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

Affiliation

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.

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