Published in J Med Chem on June 03, 2004
Natural products: a continuing source of novel drug leads. Biochim Biophys Acta (2013) 4.12
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci U S A (2011) 3.23
Artemisinin activity against Plasmodium falciparum requires hemoglobin uptake and digestion. Proc Natl Acad Sci U S A (2011) 2.94
Malaria biology and disease pathogenesis: insights for new treatments. Nat Med (2013) 2.38
Artemisinin-resistant malaria: research challenges, opportunities, and public health implications. Am J Trop Med Hyg (2012) 1.97
The antimalarial drug artemisinin alkylates heme in infected mice. Proc Natl Acad Sci U S A (2005) 1.81
Artemisinins. Postgrad Med J (2005) 1.66
Artemisinin directly targets malarial mitochondria through its specific mitochondrial activation. PLoS One (2010) 1.45
Accumulation of artemisinin trioxane derivatives within neutral lipids of Plasmodium falciparum malaria parasites is endoperoxide-dependent. Biochem Pharmacol (2008) 1.35
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). Antimicrob Agents Chemother (2007) 1.35
In vitro inhibition of Toxoplasma gondii by four new derivatives of artemisinin. Antimicrob Agents Chemother (2006) 1.31
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells. J Med Chem (2009) 1.23
Selection of a trioxaquine as an antimalarial drug candidate. Proc Natl Acad Sci U S A (2008) 1.18
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals. Antimicrob Agents Chemother (2009) 1.15
Endoperoxide synthesis by photocatalytic aerobic [2 + 2 + 2] cycloadditions. Org Lett (2012) 1.15
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance. Antimicrob Agents Chemother (2010) 1.14
The role of heme and the mitochondrion in the chemical and molecular mechanisms of mammalian cell death induced by the artemisinin antimalarials. J Biol Chem (2010) 1.13
Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines. J Med Chem (2008) 1.09
Artemisinin dimer anticancer activity correlates with heme-catalyzed reactive oxygen species generation and endoplasmic reticulum stress induction. Int J Cancer (2009) 1.06
Reaction of artemisinin with haemoglobin: implications for antimalarial activity. Biochem J (2005) 1.01
Synthesis and antimalarial activity of new 4-amino-7-chloroquinolyl amides, sulfonamides, ureas and thioureas. Bioorg Med Chem (2008) 1.00
Dihydroartemisinin enhances Apo2L/TRAIL-mediated apoptosis in pancreatic cancer cells via ROS-mediated up-regulation of death receptor 5. PLoS One (2012) 0.99
Controlled oxidation of remote sp3 C-H bonds in artemisinin via P450 catalysts with fine-tuned regio- and stereoselectivity. J Am Chem Soc (2012) 0.99
The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives. Chem Rev (2013) 0.98
Antimalarial iron chelator, FBS0701, shows asexual and gametocyte Plasmodium falciparum activity and single oral dose cure in a murine malaria model. PLoS One (2012) 0.96
Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum. Bioorg Med Chem (2005) 0.95
A single, low, oral dose of a 5-carbon-linked trioxane dimer orthoester plus mefloquine cures malaria-infected mice. Bioorg Med Chem Lett (2010) 0.95
Microbial transformation of artemisinin to 5-hydroxyartemisinin by Eurotium amstelodami and Aspergillus niger. J Ind Microbiol Biotechnol (2005) 0.94
Artemisinin Action and Resistance in Plasmodium falciparum. Trends Parasitol (2016) 0.93
Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes. J Med Chem (2011) 0.92
The antimalarial trioxaquine DU1301 alkylates heme in malaria-infected mice. Antimicrob Agents Chemother (2008) 0.92
Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii. J Med Chem (2010) 0.91
Recent progress in the development of anti-malarial quinolones. Malar J (2014) 0.90
Anti-plasmodium activity of angiotensin II and related synthetic peptides. PLoS One (2008) 0.90
Nox4-dependent ROS modulation by amino endoperoxides to induce apoptosis in cancer cells. Cell Death Dis (2013) 0.90
Efficient and stereocontrolled synthesis of 1,2,4-trioxolanes useful for ferrous iron-dependent drug delivery. Org Lett (2014) 0.87
