Acridone

Abstract: Seven transformation products of carbamazepine generated by at least one of three common water treatment technologies (UV-radiation, oxidation with chlorine dioxide (ClO2), and biological treatment with activated sludge) were identified by complementary use of ion trap, single quadrupole, and quadrupole-time-of-flight mass spectrometers. Acridine was formed during all of the three treatment processes, while acridine 9-carbaldehyde was identified as an intermediate during ClO2 oxidation. Further treatment of acridine with ClO2 produced 9-hydroxy-acridine. UV-treatment resulted in the formation of acridone, hydroxy-(9H,10H)-acridine-9-carbaldehyde, acridone-N-carbaldehyde, and 1-(2-benzaldehyde)-(1H,3H)-quinazoline-2,4-dione, while biological breakdown of acridine yielded acridone. In parallel, the transformation product iminostilbene was observed during sample analysis. In addition, this study compared the treatment technologies according to the removal of carbamazepine and the production and decay of its ...

Abstract: Acridine derivatives are interesting chemotherapeutic agents that were first used as antibacterial and antiparasite agents. In this review we wish to concentrate our attention on the anticancer properties of acridines used in clinics since the 1970's. Based on recent results, an outlook on antitumour acridine chemotherapy will be proposed. The biological activity of acridines is mainly attributed to the planarity of these aromatic structures, which can intercalate within the double-stranded DNA structure, thus interfering with the cellular machinery. Recent understanding of the mode of action of acridines leads to continuous and exciting research in this heterocyclic family. Indeed, biological targets such as topoisomerases I and II, telomerase/telomere and protein kinases emerge and allow the design of novel acridine-based patterns. This review further pinpoints the latest progress in the development of anticancer agents based on naturally occurring and synthetic acridines (e.g. acridones, pyridoacridines); for this matter in vitro/in vivo studies and clinical trial results will be discussed. The DNA-affinic property of acridine is also useful to vectorise drugs into cell nuclei and some applications in hypoxia-selective treatment, platinum or N-mustard derived conjugates will be reported. Some other properties including inhibition of multidrug resistance or potential impact on Alzheimer disease will be treated. It is noteworthy that the position and the nature of the substituent on the heterocyclic core are determinants for the biological property and selectivity observed. So, we wish also to disclose a summary of recent synthetic methodologies developed for acridine synthesis.

Abstract: Many people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. To date, many acridine/acridone analogues have been obtained, which, inter alia, exhibit antitumour (e.g., (1–5)), antimicrobial (e.g., (59)), and antiviral (e.g., (61)) activities and are applicable in the treatment of Alzheimer's disease (e.g., (26)). However, in many cases, their clinical application is limited and excluded because of side effects. In this survey, we describe acridine and acridone derivatives reported since 2013, methods of their synthesis and their potential clinical applications.