A fast entry to the novel medicinally-important 9-anilinoacridine peptidyls by solid phase organic synthesis (SPOS)

A new approach to the synthesis of novel medicinally-important mono- and bis-9-anilinoacridine (9-AnA) peptidyl derivatives is described. The method generates efficiently 9-AnAs with variable spacer lengths and charged, polar or hydrophobic residues at desired positions, which can increase binding affinity, conformational stability, intracellular transport and/or biological activity. The synthetic routes reported in this work are both general and applicable, and significantly expand the scope of potential 9-aminoacridine (9-AA) anticancer candidates.