Synthesis and antitumor activity of novel amsacrine analogs: The critical role of the acridine moiety in determining their biological activity

Abstract

A new series of N-[4-(2′-oxo-2 H-pyrano[2,3- b]quinolin-5′-ylamino)-phenyl] -methanesulfonamides was prepared and analyzed as novel amsacrine-like derivatives. Our preliminary biological evaluation has shown that the replacement of the acridine moiety with the analogous 2-oxo-2 H-pyrano[2,3- b]quinoline system drastically reduced both their anticancer activity and their propency to intercalate into double stranded DNA.