2-7-dibromocryptolepine and Malaria

2-7-dibromocryptolepine has been researched along with Malaria* in 1 studies

Other Studies

1 other study(ies) available for 2-7-dibromocryptolepine and Malaria

ArticleYear
Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents.
    Journal of medicinal chemistry, 2001, Sep-13, Volume: 44, Issue:19

    The indoloquinoline alkaloid cryptolepine 1 has potent in vitro antiplasmodial activity, but it is also a DNA intercalator with cytotoxic properties. We have shown that the antiplasmodial mechanism of 1 is likely to be due, at least in part, to a chloroquine-like action that does not depend on intercalation into DNA. A number of substituted analogues of 1 have been prepared that have potent activities against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum and also have in common with chloroquine the inhibition of beta-hematin formation in a cell-free system. Several compounds also displayed activity against Plasmodium berghei in mice, the most potent being 2,7-dibromocryptolepine 8, which suppressed parasitemia by 89% as compared to untreated infected controls at a dose of 12.5 mg kg(-1) day(-1) ip. No correlation was observed between in vitro cytotoxicity and the effect of compounds on the melting point of DNA (DeltaT(m) value) or toxicity in the mouse-malaria model.

    Topics: Alkaloids; Animals; Antimalarials; Antineoplastic Agents; Cattle; DNA; Drug Screening Assays, Antitumor; Heating; Hemin; Indole Alkaloids; Indoles; Malaria; Mice; Nucleic Acid Denaturation; Plasmodium berghei; Plasmodium falciparum; Quinolines; Structure-Activity Relationship; Tumor Cells, Cultured

2001