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...
Main Authors: | , , , , , |
---|---|
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 |
id |
doaj-da7a4e8d1fbb4168867a0ee7cf3df5cc |
---|---|
record_format |
Article |
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 |
work_keys_str_mv |
AT nazartrotsko synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives AT agataprzekora synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives AT justynazalewska synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives AT grazynaginalska synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives AT agatapaneth synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives AT monikawujec synthesisandinvitroantiproliferativeandantibacterialactivityofnewthiazolidine24dionederivatives |
_version_ |
1724985837787021312 |