Towards Light Activated Ruthenium-Arene (RAPTA-type) Prodrug Candidates.

Towards Light Activated Ruthenium-Arene (RAPTA-type) Prodrug Candidates. Chembiochem. 2019 May 18;: Authors: Renfrew AK, Karges J, Scopelliti R, Bobbink FD, Nowak-Sliwinska P, Gasser G, Dyson P Abstract Cancer is currently one of the deadliest diseases worldwide. Based on the high incidence of this disease, the side-effects associated with current chemotherapies and the appearance of drug resistance, considerable efforts have been directed towards the development of new anticancer drugs with new modes of action during. Metal-based compounds were shown to be particularly attractive candidates due to their metabolic mechanisms which differ substantially to organic drugs. Of special interest in this context are organometallic ruthenium(II) complexes of the type [Ru(η6-arene)(pta)Cl2] (arene = p-cymene, toluene, benzene, etc.; pta = 1,3,5-triaza-7-phosphaadamantane), abbreviated RAPTA. Complementary to chemotherapy, photoactivated chemotherapy (PACT) is a technique that has received increasing attention towards the development of treatment of numerous kinds of cancer. With this in mind, we have designed a photoactive RAPTA-type complex bearing azide ligands. The diazide complex, [Ru(η6-p-cymene)pta(N3)2], is inert in water but slowly releases the azide ligand on exposure to light. Consequently, the in vitro cytotoxicity of the complex in the dark as well as upon light exposure at 450 nm in human cervical carcinoma (HeLa) and non-cancer...
Source: Chembiochem - Category: Biochemistry Authors: Tags: Chembiochem Source Type: research