9-Nitrocamptothecin (9-NC) is a water insoluble derivative of camptothecin [
C1495] with broad antitumor activity. Its metabolite is 9-aminocamptothecin [
A2063]. Camptotecin and its derivatives interfere with DNA synthesis by inhibiting the enzyme topoisomerase-I. In order to prevent and correct of topological problems caused by the DNA double helix, topoisomerase-I catalyzes the relaxation of negatively supercoiled DNA, the knotting and unknotting DNA and the linking complementary rings of single-stranded DNA into double-stranded rings. Then the inhibition action induces breaks in single strand DNA. Eventually, this leads to double-strand DNA breaks and apoptosis or cell death.