In the last four decades, the emphasis was laid on the research of small organic molecules
with potential anti-cancer activity. Linezolid was the first oxazolidinone derivative approved by FDA
for MRSA treatment. Despite its major role in antimicrobial activity, these molecules display other
properties, also serving as an antitumor agent. The importance of drug repurposing could be highlighted
by the use of Oxazolidinone derivatives in pre-clinical studies, which are able to act through
different pathways, such as partial agonist of transcription factor PPAR-γ, an inhibitor of key enzymes
related to hormone-dependent disorders and even on sphingolipid metabolism as well. The purpose of
this short review is to discuss the application of oxazolidinone derivatives as an antitumor agent by
highlighting the most promising molecules studied by many research groups worldwide. Main biological
activity against several tumor cell lines, including hematopoietic and solid cancer cell lines have
been discussed. In addition, this study intends to report how different types of oxazolidinone derivatives
can act as antitumor agents describing their distinct mechanisms of action based on their targets.
Keywords: Cancer, ceramide, oxazolidinone, PPAR, therapeutic, 17β-HSD.
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