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

Pharmacological Reports : PR
Júlia Furtado CamposIvan da Rocha Pitta

Abstract

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<0.05) and BECN1 (p<0.05). NB-3 significantly modulated the expression of RIPK3 (p=0.02) and DDIT3 (p=0.014), while NB-2 induced an increase of CDKN1A (p=0.03) and NB-4 induced PPARγ gene (p=0.0006). NB-5 showed antitumor effects in solid and hematopoietic cancer cells, while other derivatives p...Continue Reading

References

May 1, 1991·Journal of Medicinal Chemistry·R L DowR W Stevenson
Feb 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·D Wolf, V Rotter
Jul 14, 1998·Molecular Cell·E MuellerB M Spiegelman
Feb 19, 2002·Antimicrobial Agents and Chemotherapy·Casey Chun ZhouBrian J Stockman
Oct 29, 2002·Nature Cell Biology·Joanna K SaxWafik S El-Deiry
Jul 3, 2004·The Lancet Oncology·Christian GrommesMichael T Heneka
Aug 25, 2004·Cancer Treatment Reviews·Stamos TheocharisGregory Kouraklis
Oct 16, 2004·Expert Review of Anti-infective Therapy·Dennis L StevensKarl Madaras-Kelly
Feb 15, 2005·Journal of Pharmaceutical and Biomedical Analysis·Arun K AgrawalRonald B Franklin
Jul 5, 2006·Molecular Cancer Therapeutics·Andrei L Gartel
Jan 3, 2007·Biochemical and Biophysical Research Communications·Hyun-Ock PaeHun-Taeg Chung
Apr 7, 2007·The International Journal of Biochemistry & Cell Biology·Matthias Ocker, Regine Schneider-Stock
Aug 25, 2007·Nature Reviews. Molecular Cell Biology·M Chiara MaiuriGuido Kroemer
Jan 29, 2008·Anti-cancer Agents in Medicinal Chemistry·S A BrooksP M Rudd
Jul 25, 2008·Nature·Alberto MantovaniFrances Balkwill
Mar 28, 2009·Cell Death and Differentiation·A Eisenberg-LernerA Kimchi
Jul 9, 2009·Journal of Cellular and Molecular Medicine·Jennifer S CarewSteffan T Nawrocki
Nov 13, 2010·Cell Death and Differentiation·Z T SchugE Gottlieb
Feb 12, 2011·Cell Death and Differentiation·R KangD Tang
Mar 8, 2011·Cell·Douglas Hanahan, Robert A Weinberg
May 19, 2011·Nature Reviews. Clinical Oncology·Filip JankuRazelle Kurzrock
Oct 8, 2011·Bioorganic & Medicinal Chemistry·Alok SinghWon Koo Lee
Dec 24, 2011·Annals of the New York Academy of Sciences·Karen Joy Shaw, Michael R Barbachyn
Jan 11, 2012·Current Cancer Drug Targets·J J G MarinR I R Macias
Mar 7, 2012·Proceedings of the National Academy of Sciences of the United States of America·Cecilia Garcia-PerezGyörgy Hajnóczky
May 2, 2012·Bioorganic & Medicinal Chemistry·Francisco W A BarrosMarilia O F Goulart
Dec 22, 2012·Medical Principles and Practice : International Journal of the Kuwait University, Health Science Centre·Samuel B Kombian, Oludotun A Phillips
Aug 6, 2013·Genes & Development·Kenta Moriwaki, Francis Ka-Ming Chan
May 6, 2014·European Journal of Medicinal Chemistry·Annavareddi NareshBatchu Venkateswara Rao
May 31, 2014·Anti-cancer Agents in Medicinal Chemistry·Tanushree PalC S Ramaa
Jul 6, 2014·The Journal of Antimicrobial Chemotherapy·Sisi WuZhenling Wang
Dec 3, 2014·Molecular Cell·Pratyusha MandalWilliam J Kaiser
Mar 5, 2015·Seminars in Cell & Developmental Biology·Najoua LalaouiPaul G Ekert
Jan 1, 2012·International Journal of Medicinal Chemistry·Neha PanditBirendra Shrivastava
Jul 21, 2015·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Ammad Ahmad FarooqiHsueh-Wei Chang

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