound 18 appears to be a very promising agent for anticancer treatment. Taylor & Francis 2017-11-03 /pmc/articles/PMC6010082/ /pubmed/29098896 http://dx.doi.org/10.1080/14756366.2017.1387543 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Trotsko, Nazar
Przekora, Agata
Zalewska, Justyna
Ginalska, Grażyna
Paneth, Agata
Wujec, Monika
Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title_full Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title_fullStr Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title_full_unstemmed Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title_short Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
title_sort synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010082/
https://www.ncbi.nlm.nih.gov/pubmed/29098896
http://dx.doi.org/10.1080/14756366.2017.1387543
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