A Concise Paradigm for the Construction of Amide Linker of 2,7-Diamidoanthraquinone Derivatives as Potential Telomerase Inhibitors

Abstract

A series of 2,7-bis(aminoalkanamido) anthraquinones have been synthesized by treatment of the corresponding bis (haloalkanamido) derivatives with appropriate amines. We have previously described a series of 1,4-,1,5-,1,8- and 2,6-difunctionalized anthraquinones, which exhibit different spectra of potency, together with human telomerase evaluation. A representative compounds in the series have been examined by their NMR spectroscopic study and some indications of structural identification have been discerned. The present study details the preparation of further, distinct series of symmetrical substituent on the 2,7-position regioisomeric difunctionalized amidoanthraquinone and SAR optimization will be reported in due course.