“…Ellipticine (1; 5,ll-dimethyl-6H-pyrido [4,[3][4][5][6]carbazole) and its methoxy analogue 2 are alkaloids that exhibit antitumor activity in rodent models. 1 To the best of our knowledge, of the many ellipticine analogues that have been synthesized, only 2 and elliptinium acetate (3; 9hydroxy-2,5,ll-trimethyl-6J/-pyrido [4,[3][4][5]carbazolium acetate) demonstrated significant antitumor activity in In a previous paper,3 we proposed a new mechanism of action at the molecular level to account for the antitumor activity of ellipticine. It was suggested that in the host, 1 was metabolized to 4, which in turn was subjected to biooxidation followed by enzymatic esterification to give first 5 and then 6.…”