Synthesis of five- and six-membered cyclic organic peroxides: Key transformations into peroxide ring-retaining products. Beilstein J Org Chem (2014) 0.87
Drug delivery to the malaria parasite using an arterolane-like scaffold. ChemMedChem (2014) 0.85
Ferrous iron-dependent delivery of therapeutic agents to the malaria parasite. Future Med Chem (2012) 0.83
Artemisinin effectiveness in erythrocytes is reduced by heme and heme-containing proteins. Biochem Pharmacol (2007) 0.83
Novel multiarm polyethylene glycol-dihydroartemisinin conjugates enhancing therapeutic efficacy in non-small-cell lung cancer. Sci Rep (2014) 0.83
Antimalarial Preclinical Drug Development: A Single Oral Dose of A 5-Carbon-linked Trioxane Dimer Plus Mefloquine Cures Malaria-Infected Mice. Drug Dev Res (2009) 0.82
Stability of peroxide antimalarials in the presence of human hemoglobin. Antimicrob Agents Chemother (2009) 0.81
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition. Bioorg Med Chem Lett (2009) 0.81
Real-time imaging of the intracellular glutathione redox potential in the malaria parasite Plasmodium falciparum. PLoS Pathog (2013) 0.80
Self-assembled targeted nanoparticles based on transferrin-modified eight-arm-polyethylene glycol-dihydroartemisinin conjugate. Sci Rep (2016) 0.80
Plasmodium drug targets outside the genetic control of the parasite. Curr Pharm Des (2013) 0.79
Novel endoperoxide-based transmission-blocking antimalarials with liver- and blood-schizontocidal activities. ACS Med Chem Lett (2013) 0.79
Recent advances in the search for antiviral agents against human papillomaviruses. Antivir Ther (2007) 0.79
Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria. ACS Med Chem Lett (2015) 0.77
Two distinct and competitive pathways confer the cellcidal actions of artemisinins. Microb Cell (2015) 0.77
Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers). Antimicrob Agents Chemother (2007) 0.76
The molecular and cellular action properties of artemisinins: what has yeast told us? Microb Cell (2016) 0.76
Untargeted Proteomics and Systems-Based Mechanistic Investigation of Artesunate in Human Bronchial Epithelial Cells. Chem Res Toxicol (2015) 0.76
Alkylating ability of artemisinin after Cu(I)-induced activation. J Biol Inorg Chem (2009) 0.76
A reactivity-based probe of the intracellular labile ferrous iron pool. Nat Chem Biol (2016) 0.76
Timing is everything for artemisinin action. Proc Natl Acad Sci U S A (2013) 0.76
Pharmacokinetics of the Antischistosomal Lead Ozonide OZ418 in Uninfected Mice Determined by Liquid Chromatography-Tandem Mass Spectrometry. Antimicrob Agents Chemother (2016) 0.76
Synthesis and antimalarial activity of 3,3-spiroanellated 5,6-disubstituted 1,2,4-trioxanes. ACS Med Chem Lett (2012) 0.75
Preparation and characterization of micronized artemisinin via a Rapid Expansion of Supercritical Solutions (RESS) Method. Int J Mol Sci (2012) 0.75
Synthesis of spiroannulated and 3-arylated 1,2,4-trioxanes from mesitylol and methyl 4-hydroxytiglate by photooxygenation and peroxyacetalization. Beilstein J Org Chem (2010) 0.75
A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models. J Med Chem (2016) 0.75
Endoperoxide antimalarials: development, structural diversity and pharmacodynamic aspects with reference to 1,2,4-trioxane-based structural scaffold. Drug Des Devel Ther (2016) 0.75
Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine. Pharmaceuticals (Basel) (2009) 0.75
Mixed steroidal tetraoxanes induce apoptotic cell death in tumor cells. Invest New Drugs (2008) 0.75
Comparative analysis of the safety and tolerability of fixed-dose artesunate/amodiaquine versus artemether/lumefantrine combinations for uncomplicated falciparum malaria in pregnancy: a randomized open label study. Clin Pharmacol (2017) 0.75
Accumulation of artemisinin trioxane derivatives within neutral lipids of Plasmodium falciparum malaria parasites is endoperoxide-dependent. Biochem Pharmacol (2008) 1.35
In vitro inhibition of Toxoplasma gondii by four new derivatives of artemisinin. Antimicrob Agents Chemother (2006) 1.31
Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activity. J Med Chem (2006) 1.25
