Acridine/acridone: a simple scaffold with a wide range of application in oncology

Abstract

Background: The acridine scaffold is of interest since its DNA affinity and intercalative properties make it an important pharmacophore for the design of antitumor drugs targeting DNA. The global substitution on the heterocycle is crucial for a specific biological activity and also selectivity for tumor cells. Objective: Our aim is to review the most promising therapeutic developments within the vast research field dealing with acridine derivatives by pinpointing the new trends and the promising therapeutic directions. Methods: Our patent search covered the 2000 – 2008 period and was enriched with literature data. We focused on cancer/tumor-targeted new therapies where the acridine/acridone derivatives play a key role in the biological function studied. Results/conclusion: The most important therapies are those focusing specifically on tumor cells. Therefore, photodynamic therapy and hypoxia-selective drugs are of particular interest.