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Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones

A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensi...

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Autores principales: Havrylyuk, Dmytro, Zimenkovsky, Borys, Vasylenko, Olexandr, Day, Craig W., Smee, Donald F., Grellier, Philippe, Lesyk, Roman
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115615/
https://www.ncbi.nlm.nih.gov/pubmed/23811085
http://dx.doi.org/10.1016/j.ejmech.2013.05.044
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author Havrylyuk, Dmytro
Zimenkovsky, Borys
Vasylenko, Olexandr
Day, Craig W.
Smee, Donald F.
Grellier, Philippe
Lesyk, Roman
author_facet Havrylyuk, Dmytro
Zimenkovsky, Borys
Vasylenko, Olexandr
Day, Craig W.
Smee, Donald F.
Grellier, Philippe
Lesyk, Roman
author_sort Havrylyuk, Dmytro
collection PubMed
description A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensitivity profile toward the leukemia subpanel cell lines with GI(50) value ranges of 2.12–4.58 μM (4d) and 1.64–3.20 μM (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2-yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Trypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses.
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spelling pubmed-71156152020-04-02 Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones Havrylyuk, Dmytro Zimenkovsky, Borys Vasylenko, Olexandr Day, Craig W. Smee, Donald F. Grellier, Philippe Lesyk, Roman Eur J Med Chem Original Article A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensitivity profile toward the leukemia subpanel cell lines with GI(50) value ranges of 2.12–4.58 μM (4d) and 1.64–3.20 μM (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2-yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Trypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses. Elsevier Masson SAS. 2013-08 2013-06-06 /pmc/articles/PMC7115615/ /pubmed/23811085 http://dx.doi.org/10.1016/j.ejmech.2013.05.044 Text en Copyright © 2013 Elsevier Masson SAS. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Original Article
Havrylyuk, Dmytro
Zimenkovsky, Borys
Vasylenko, Olexandr
Day, Craig W.
Smee, Donald F.
Grellier, Philippe
Lesyk, Roman
Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title_full Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title_fullStr Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title_full_unstemmed Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title_short Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
title_sort synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115615/
https://www.ncbi.nlm.nih.gov/pubmed/23811085
http://dx.doi.org/10.1016/j.ejmech.2013.05.044
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