4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 19, Pages 5808-5811

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.07.113

Keywords

Photodynamic therapy (PDT); Photosensitizer; Photocytotoxicity; Temoporfin; Chlorins

Funding

  1. Arbeitsgemeinschaft industrieller Forschungsvereinigungen 'Otto-von-Guericke' e. V. (AiF) [KF0579901UL7, KF0249303UL7]

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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.

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