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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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Detalles Bibliográficos
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
Descripción
Sumario: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.