5-Azacytidine is a Potential Chemotherapeutic Agents for...

Overview 5-Azacytidine is a chemical analogue of cytidine, a nucleoside present in DNA and RNA with antineoplastic activity. It is sold under the brand name Vidaza. The drug was first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer. It is an inhibitor of DNA methylation and was approved by the US FDA for the treatment of Myelodysplastic syndromes (MDS) in May 2004. MDS are diseases caused by abnormalities in the blood-forming cells of the bone marrow, which result in low production of healthy blood cells. Cytotoxic effect is exerted on rapidly dividing cancerous cells by the drug. This restores the normal function of genes to control proper cellular differentiation and proliferation. The systematic (IUPAC) name of this drug is 4-amino-1-B-D-ribofuranosyl-1, 3, 5-triazin-2 (1H)- one and the molecular formula is C8H12N4O5. (1) DNA methylation is one of several epigenetic events taking place in the mammalian genome that cells use to control gene expression. DNA methylation plays a vital role in numerous cellular processes whereas abnormal patterns of methylation have been related to several human diseases like tumors. (2) For example, hypermethylation is most extensively studied of all epigenetic modifications. It represses transcription of the promoter regions of tumor suppressor genes, thereby leading to gene silencing and cancer development. Hypermethylation at the CpG islands has been described in MDS, acute myelogenous leukemia (AML), and