Passarella Daniele, Belinghieri Francesca, Scarpellini Michele, Pratesi Graziella, Zunino Franco, Gia Ornella Maria, Via Lisa Dalla, Santoro Giuseppe, Danieli Bruno
Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
Bioorg Med Chem. 2008 Mar 1;16(5):2431-8. doi: 10.1016/j.bmc.2007.11.063. Epub 2007 Nov 28.
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.
本文介绍了10种吡咯并亚氨基醌衍生物的合成。该策略基于通过与伯胺反应对一种常见中间体进行精心制备。所获得的所有化合物均已针对三种不同的细胞系（NCI-H460、HeLa和HL-60）进行了抗增殖活性测试。本文讨论了4种选定化合物影响核酶DNA拓扑异构酶II的酶活性以及形成凋亡过程中发生的典型DNA片段化的能力。
