Synthesis and biological evaluation of pyrroloiminoquinone derivatives

  • Bioorg Med Chem. 2008 Mar 1;16(5):2431-8. doi: 10.1016/j.bmc.2007.11.063.
Daniele Passarella  1 ,  Francesca Belinghieri ,  Michele Scarpellini ,  Graziella Pratesi ,  Franco Zunino ,  Ornella Maria Gia ,  Lisa Dalla Via ,  Giuseppe Santoro ,  Bruno Danieli
Affiliations
  • 1. Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
PMID: 18077173 DOI: 10.1016/j.bmc.2007.11.063
Abstract

Synthesis of 10 pyrroloiminoquinone derivatives is presented. The strategy is based around the elaboration of a common intermediate by reaction with primary amines. All the compounds obtained have been subjected to antiproliferative activity with three different cell lines (NCI-H460, HeLa, and HL-60). The capacity of 4 selected compounds to affect the enzymatic activity of the nuclear enzyme DNA Topoisomerase II and to form the typical DNA fragmentation which occurs in the apoptotic process is discussed here.