Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers. Bioorganic & medicinal chemistry [Bioorg Med Chem] Journal article | | Title | Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers. | | Author(s) | Slade D, Galal AM, Gul W, Radwan MM, Ahmed SA, Khan SI, Tekwani BL, Jacob MR, Ross SA, Elsohly MA | | Institution | National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA. | | Source | Bioorg Med Chem 2009 Oct 29. | | 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 [IC(50): 3.0-6.7nM (D6) and 4.2-5.9nM (W2)] were appreciably more active than artemisinin (1) [IC(50): 32.9nM (D6) and 42.5nM (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 (IC(50): 0.16 and 0.55muM, 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19879765 |
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