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. 2011 Oct 1;21(19):5808-11.
doi: 10.1016/j.bmcl.2011.07.113. Epub 2011 Aug 8.

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

Daniel Aicher  1 , Susanna Gräfe, Christian B W Stark, Arno Wiehe
Affiliations

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

Daniel Aicher et al. Bioorg Med Chem Lett. .

Abstract

The synthesis of novel β-functionalized derivatives of the clinically used photosensitizer Temoporfin has been achieved by nucleophilic addition reactions to a corresponding diketo chlorin. The β-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.

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