Antimalarial, Antiproliferative, and Antitumor Activities of Artemisinin-Derived, Chemically Robust, Trioxane Dimers
- 30 September 1999
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 42 (21) , 4275-4280
- https://doi.org/10.1021/jm990363d
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.Keywords
This publication has 10 references indexed in Scilit:
- Antimalarial artemisinin analogs. Synthesis via chemoselective CC bond formation and preliminary biological evaluationTetrahedron, 1999
- Vitamin DPublished by Springer Nature ,1999
- Trioxane dimers have potent antimalarial, antiproliferative and antitumor activities in vitroPublished by Elsevier ,1998
- Copper(I) Catalyzed Conjugate Addition of Grignard Reagents to Acrylic Acids: Homologation of Artemisinic Acid and Subsequent Conversion to 9-Substituted Artemisinin AnalogsTetrahedron Letters, 1997
- Preparation and Characterization of a New Artemisinin-Derived DimerJournal of Natural Products, 1996
- Broad Efforts Focus On Synthesis And Characterization Of PorphyrinsChemical & Engineering News, 1995
- Antimalarial Activity of Novel Ring-Contracted Artemisinin DerivativesJournal of Medicinal Chemistry, 1995
- Conversion of methyl ketones into terminal acetylenes and (E)-trisubstituted olefins of terpenoid originThe Journal of Organic Chemistry, 1980
- Notes- Preparation of m- and p-DiethynylbenzenesThe Journal of Organic Chemistry, 1960
- Oxidation of 2,6-Di-tert-butyl-4-methylphenol. The Structure of C14H22O31The Journal of Organic Chemistry, 1959