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 IC50 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.
|Numero di pagine||16|
|Rivista||BIOORGANIC & MEDICINAL CHEMISTRY|
|Stato di pubblicazione||Published - 2008|
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