Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents
作者:Constance Genès、Gaëlle Lenglet、Sabine Depauw、Raja Nhili、Soizic Prado、Marie-Hélène David-Cordonnier、Sylvie Michel、François Tillequin、François-Hugues Porée
DOI:10.1016/j.ejmech.2011.02.065
日期:2011.6
Benzo[c]phenanthrolines and benzo[c]phenanthrolinones substituted by dialkylaminoalkyl side chains at position N5 and C6, respectively, were synthesised and their biological activity evaluated. They displayed interessant cytotoxicity associated with some DNA interactions. However, the low topoisomerase 1 affinity suggests that other cellular targets are responsible for the antiproliferative activity
分别合成了在位置N5和C6处被二烷基氨基烷基侧链取代的苯并[ c ]菲咯啉和苯并[ c ]菲咯啉酮,并对其生物学活性进行了评估。他们表现出与某些DNA相互作用有关的间质细胞毒性。但是,低的拓扑异构酶1亲和力表明其他细胞靶标负责抗增殖活性。