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

Authors
Posner, GH Ploypradith, P Parker, MH O'Dowd, H Woo, SH Northrop, J Krasavin, M Dolan, P Kensler, TW Xie, SJ Shapiro, TA
Citation
Gh. Posner et al., Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers, J MED CHEM, 42(21), 1999, pp. 4275-4280
Citations number
28
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
42
Issue
21
Year of publication
1999
Pages
4275 - 4280
Database
ISI
SICI code
0022-2623(19991021)42:21<4275:AAAAAO>2.0.ZU;2-2
Abstract
Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) we re prepared as dimers using some novel chemistry. As designed, each dimer w as 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 inh ibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.