Synthesis and biological evaluation of pyrroloiminoquinone derivatives

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.

A series of pyrroloiminoquinone derivatives has been synthesized and tested for their antiproliferative activity toward NCI-H460, HeLa and HL-60. The capacity of selected compounds to affect the enzymatic activity of topoisomerase II and the interaction with DNA extracted from HeLa cells is discussed. An effective inhibitory effect on topoisomerase II is demonstrated.Figure optionsDownload as PowerPoint slide