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells. J Med Chem (2009) 1.23
Vitamin D and vitamin D analogs as cancer chemopreventive agents. Nutr Rev (2003) 1.16
Malaria-infected mice live until at least day 30 after a new monomeric trioxane combined with mefloquine are administered together in a single low oral dose. J Med Chem (2009) 1.04
Effect of artemisinins and other endoperoxides on nitric oxide-related signaling pathway in RAW 264.7 mouse macrophage cells. Nitric Oxide (2008) 1.02
Recombinant luciferase-expressing human cytomegalovirus (CMV) for evaluation of CMV inhibitors. Virol J (2011) 1.01
Artemisinin derivatives inhibit Toxoplasma gondii in vitro at multiple steps in the lytic cycle. J Antimicrob Chemother (2008) 1.00
Biological mechanisms of action of novel C-10 non-acetal trioxane dimers in prostate cancer cell lines. J Med Chem (2006) 1.00
An artemisinin-derived dimer has highly potent anti-cytomegalovirus (CMV) and anti-cancer activities. PLoS One (2011) 1.00
A single, low, oral dose of a 5-carbon-linked trioxane dimer orthoester plus mefloquine cures malaria-infected mice. Bioorg Med Chem Lett (2010) 0.95
Apc(MIN) modulation of vitamin D secosteroid growth control. Carcinogenesis (2010) 0.94
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3). J Med Chem (2004) 0.94
Antimalarial and antitumor evaluation of novel C-10 non-acetal dimers of 10beta-(2-hydroxyethyl)deoxoartemisinin. J Med Chem (2004) 0.92
Artemisinin-derived dimer diphenyl phosphate is an irreversible inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother (2012) 0.91
Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii. J Med Chem (2010) 0.91
Vitamin D receptor modulates the neoplastic phenotype through antagonistic growth regulatory signals. Mol Carcinog (2009) 0.90
Cyclopentanone ring expansion leading to functionalized delta-lactams: short synthesis of simple sedum alkaloids. Org Lett (2007) 0.90
Antimalarial chemotherapeutic peroxides: artemisinin, yingzhaosu A and related compounds. Int J Parasitol (2002) 0.89
Enantiomeric 1,2,4-trioxanes display equivalent in vitro antimalarial activity versus Plasmodium falciparum malaria parasites: implications for the molecular mechanism of action of the artemisinins. Chembiochem (2005) 0.88
Differentiation-inducing potency of the seco-steroid JK-1624F2-2 can be increased by combination with an antioxidant and a p38MAPK inhibitor which upregulates the JNK pathway. J Steroid Biochem Mol Biol (2007) 0.88
Anticancer effects of the novel 1alpha, 25-dihydroxyvitamin D3 hybrid analog QW1624F2-2 in human neuroblastoma. J Cell Biochem (2006) 0.88
Estrogenic activity of glabridin and glabrene from licorice roots on human osteoblasts and prepubertal rat skeletal tissues. J Steroid Biochem Mol Biol (2004) 0.87
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs. J Med Chem (2013) 0.85
Malaria-infected mice are completely cured by one 6 mg/kg oral dose of a new monomeric trioxane sulfide combined with mefloquine. J Med Chem (2011) 0.85
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides. J Med Chem (2003) 0.85
Antiproliferative, low-calcemic, fluorinated sulfone analogs of 1alpha,25-dihydroxyvitamin D3: chemical synthesis and biological evaluation. Bioorg Med Chem (2007) 0.84
Asymmetric, organocatalytic, three-step synthesis of gamma-hydroxy-(E)-alpha,beta-unsaturated sulfones and esters. Org Lett (2008) 0.84
Antitumor effects of two less-calcemic vitamin D analogs (Paricalcitol and QW-1624F2-2) in squamous cell carcinoma cells. Oncology (2007) 0.83
Antimalarial Preclinical Drug Development: A Single Oral Dose of A 5-Carbon-linked Trioxane Dimer Plus Mefloquine Cures Malaria-Infected Mice. Drug Dev Res (2009) 0.82
A 24-phenylsulfone analog of vitamin D inhibits 1alpha,25-dihydroxyvitamin D(3) degradation in vitamin D metabolism-competent cells. J Pharmacol Exp Ther (2006) 0.81
A-ring hydroxymethyl 19-nor analogs of the natural hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and preliminary biological evaluation. Bioorg Med Chem (2005) 0.81
