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

A new series of N-[4-(2′-oxo-2H-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-2H-pyrano[2,3-b]quinoline system drastically reduced both their anticancer activity and their propency to intercalate into double stranded DNA.

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