Abstract
Analogues of the antitumour alkaloids fagaronine and nitidine have been synthesized to investigate their structure-activity relationships against P388 leukaemia in mice. Bulky substituents at the 12-position are well tolerated, whereas substituents larger than methoxy in the 2-position result in total loss of activity. The effects of hydroxy groups in the 2- and 12-positions, which are respectively potency-enhancing and potency destroying, are rationalized in terms of their potential influence on bioavailability. Suitable choice of substituents may allow the production of more potent analogues with improved ability to penetrate lipid membranes.
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