A non-calcemic Vitamin D analog modulates both nuclear and putative membranal estrogen receptors in cultured human vascular smooth muscle cells. J Steroid Biochem Mol Biol (2004) 0.80
In vitro combination of anti-cytomegalovirus compounds acting through different targets: role of the slope parameter and insights into mechanisms of Action. Antimicrob Agents Chemother (2013) 0.80
Unique and highly selective anticytomegalovirus activities of artemisinin-derived dimer diphenyl phosphate stem from combination of dimer unit and a diphenyl phosphate moiety. Antimicrob Agents Chemother (2013) 0.80
Inhibition of prostate cancer-meditated osteoblastic bone lesions by the low-calcemic analog 1alpha-hydroxymethyl-16-ene-26,27-bishomo-25-hydroxy vitamin D3. J Steroid Biochem Mol Biol (2005) 0.79
Malaria-infected mice live until at least day 30 after a new artemisinin-derived thioacetal thiocarbonate combined with mefloquine are administered together in a single, low, oral dose. J Med Chem (2012) 0.79
Cyanocuprates convert carboxylic acids directly into ketones. Org Lett (2011) 0.79
Vitamin D analogs as modulators of vitamin D receptor action. Curr Top Med Chem (2003) 0.79
QW-1624F2-2, a synthetic analogue of 1,25-dihydroxyvitamin D3, enhances the response to other deltanoids and suppresses the invasiveness of human metastatic breast tumor cells. Mol Cancer Ther (2006) 0.79
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation. J Med Chem (2006) 0.78
α-Chloro-β,γ-ethylenic esters: enantiocontrolled synthesis and substitutions. Org Lett (2010) 0.78
Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: a structure-activity study. Bioorg Med Chem (2013) 0.78
Asymmetric, organocatalytic, three-step synthesis of alpha-hydroxy-(E)-beta,gamma-unsaturated esters. Org Lett (2010) 0.78
Highly stereocontrolled and regiocontrolled syntheses of 2,3,4-trisubstituted alkanoates and lactones. J Org Chem (2011) 0.78
'Novel alkyl side chain sulfone 1alpha,25-dihydroxyvitamin D3 analogs: a comparison of in vitro antiproliferative activities and in vivo calcemic activities'. Bioorg Med Chem (2009) 0.78
Unexpected steric effects of "remote" alkyl groups on the rate of conjugate additions to alkyl alpha,beta-ethylenic sulfones, sulfoxides, and esters. J Org Chem (2007) 0.78
Malaria: new chemotherapeutic peroxide drugs. Mini Rev Med Chem (2002) 0.77
A thiazole derivative of artemisinin moderately reduces Toxoplasma gondii cyst burden in infected mice. J Parasitol (2014) 0.77
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation. J Med Chem (2007) 0.77
Treatment with non-hypercalcemic analogs of 1,25-dihydroxyvitamin D3 increases responsiveness to 17beta-estradiol, dihydrotestosterone or raloxifene in primary human osteoblasts. J Steroid Biochem Mol Biol (2004) 0.77
Less calcemic Vitamin D analogs enhance creatine kinase specific activity and modulate responsiveness to gonadal steroids in the vasculature. J Steroid Biochem Mol Biol (2006) 0.77
Highly antiproliferative, low-calcemic, side-chain amide and hydroxamate analogs of the hormone 1alpha,25-dihydroxyvitamin D3. Bioorg Med Chem (2006) 0.76
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases(). Medchemcomm (2012) 0.76
Modulation of the response to estradiol-17beta of rat vascular tissues by a non calcemic vitamin D analog. J Steroid Biochem Mol Biol (2004) 0.76
Responsiveness to phytoestrogens in primary human osteoblasts is modulated differentially by a "less-calcemic" analog of 1,25 dihydroxyvitamin D(3): JK 1624F(2)-2 (JKF). J Steroid Biochem Mol Biol (2006) 0.76
Titanium-promoted stereoselective synthesis of hydroindolones from p-quinamines by domino conjugate additions. Angew Chem Int Ed Engl (2002) 0.76
Differential photoprotective effects of 1,25-dihydroxyvitamin D3 and a low calcaemic deltanoid. Photochem Photobiol Sci (2012) 0.76
Three-component, one-flask synthesis of rhodanines (thiazolidinones). J Org Chem (2011) 0.75
Modulation of response to estrogens in cultured human female bone cells by a non-calcemic Vitamin D analog: changes in nuclear and membranal binding. J Steroid Biochem Mol Biol (2004) 0.75