Reactive Oxygen Species (ROS) are chemically reactive molecules formed as a natural byproduct of metabolism in cells. These species play an important role in cell signaling and homeostasis. Recent literature studies have shown that bulk cancer cells, including cancer stem cells, have elevated levels of ROS when compared to normal cells. Based on the literature support, our lab is designing novel ROS activated pro-drugs that target cancer cells over normal cells. We recently synthesized a new scaffold which undergoes oxidation in presence of ROS to activate. We hypothesize that upon oxidation, this new agent may undergo a cyclic transition state that may interact with DNA or act as a strong electrophile which may react with anti-oxidants in the cell to cause its depletion, leading to cell death. We are synthesizing a new series of these agents with modifications at various locations in the lead molecule to understand structure activity relationship (SAR). This study will help us design agents with increased specificity and cytotoxicity.

Novel ROS activated prodrugs: A therapeutic approach to selectively target cancer cells

246th National Meeting (2013)

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