Abstract:
: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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Barraja P,Diana P,Montalbano A,Carbone A,Cirrincione G,Viola G,Salvador A,Vedaldi D,Dall'acqua Fdoi
10.1016/j.bmc.2008.10.002subject
Has Abstractpub_date
2008-11-15 00:00:00pages
9668-83issue
22eissn
0968-0896issn
1464-3391pii
S0968-0896(08)00940-1journal_volume
16pub_type
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更新日期:2014-10-15 00:00:00
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