The molecules of the anti cancer drug azonafides (an anthracene derivative) transform to a dimeric form even with the influence of ambient day-light as was found at the LMU University of Munich. Two molecules each of the drug forms a novel molecule with a different shape and different properties.
The newly found reaction of dimerisation causes two important consequences for the treatment of cancer: Firstly, prvious medical results should be critically re-evaluated because the photo dimerisation was unknown and the applied dose of the drug was arbitrary in medical tests and depended on the exposure to light during synthesis, handling and application. Secondly, the knowledge of the photo reaction allows the drug to be switched on or off according to local requirements of application. Thus, completely novel ways of application for the therapy of cancer become possible.
It is necessary to clarify whether the starting material is the entire drug or the product of photo dimerisation. The concentration of the drug decreases by the influence of light in the first case so that the medicament becomes inactive. On the other hand, if the entire drug would be formed with light in the second case the medicament would be inactive if not exposed to light.
Azonafides and its derivatives are known for their DNA intercalation and their inhibition of topoisomerase II. The drug inhibits the growth of tumours, even at low concentration. Pre clinical studies indicate activity against leukaemia melanomas and various types of other tumour such as mama, lung and kidney carcinomas. Drugs based on azonafides are of particular interest for the treatment of cancer because the problematic phenomenon of multi drug resistance (MDR) is not pronounced. Furthermore, the low toxicity of the drugs is of special advantage.
Publication:
„Anthracene Carboxyimides and Their
Dimers“,
Heinz Langhals, Gertrud Schönmann, Kurt Polborn, Chem. Eur.
J. 2008, 797-800; Published Online: Apr. 17, 2008.
http://www3.interscience.wiley.com/cgi-bin/abstract/118678164/ABSTRACT.
DOI: 10.1002/chem.200701844.
H. Langhals, 2009. - Impressum - Datenschutz - Kontakt