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Expert Opinion on Therapeutic Patents Volume 18, 2008 - Issue 11
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Acridine/acridone: a simple scaffold with a wide range of application in oncology

Philippe Belmont Both authors contributed equally to this work; Université Claude Bernard Lyon 1, Université de Lyon, Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), Laboratoire de Synthèse et Méthodologie Organiques, Bâtiment CPE, UMR CNRS 5246, 43 boulevard du 11 Novembre 1918, 69622 Villeurbanne cedex, Lyon, France +33 4 72 44 58 68; +33 4 72 43 29 63; [email protected]
&
Ismet Dorange Both authors contributed equally to this work; Medivir AB, PO Box 1086, SE-14122 Huddinge, Sweden
Pages 1211-1224 | Published online: 29 Oct 2008
 
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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.

Notes

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