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Synthesis, Assessment of Antineoplastic Activity, and Molecular Docking of Novel 2-Thioxo-oxazolidin-4-one Derivatives
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Background:
Oxazolidinones display several biological effects, including anticancer activity.
The purpose of this present work was to investigate a series of novel oxazolidinone derivatives
with potential antineoplastic activity. Their mechanisms of death induction and effects in the cell
cycle were also evaluated. A molecular docking study was accomplished through proteins of the
Cyclin-Dependent Kinases family (CDK). The new compound LPSF/NBM-2 was appeared to promote
cell cycle arrest at the G2/M phase and increase the percentage of apoptotic cells.
Methods:
Oxazolidinone derivatives were obtained through Knoevenagel condensation. The cytotoxic
assay was evaluated through the MTT method. Moreover, flow cytometry was performed in order
to investigate the effects of the new compounds on the cell cycle, induction of cell death, and apoptosis.
A blind docking was performed through the SwissDock online server and the analysis of the
results was performed using the UCSF Chimera and Biovia discovery studio software.
Results:
LPSF/NBM-1 and LPSF/NBM-2 displayed the most cytotoxic activity against HL-60 (IC50
= 54.83 μM) and MOLT-4 (IC50 = 51.61 μM) cell lines. LPSF/NBM-2 showed an increased percentage
of cell population at the G2/M phase. Molecular-docking results of LPSF/NBM-1 and
LPSF/NBM-2 suggested a binding affinity with the evaluated CDK proteins.
Conclusion:
LPSF/NBM-1 and LPSF/NBM-2 displayed cytotoxic profiles against Hl-60 and
MOLT-4. LPSF/NBM-2 increased cell population percentage at the G2/M phase and promoted cell
death compared to non-treated cells in the MOLT-4 cell line. Based on these findings, oxazolidinone
derivatives could be highlighted as possible cytostatic agents against lymphoma cells. Molecular
docking results suggested the action of LPSF/NBM-1 and LPSF/NBM-2 compounds on enzymes of
cyclin-dependent kinases family, however, more studies are needed to establish this correlation.
Title: Synthesis, Assessment of Antineoplastic Activity, and Molecular Docking
of Novel 2-Thioxo-oxazolidin-4-one Derivatives
Description:
Background:
Oxazolidinones display several biological effects, including anticancer activity.
The purpose of this present work was to investigate a series of novel oxazolidinone derivatives
with potential antineoplastic activity.
Their mechanisms of death induction and effects in the cell
cycle were also evaluated.
A molecular docking study was accomplished through proteins of the
Cyclin-Dependent Kinases family (CDK).
The new compound LPSF/NBM-2 was appeared to promote
cell cycle arrest at the G2/M phase and increase the percentage of apoptotic cells.
Methods:
Oxazolidinone derivatives were obtained through Knoevenagel condensation.
The cytotoxic
assay was evaluated through the MTT method.
Moreover, flow cytometry was performed in order
to investigate the effects of the new compounds on the cell cycle, induction of cell death, and apoptosis.
A blind docking was performed through the SwissDock online server and the analysis of the
results was performed using the UCSF Chimera and Biovia discovery studio software.
Results:
LPSF/NBM-1 and LPSF/NBM-2 displayed the most cytotoxic activity against HL-60 (IC50
= 54.
83 μM) and MOLT-4 (IC50 = 51.
61 μM) cell lines.
LPSF/NBM-2 showed an increased percentage
of cell population at the G2/M phase.
Molecular-docking results of LPSF/NBM-1 and
LPSF/NBM-2 suggested a binding affinity with the evaluated CDK proteins.
Conclusion:
LPSF/NBM-1 and LPSF/NBM-2 displayed cytotoxic profiles against Hl-60 and
MOLT-4.
LPSF/NBM-2 increased cell population percentage at the G2/M phase and promoted cell
death compared to non-treated cells in the MOLT-4 cell line.
Based on these findings, oxazolidinone
derivatives could be highlighted as possible cytostatic agents against lymphoma cells.
Molecular
docking results suggested the action of LPSF/NBM-1 and LPSF/NBM-2 compounds on enzymes of
cyclin-dependent kinases family, however, more studies are needed to establish this correlation.
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