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Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction |
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| Authors: | Feng Tzu-Shean Guantai Eric M Nell Margo J van Rensburg Constance E J Hoppe Heinrich C Chibale Kelly |
| Affiliation: | a Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa b Division of Pharmacology, University of Cape Town, Observatory 7925, South Africa c Division of Pharmacology, School of Pharmacy, University of Nairobi, Box 19676-00202, Kenya d Department of Pharmacology, University of Pretoria, Hatfield 0028, South Africa e Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa |
| 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. |
| Keywords: | Anticancer Antiplasmodial Aza-Michael addition reaction Chloroquinoline Dihydroartemisinin |
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