Abstract
To develop new cytotoxins, which could find use as anti-cancer agents, polyamine conjugates were synthesized containing spermine and an anthracene or acridine unit. Spermine is known to groove-bind to DNA; anthracene and acridine are known to intercalate. It was hoped that these polyamine-polyaromatic conjugates would use both modes of binding. Studies of growth inhibition of B16 murine melanoma cells showed the conjuates to be more effective than either spermine, anthracene-9-carboxylic acid or acridine-9-carboxylic acid, and of the conjugates, the acridine derivative showed greatest activity.
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