Synthesis of highly functionalized anthraquinones and evaluation of their antitumor activity

Highly functionalized anthraquinones which derive from the natural products mensacarcin, islandicin, and chrysophanol have been efficiently synthesized using a Diels-Alder reaction as key step. The introduction of the proposed pharmaco-phoric side chain unit has been achieved by an addition of an aryllithimn species onto different aldehydes. Furthermore, the antitumor activity of these novel compounds has been studied by the in vitro growth inhibition of human lung carcinoma cells of line A549. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007).