| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361920 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A series of dihydroartemisinin derivatives were synthesized via an aza-Michael addition reaction to a dihydroartemisinin-based acrylate and were evaluated for antiplasmodial and antitumor activity. The target compounds showed excellent antiplasmodial activity, with dihydroartemisinin derivatives 5, 7, 9 and 13 exhibiting IC50 values of ⩽10 nM against both D10 and Dd2 strains of Plasmodium falciparum. Derivative 4d was the most active against the HeLa cancer cell line, with an IC50 of 0.37 μM and the highest tumor specificity.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tzu-Shean Feng, Eric M. Guantai, Margo J. Nell, Constance E.J. van Rensburg, Heinrich C. Hoppe, Kelly Chibale,