Synthesis of β-functionalized Temoporfin derivatives for an application in photodynamic therapy

The synthesis of novel beta-functionalized derivatives of the clinically used photosensitizer Temoporfin has been achieved by nucleophilic addition reactions to a corresponding diketo chlorin. The beta-substituted dihydroxychlorin products exhibit a strong absorption in the red spectral region, a high singlet oxygen quantum yield, and were found to be highly effective in in vitro assays against HT-29 tumor cells. (C) 2011 Elsevier Ltd. All rights reserved.