Author/Authors :
Daniele Passarella، نويسنده , , Francesca Belinghieri، نويسنده , , Michele Scarpellini، نويسنده , , Graziella Pratesi، نويسنده , , Franco Zunino، نويسنده , , Ornella Maria Gia، نويسنده , , Lisa Dalla Via، نويسنده , , Giuseppe Santoro، نويسنده , , Bruno Danieli، نويسنده ,
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.
Keywords :
antiproliferative activity , Pyrroloiminoquinone derivatives , topoisomerase II , DNA fragmentation