Synthesis and photochemotherapeutic activity of thiopyrano[2,3-e]indol-2-ones

  • Bioorg Med Chem Lett. 2005 May 2;15(9):2291-4. doi: 10.1016/j.bmcl.2005.03.016.
Paola Barraja  1 ,  Laura Sciabica ,  Patrizia Diana ,  Antonino Lauria ,  Alessandra Montalbano ,  Anna Maria Almerico ,  Gaetano Dattolo ,  Girolamo Cirrincione ,  Silvia Disarò ,  Giuseppe Basso ,  Giampietro Viola ,  Francesco Dall'Acqua
Affiliations
  • 1. Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo Via Archirafi 32, 90123 Palermo, Italy.
PMID: 15837311 DOI: 10.1016/j.bmcl.2005.03.016
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.