Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes
AuthorsOpsenica, Dejan M.
Šolaja, Bogdan A.
Article (Published version)
MetadataShow full item record
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). (C) 2003 Elsevier Science Ltd. All rights reserved.
Source:Bioorganic and Medicinal Chemistry, 2003, 11, 13, 2761-2768
- Pergamon-Elsevier Science Ltd, Oxford