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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Main Authors: Nazar Trotsko, Agata Przekora, Justyna Zalewska, Grażyna Ginalska, Agata Paneth, Monika Wujec
Format: Article
Language:English
Published: Taylor & Francis Group 2018-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Online Access:http://dx.doi.org/10.1080/14756366.2017.1387543
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spelling doaj-da7a4e8d1fbb4168867a0ee7cf3df5cc2020-11-25T01:54:58ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742018-01-01331172410.1080/14756366.2017.13875431387543Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivativesNazar Trotsko0Agata Przekora1Justyna Zalewska2Grażyna Ginalska3Agata Paneth4Monika Wujec5Medical University of LublinMedical University of LublinMedical University of LublinMedical University of LublinMedical University of LublinMedical University of LublinIn 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 IC50 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 IC50 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.http://dx.doi.org/10.1080/14756366.2017.1387543Antiproliferative activityIC50thiazolidinedionesthiosemicarbazonesantibacterial activity
collection DOAJ
language English
format Article
sources DOAJ
author Nazar Trotsko
Agata Przekora
Justyna Zalewska
Grażyna Ginalska
Agata Paneth
Monika Wujec
spellingShingle Nazar Trotsko
Agata Przekora
Justyna Zalewska
Grażyna Ginalska
Agata Paneth
Monika Wujec
Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
Journal of Enzyme Inhibition and Medicinal Chemistry
Antiproliferative activity
IC50
thiazolidinediones
thiosemicarbazones
antibacterial activity
author_facet Nazar Trotsko
Agata Przekora
Justyna Zalewska
Grażyna Ginalska
Agata Paneth
Monika Wujec
author_sort Nazar Trotsko
title 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_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_sort synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
publisher Taylor & Francis Group
series Journal of Enzyme Inhibition and Medicinal Chemistry
issn 1475-6366
1475-6374
publishDate 2018-01-01
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 IC50 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 IC50 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.
topic Antiproliferative activity
IC50
thiazolidinediones
thiosemicarbazones
antibacterial activity
url http://dx.doi.org/10.1080/14756366.2017.1387543
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