title: Synthesis and biological evaluation of pyrroloiminoquinone derivatives.
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.
authors: Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
authors: Daniele
authors: D
authors: Passarella
authors: Francesca
authors: F
authors: Belinghieri
authors: Michele
authors: M
authors: Scarpellini
authors: Graziella
authors: G
authors: Pratesi
authors: Franco
authors: F
authors: Zunino
authors: Ornella Maria
authors: OM
authors: Gia
authors: Lisa Dalla
authors: LD
authors: Via
authors: Giuseppe
authors: G
authors: Santoro
authors: Bruno
authors: B
authors: Danieli
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000235:genetics; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D047608:Pyrroloiminoquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D047608:Pyrroloiminoquinones; D059005:Topoisomerase II Inhibitors; D004247:DNA; D004250:DNA Topoisomerases, Type II