Organometallic antitumor complexes have become an increasingly important class of medicinal agents. In particular, organoferrous prodrugs are promising due to their low cost and relative ease of synthesis. We have focused our research efforts on designing and synthesizing innovative molecules for cancer therapy that generate free iron(II) <i>in situ</i> via stable organometallic precursors. We propose the generation of free iron in cells can disrupt iron homeostasis and lead to cell death. This new class of organoferrous prodrugs are designed to circumvent iron transport and storage mechanisms in tumor cells; <i>in situ </i>generation of free iron(II) causes rapid conversion of endogenous hydrogen peroxide to hydroxyl radials with a high degree of spatiotemporal control. It is proposed that the resultant rapid disruption of hydrogen peroxide and iron homeostasis will shut down beneficial hydrogen peroxide cell signaling processes, increase the fatal concentration of hydroxyl radical in cells, and ultimately cell death. Herein, we will present the design, synthesis, and bioactivity of our organoferrous agents.

Synthesis and design of organoferrous compounds as anti-tumor agents

251st National Meeting (2016)

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