Synthesis and in vitro anticancer activity of new 2-thioxo-oxazolidin-4-one derivatives

[Display omitted] Oxazolidinones derivatives exhibit different biological properties, including anticancer activity. This work aimed to investigate the anticancer potential of five novel 2-Thioxo-oxazolidin-4-one derivatives. Cytotoxicity assays were performed in human peripheral blood mononuclear c...

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Bibliographic Details
Published in:Pharmacological reports 2017-08, Vol.69 (4), p.633-641
Main Authors: Campos, Júlia Furtado, Pereira, Michelly Cristiny, de Sena, Wanessa Layssa Batista, de Barros Martins, Caio Gomes, de Oliveira, Jamerson Ferreira, da Cruz Amorim, Cezar Augusto, de Melo Rêgo, Moacyr Jesus Barreto, da Rocha Pitta, Marina Galdino, de Lima, Maria do Carmo Alves, da Rocha Pitta, Maira Galdino, da Rocha Pitta, Ivan
Format: Article
Language:English
Subjects:
anticancer activity
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Cell Cycle - drug effects
cell death
Cell Line, Tumor
Cell Survival - drug effects
cytotoxicity
Drug Safety and Pharmacovigilance
Humans
Imidazolidines - chemical synthesis
Imidazolidines - chemistry
Imidazolidines - pharmacology
Leukocytes, Mononuclear - drug effects
Molecular Structure
Original Article
oxazolidinone
Pharmacotherapy
Pharmacy
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Summary:[Display omitted] Oxazolidinones derivatives exhibit different biological properties, including anticancer activity. This work aimed to investigate the anticancer potential of five novel 2-Thioxo-oxazolidin-4-one derivatives. Cytotoxicity assays were performed in human peripheral blood mononuclear cells (PBMCs) from healthy individuals and seven tumor cell lines. Apoptosis detection and cell cycle were evaluated by flow cytometry and the expression of genes involved in cell death processes by Real-Time PCR. All oxazolinedione derivatives were not cytotoxic in PBMCs. NB-5 showed the best results in cancer cells, inhibiting the growth of all tumor cell lines tested. NB-4 exhibited the highest cytotoxicity in Jurkat cells (IC50=15.19μM) and NB-3 showed better anticancer effects in HL-60 (17.84μM). Only NB-4 significantly induced apoptosis in acute leukemia cells (p=0.001). All compounds caused a significant increase in expression of pro-apoptotic gene BID (p
ISSN:1734-1140
2299-5684
DOI:10.1016/j.pharep.2017.03.005