Drug resistance to commonly utilized chemotherapeutics (i.e. cisplatin) has begun to emerge necessitating a search for new anticancer agents. To this end, this work details the synthesis, characterization, aqueous chemistry, and anticancer activity of a series of gold(III) 7-substituted dipyrido[3,2-a:2',3'-c] phenazine complexes. This work represents a continuation of our previous work in which the gold(III) dipyrido[3,2-a:2`,3`-c]phenazine was found to have a lower cytotoxicity among the complexes tested. The aromatic heterocyclic functionality was changed by varying the shape and polarity of the substituents with the hope that substituents may alter the extent of intercalation and bind to DNA at sequence-specific regions. Anticancer activity and DNA interaction studies were conducted to determine whether stacking interactions differ among this ligand series.