82596-25-6Relevant articles and documents
Antimalarial and Antitumor Evaluation of Novel C-10 Non-Acetal Dimers of 10β-(2-Hydroxyethyl)deoxoartemisinin
Jeyadevan, J. Prince,Bray, Patrick G.,Chadwick, James,Mercer, Amy E.,Byrne, Aoife,Ward, Stephen A.,Park, B. Kevin,Williams, Dominic P.,Cosstick, Rick,Davies, Jill,Higson, Adrian P.,Irving, Ed,Posner, Gary H.,O'Neill, Paul M.
, p. 1290 - 1298 (2004)
Four series of C-10 non-acetal dimers were prepared from key trioxane alcohol 10β-(2-hydroxyethyl)deoxoartemisinin (9b). All of the dimers prepared displayed potent low nanomolar antimalarial activity versus the K1 and HB3 strains of Plasmodium falciparum
Synthesis of Artemisinin-Estrogen Hybrids Highly Active against HCMV, P. falciparum, and Cervical and Breast Cancer
Fr?hlich, Tony,Kiss, Anita,W?lfling, János,Mernyák, Erzsébet,Kulmány, ágnes E.,Minorics, Renáta,Zupkó, István,Leidenberger, Maria,Friedrich, Oliver,Kappes, Barbara,Hahn, Friedrich,Marschall, Manfred,Schneider, Gyula,Tsogoeva, Svetlana B.
, p. 1128 - 1133 (2018)
Artemisinin-estrogen hybrids were for the first time both synthesized and investigated for their in vitro biological activity against malaria parasites (Plasmodium falciparum 3D7), human cytomegalovirus (HCMV), and a panel of human malignant cells of gynecological origin containing breast (MCF7, MDA-MB-231, MDA-MB-361, T47D) and cervical tumor cell lines (HeLa, SiHa, C33A). In terms of antimalarial efficacy, hybrid 8 (EC50 = 3.8 nM) was about two times more active than its parent compound artesunic acid (7) (EC50 = 8.9 nM) as well as the standard drug chloroquine (EC50 = 9.8 nM) and was, therefore, comparable to the clinically used dihydroartemisinin (6) (EC50 = 2.4 nM). Furthermore, hybrids 9-12 showed a strong antiviral effect with EC50 values in the submicromolar range (0.22-0.38 μM) and thus possess profoundly stronger anti-HCMV activity (approximately factor 25) than the parent compound artesunic acid (7) (EC50 = 5.41 μM). These compounds also exerted a higher in vitro anti-HCMV efficacy than ganciclovir used as the standard of current antiviral treatment. In addition, hybrids 8-12 elicited substantially more pronounced growth inhibiting action on all cancer cell lines than their parent compounds and the reference drug cisplatin. The most potent agent, hybrid 12, exhibited submicromolar EC50 values (0.15-0.93 μM) against breast cancer and C33A cell lines.
Identification of HSP90 as a direct target of artemisinin for its anti-inflammatory activity: Via quantitative chemical proteomics
Wu, Guolin,Cheng, Bao,Qian, Hui,Ma, Shengming,Chen, Qin
, p. 6854 - 6859 (2019/07/22)
The anti-malarial drug artemisinin (ART) possesses potent anti-inflammatory activity, yet its underlying mechanism of action has remained elusive. Here we employed quantitative chemical proteomics to in situ profile the cellular targets of ART and identified heat shock protein 90 (HSP90) as a direct target. Further study revealed that ART suppressed the production of nitric oxide (NO) in macrophages via inhibiting the interaction between HSP90 and inducible NO synthase (iNOS).
Artemisin derivative and its preparation and use
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Paragraph 0166-0168; 0256-0258, (2016/10/08)
Provided are artemisinin derivatives of formula (I) or pharmaceutically acceptable salts thereof, or enantiomers, diastereomers, and racemic bodies thereof, and a pharmaceutical composition of the compounds, the preparation process and uses thereof. Artemisinin derivatives of formula (I) have excellent effects in the treatment of tumours.
