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  • Title: Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes.
    Author: Opsenica D, Angelovski G, Pocsfalvi G, Juranić Z, Zizak Z, Kyle D, Milhous WK, Solaja BA.
    Journal: Bioorg Med Chem; 2003 Jul 03; 11(13):2761-8. PubMed ID: 12788350.
    Abstract:
    Several cis and trans bis-steroidal 1,2,4,5-tetraoxanes possessing amide terminus were synthesised and evaluated as antimalarials and antiproliferatives. The compounds exhibited submicromolar antimalarial activity against Plasmodium falciparum D6 and W2 strains. The existence of HN-C(O) moiety was found necessary for pronounced antimalarial and antiproliferative activity. In antiproliferative screen, the trans tetraoxane 6 was found to exhibit a pronounced cytotoxicity on 14 cancer cell lines. In addition, tetraoxanes 11 and 12 exhibited significant cytotoxic activity too; microscopic examination of treated HeLa cells showed morphological appearance reminiscent for apoptosis (condensed and/or fragmented nuclei).
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