title: Synthesis and photochemotherapeutic activity of thiopyrano[2,3-e]indol-2-ones.
abstract: A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.
authors.affiliation: Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo Via Archirafi 32, 90123 Palermo, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Barraja
authors.forename: Laura
authors.initials: L
authors.lastname: Sciabica
authors.forename: Patrizia
authors.initials: P
authors.lastname: Diana
authors.forename: Antonino
authors.initials: A
authors.lastname: Lauria
authors.forename: Alessandra
authors.initials: A
authors.lastname: Montalbano
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Almerico
authors.forename: Gaetano
authors.initials: G
authors.lastname: Dattolo
authors.forename: Girolamo
authors.initials: G
authors.lastname: Cirrincione
authors.forename: Silvia
authors.initials: S
authors.lastname: Disarò
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Basso
authors.forename: Giampietro
authors.initials: G
authors.lastname: Viola
authors.forename: Francesco
authors.initials: F
authors.lastname: Dall'Acqua
mesh_terms: D002455:Cell Division / Q000187:drug effects / Q000528:radiation effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D004273:DNA, Neoplasm / Q000187:drug effects / Q000528:radiation effects; D018922:HL-60 Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D010778:Photochemotherapy / Q000379:methods; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D011714:Pyrans / Q000138:chemical synthesis* / Q000494:pharmacology; D014466:Ultraviolet Rays
chemical_list: D004273:DNA, Neoplasm; D007211:Indoles; D017319:Photosensitizing Agents; D011714:Pyrans