Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

Gary H. Posner, Poonsakdi Ploypradith, Michael H. Parker, Hardwin O'Dowd, Soon Hyung Woo, John Northrop, Mikhail Krasavin, Patrick Dolan, Thomas W. Kensler, Suji Xie, Theresa A. Shapiro

Research output: Contribution to journalArticlepeer-review

Abstract

Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

Original languageEnglish (US)
Pages (from-to)4275-4280
Number of pages6
JournalJournal of medicinal chemistry
Volume42
Issue number21
DOIs
StatePublished - 1999

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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