New Anthracenediones with Potential Anticancer Activity: Synthesis and Characterization of Bis-diethylaminopropionamido Derivatives

A number of new anthracenedione derivatives has been synthesized, which bear two charged side chains at different positions of the fused ring system. Hydroxyl groups at positions 1, 5 and/or 8 may also be present. These compounds resemble the well known antitumor drug mitoxantrone. The synthetic route included preparation of nitro‐derivatives, which were reduced to the corresponding amino‐derivatives, acylated with haloacyl halides and finally transformed into the tertiary amino analogues using the appropriate secondary amine. The new anthracenediones exhibit outstanding inhibition of cell proliferation in vitro. Some of them are promising in view of an application as anticancer drugs. Neue Anthrachinone mit potentieller Wirkung gegen Krebs: Synthese und Darstellung einiger Bis‐diethylaminopropionamid Derivate Neue 9,10‐Anthrachinonderivate mit Aminoalkylamido‐ und Hydroxy‐Substituenten wurden hergestellt. Nitroverbindungen wurden zu den entsprechenden Aminen reduziert. Diese wurden dann mit Chlorpropionylchlorid acyliert und endlich mit Diethylamin umgesetzt. Die neuen Derivate sind sehr aktiv in vitro und könnten gegen Krebs nützlich sein.