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Antimalarial and Antiproliferative Evaluation of Bis-Steroidal Tetraoxanes

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http://pubman.mpdl.mpg.de/cone/persons/resource/persons83784

Angelovski,  G
Department Physiology of Cognitive Processes, Max Planck Institute for Biological Cybernetics, Max Planck Society;

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Citation

Opsenica, D., Angelovski, G., Pocsfalvi G, Juranic Z, Zizak Z, Kyle D, Milhous, W., & Solaja, B. (2003). Antimalarial and Antiproliferative Evaluation of Bis-Steroidal Tetraoxanes. Bioorg. Med. Chem., 11, 2761-2768.


Cite as: http://hdl.handle.net/11858/00-001M-0000-0013-DD60-6
Abstract
Azamacrocyclic fluorophores containing piperazine units were synthesized using sequential rhodium-catalyzed regioselective hyd 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).