In the last fifty years, modified nucleosides and nucleobases, otherwise known as antimetabolites, have found use as therapeutic agents to treat various types of cancer. Current FDA-approved antimetabolite anti-cancer drugs, although effective, have numerous detrimental off target side effects. Our aim is to develop novel modified antimetabolites with improved properties, in particular with wider therapeutic window. Thus, a library of thymine derivatives bearing modifications at the 5-methyl position has been synthesized followed by cellular testing which has demonstrated their cytotoxicity towards MCF7 breast cancer cells. Structure-activity relationship study has revealed the lead compound, which has provided the opportunity to elucidate the mechanism of action of these novel modified nucleobases. With these in hand, we have the potential to develop novel anti-cancer agents with increased efficiency and minimized side effects. 

Novel modified nucleobases that show cytotoxicity towards breast cancer cells

248th National Meeting (2014)

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