Antimalarial and Antiproliferative Evaluation of Bis-Steroidal Tetraoxanes

Opsenica, D; Angelovski, G; Pocsfalvi, G; Juranic, Z; Zizak, Z; Kyle, D; Milhous, WK; Solaja, BA

doi:10.1016/S0968-0896(03)00224-4

アイテム詳細

登録内容を編集ファイル形式で保存

一時保存へ追加

タグ情報を表示リリース履歴を表示詳細要約

公開

学術論文

Antimalarial and Antiproliferative Evaluation of Bis-Steroidal Tetraoxanes

MPS-Authors

There are no MPG-Authors in the publication available

External Resource

https://www.sciencedirect.com/science/article/pii/S0968089603002244
(出版社版)

Fulltext (restricted access)

There are currently no full texts shared for your IP range.

フルテキスト (公開)

公開されているフルテキストはありません

付随資料 (公開)

There is no public supplementary material available

引用

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. Bioorganic & Medicinal Chemistry, 11(13), 2761-2768. doi:10.1016/S0968-0896(03)00224-4.

引用: https://hdl.handle.net/11858/00-001M-0000-0013-DD60-6

要旨

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).