Multifunctionalization of Deferasirox as a Novel Cancer Treatment

Metal ions are needed in numerous processes that are crucial for the survival and well-being of all living organisms. In the human body, iron cations are essential for blood production, as well as oxygen transport from the lungs to the rest of the body. Iron cations are also vital for protein functions, such as those required for cell replication; thus, they can play a key role in the proliferation, metabolism, and growth of cancer cells. However, this same role can be exploited to inhibit the growth of cancer cells. This can be accomplished through the use of chelating agents, or chelators – small molecules that bind very tightly to sequester metal ions and eliminating their utility. Here, we investigate the orally active iron chelator Deferasirox for its potential as an antiproliferative agent against various cancer cell lines. We developed several Deferasirox derivatives to increase cell permeability for our derivatives, allowing us to access and sequester the iron cations within cancer cells. Our derivatives illustrated noteworthy results at rapidly inhibiting cancer cell growth. We believe future derivatives and different types of chelators may be of interest in exploiting other metal ions, such as copper and zinc, in anticancer therapies.Chemistr