Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes
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Opsenica, Dejan M.Angelovski, G
Pocsfalvi, G
Juranić, Z.
Žižak, Željko S.
Kyle, D
Milhous, WK
Šolaja, Bogdan A.
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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.
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Bioorganic and Medicinal Chemistry, 2003, 11, 13, 2761-2768Publisher:
- Pergamon-Elsevier Science Ltd, Oxford
DOI: 10.1016/S0968-0896(03)00224-4
ISSN: 0968-0896
PubMed: 12788350
WoS: 000183590100011
Scopus: 2-s2.0-0037871977
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Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Opsenica, Dejan M. AU - Angelovski, G AU - Pocsfalvi, G AU - Juranić, Z. AU - Žižak, Željko S. AU - Kyle, D AU - Milhous, WK AU - Šolaja, Bogdan A. PY - 2003 UR - https://cherry.chem.bg.ac.rs/handle/123456789/559 AB - 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. PB - Pergamon-Elsevier Science Ltd, Oxford T2 - Bioorganic and Medicinal Chemistry T1 - Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes VL - 11 IS - 13 SP - 2761 EP - 2768 DO - 10.1016/S0968-0896(03)00224-4 ER -
@article{ author = "Opsenica, Dejan M. and Angelovski, G and Pocsfalvi, G and Juranić, Z. and Žižak, Željko S. and Kyle, D and Milhous, WK and Šolaja, Bogdan A.", year = "2003", 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). (C) 2003 Elsevier Science Ltd. All rights reserved.", publisher = "Pergamon-Elsevier Science Ltd, Oxford", journal = "Bioorganic and Medicinal Chemistry", title = "Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes", volume = "11", number = "13", pages = "2761-2768", doi = "10.1016/S0968-0896(03)00224-4" }
Opsenica, D. M., Angelovski, G., Pocsfalvi, G., Juranić, Z., Žižak, Ž. S., Kyle, D., Milhous, W.,& Šolaja, B. A.. (2003). Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes. in Bioorganic and Medicinal Chemistry Pergamon-Elsevier Science Ltd, Oxford., 11(13), 2761-2768. https://doi.org/10.1016/S0968-0896(03)00224-4
Opsenica DM, Angelovski G, Pocsfalvi G, Juranić Z, Žižak ŽS, Kyle D, Milhous W, Šolaja BA. Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes. in Bioorganic and Medicinal Chemistry. 2003;11(13):2761-2768. doi:10.1016/S0968-0896(03)00224-4 .
Opsenica, Dejan M., Angelovski, G, Pocsfalvi, G, Juranić, Z., Žižak, Željko S., Kyle, D, Milhous, WK, Šolaja, Bogdan A., "Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes" in Bioorganic and Medicinal Chemistry, 11, no. 13 (2003):2761-2768, https://doi.org/10.1016/S0968-0896(03)00224-4 . .