Synthesis and photochemotherapeutic activity of thiopyrano[2,3-e]indol-2-ones.
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.
Barraja
Paola
P
Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo Via Archirafi 32, 90123 Palermo, Italy.
Sciabica
Laura
L
Diana
Patrizia
P
Lauria
Antonino
A
Montalbano
Alessandra
A
Almerico
Anna Maria
AM
Dattolo
Gaetano
G
Cirrincione
Girolamo
G
Disarò
Silvia
S
Basso
Giuseppe
G
Viola
Giampietro
G
Dall'Acqua
Francesco
F
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
D004273:DNA, Neoplasm; D007211:Indoles; D017319:Photosensitizing Agents; D011714:Pyrans