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Bioorg Med Chem ; 16(5): 2431-8, 2008 Mar 01.
Article in English | MEDLINE | ID: mdl-18077173

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.


Subject(s)
Pyrroloiminoquinones/chemical synthesis , Pyrroloiminoquinones/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , DNA/genetics , DNA Topoisomerases, Type II/metabolism , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Humans , Molecular Structure , Pyrroloiminoquinones/chemistry , Structure-Activity Relationship , Topoisomerase II Inhibitors
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