Comparative QSAR studies on substituted bis-(acridines) and bis-(phenazines)carboxamides: A new class of anticancer agents

Quantitative structure-activity relationships have been formulated for two sets of DNA binding topoisomerase agents (bis-acridines and bis-phenazines) acting on murine P388 leukemia cells, murine Lewis lung carcinoma (LLC) ce lls and human Jurkat leukemia wild-type (JL(C)) cells. For the acridines, a ll three QSARs (1-3) show only a (small negative) hydrophobic effect. In sh arp contrast, the phenazines in all three studies (4-6) show a strong hydro phobic effect, with the optimum ClogP being near 7.3 for all examples. This suggests that, despite the structural similarity of the compounds, differe nt modes of enzyme and/or DNA binding may be involved. (C) 2000 Elsevier Sc ience Ltd. All rights reserved.