Acridine derivatives as inhibitors/poisons of topoisomerase II.

The potential of acridines (amsacrine) as a topoisomerase II inhibitor or poison was first discovered in 1984, and since then, a considerable number of acridine derivatives have been tested as topoisomerase inhibitors/poisons, containing different substituents on the acridine chromophore. This review will discuss a series of studies published over the course of the last decade, which have investigated various novel acridine derivatives against topoisomerase II activity. This review will discuss a series of studies published over the course of the last decade, which have investigated of various novel acridine derivatives against topoisomerase II activity. Important recent studies have reported further interesting results concerning the effect of new acridine derivatives (4, 5, 24–27, 30, 33, 43–65, 68, 70–73, and 77) as inhibitors/poisons of topoisomerase IIα. The data presented in this article extended the potential activity of acridine derivatives to treating the Topo IIα as the universal target in drug discovery and development. [ABSTRACT FROM AUTHOR]