β-Diketones as Scaffolds for Anticancer Drug Design - From Organic Building Blocks to Natural Products and Metallodrug Components

The beta-diketone scaffold is a key intermediate in the synthesis of COX-2 inhibitors, a type of non-steroidal anti-inflammatory agents of the coxib family, which have also been shown to have excellent anticancer potential at the preclinical stage of research. Moreover, it is also present in the family of natural products named curcuminoids. Both natural products and their synthetic analogues possess interesting antibacterial, neuroprotective and anticancer properties. Coordination compounds of curcuminoids with platinum-group metals as potential anticancer agents are a hot topic of current research, with most scientific articles on this topic having been published in the last five years. Structurally simpler diketones, such as acetylacetone derivatives, are also employed in the design of new metal-based agents. Most notably, the first metal-based, non-platinum anticancer compound to enter clinical trials was budotitane - cis-diethoxy(1-phenylbutane-1,3-dionato) titanium(IV). Recently, several studies of platinum-group coordination and organometallic compounds, their biological evaluation and mode-of-action studies have been published in high-impact journals in the field of inorganic and medicinal chemistry.