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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Authors | Daniel Aicher, Susanna Gräfe, Christian B W Stark, Arno Wiehe |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 21
Issue 19
Pg. 5808-11
(Oct 01 2011)
ISSN: 1464-3405 [Electronic] England |
PMID | 21885278
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2011 Elsevier Ltd. All rights reserved. |
Chemical References |
- Antineoplastic Agents
- Mesoporphyrins
- Photosensitizing Agents
- Porphyrins
- chlorin
- Osmium
- temoporfin
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Drug Design
- Drug Evaluation, Preclinical
- HT29 Cells
- Humans
- Hydroxylation
- Mesoporphyrins
(chemistry, pharmacology)
- Molecular Structure
- Osmium
- Photochemotherapy
- Photosensitizing Agents
(chemical synthesis, chemistry, pharmacology)
- Porphyrins
(chemistry)
- Structure-Activity Relationship
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