Antiprotozoal,anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers |
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| Authors: | Desmond Slade Ahmed M Galal Waseem Gul Mohamed M Radwan Safwat A Ahmed Shabana I Khan Babu L Tekwani Melissa R Jacob Samir A Ross Mahmoud A ElSohly |
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| Institution: | 1. National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA;2. ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford, MS 38655, USA;3. Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt;4. Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677, USA;5. Department of Pharmaceutics, School of Pharmacy, University of Mississippi, University, MS 38677, USA |
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| Abstract: | Nine dihydroartemisinin acetal dimers (6–14) with diversely functionalized linker units were synthesized and tested for in vitro antiprotozoal, anticancer and antimicrobial activity. Compounds 6, 7 and 11 IC50: 3.0–6.7 nM (D6) and 4.2–5.9 nM (W2)] were appreciably more active than artemisinin (1) IC50: 32.9 nM (D6) and 42.5 nM (W2)] against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of the malaria parasite, Plasmodium falciparum. Compounds 10, 13 and 14 displayed enhanced anticancer activity in a number of cell lines compared to the control drug, doxorubicin. The antifungal activity of 7 and 12 against Cryptococcus neoformans (IC50: 0.16 and 0.55 μM, respectively) was also higher compared to the control drug, amphotericin B. The antileishmanial and antibacterial activities were marginal. A number of dihydroartemisinin acetal monomers (15–17) and a trimer (18) were isolated as byproducts from the dimer synthesis and were also tested for biological activity. |
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