THIOPYRANO[2,3-E]INDOL-2-ONES: ANGELICIN HETEROANALOGUES WITH POTENT PHOTOANTIPROLIFERATIVE ACTIVITY
| Autor: | Patrizia Diana, Giampietro Viola, Alessia Salvador, Alessandra Montalbano, Girolamo Cirrincione, Paola Barraja, Daniela Vedaldi, Anna Carbone, Francesco Dall'Acqua |
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| Přispěvatelé: | BARRAJA, P, DIANA, P, MONTALBANO, A, CARBONE, A, CIRRINCIONE, G, VIOLA, G, SALVADOR, A, VEDALDI, D, DALL'ACQUA, F |
| Jazyk: | angličtina |
| Rok vydání: | 2008 |
| Předmět: |
Indoles
Stereochemistry DNA damage Ultraviolet Rays Angelicin Thiopyrano[2 3-e ]indol-2-one Clinical Biochemistry Pharmaceutical Science HL-60 Cells Apoptosis Thiopyrano[2 Antiproliferative activity Biochemistry Chemical synthesis chemistry.chemical_compound Inhibitory Concentration 50 Jurkat Cells Photochemotherapeutic agents Furocoumarins Drug Discovery Thiolactone Tumor Cells Cultured Humans Photosensitizer 3-e ]indol-2-ones Molecular Biology Photosensitizing Agents Furocoumarin Organic Chemistry Proteins Biological activity DNA Settore CHIM/08 - Chimica Farmaceutica Mitochondria chemistry Photochemotherapeutic agent Molecular Medicine Lipid Peroxidation Phototoxicity DNA Damage |
| Popis: | A new class of compounds, the thiopyrano[2,3-e]indol-2-ones, bioisosters of the angular furocoumarin angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents. In particular 7,8-dimethyl-thiopyranoindolone 6c s showed a remarkable phototoxicity and a great dose UVA dependence reaching IC(50) values at submicromolar level. This latter photoinduced a massive apoptosis and a remarkable photodamage to lipids and proteins. Although it did not intercalate DNA, it was able to cause photooxidation of DNA bases. |
| Databáze: | OpenAIRE |
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