Synthesis and biological evaluation of pyrroloiminoquinone derivatives |
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Authors: | Passarella Daniele Belinghieri Francesca Scarpellini Michele Pratesi Graziella Zunino Franco Gia Ornella Maria Via Lisa Dalla Santoro Giuseppe Danieli Bruno |
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Institution: | Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy. |
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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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