Details

Autor(en) / Beteiligte

• Kljun, Jakob
• Turel, Iztok

Titel

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

Ist Teil von

• European journal of inorganic chemistry, 2017-03, Vol.2017 (12), p.1655-1666

Ort / Verlag

Weinheim: Wiley Subscription Services, Inc

Erscheinungsjahr

2017

Link zum Volltext

Quelle

Wiley Online Library

Beschreibungen/Notizen

• The β‐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. This microreview describes the role of the β‐diketone fragment in the field of medicinal chemistry. Non‐steroidal anti‐inflammatory drugs of the coxib family, the natural product curcumin, budotitane and other transition‐metal complexes of β‐diketonates serve to demonstrate the importance and versatility of this important subgroup of β‐dicarbonyl compounds.