title: Synthesis of β-functionalized temoporfin derivatives for an application in photodynamic therapy.
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.
authors: Universität Leipzig, Institut für Organische Chemie, Johannisallee 29, 04103 Leipzig, Germany.
authors: Daniel
authors: D
authors: Aicher
authors: Susanna
authors: S
authors: Gräfe
authors: Christian B W
authors: CB
authors: Stark
authors: Arno
authors: A
authors: Wiehe
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D019073:HT29 Cells; D006801:Humans; D006900:Hydroxylation; D008652:Mesoporphyrins / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D009992:Osmium; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011166:Porphyrins / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008652:Mesoporphyrins; D017319:Photosensitizing Agents; D011166:Porphyrins; C006969:chlorin; D009992:Osmium; C072269:temoporfin