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Methoxy‐ and acetoxy‐8‐oxoberbines ‐ synthesis, antitumor activity, and interaction with DNA

1991; Wiley; Volume: 324; Issue: 8 Linguagem: Inglês

10.1002/ardp.2503240810

1521-4184

Christian Weimar, S. von Angerer, Wolfgang Wiegrebe,

Traditional and Medicinal Uses of Annonaceae

Abstract Most of the methoxy‐8 H ‐dibenzo[ a,g ]isoquinolin‐8‐ones 3a‐h and their acetoxy derivatives 6a‐e were synthesized by condensation of 1‐oxo‐1,2,3,4‐tetrahydroisoquinolines 4a‐c and homophthalic acid anhydrides 5a and b, ether cleavage and acetylation. These protoberberinones were tested for cytostatic activity in vitro using MDA‐MB‐231 mammary tumor cells and for interaction with native calf thymus DNA. Tetramethoxy‐8‐oxoberbine 3f shows an inhibition of cell proliferation of 87% at a concentration of 10 −5 mole; its cytostatic effect does not depend on intercalation into DNA.