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Table 2 Most active compounds tested by St Jude’s Children’s Research Hospital

From: Repositioning: the fast track to new anti-malarial medicines?

Compound Class (therapeutic area) EC503D7 (μM) EC50K1 (μM)
Methylene blue Nitric oxide/guanylate cyclase inhibitor (various) <0.0003 (NA) <0.0003 (NA)
Dactinomycin Nucleoside reverse transcriptase inhibitor (oncology) 0.0009 (0, 0.13) 0.001 (0.0003, 0.006)
Sulfamerazine Dihydrofolate synthetase inhibitor (anti-infective) 0.01 (0.01, 0.01) 0.01 (0.01, 0.01)
Methotrexate Dihydrofolate reductase inhibitor (oncology) 0.01 (0.009, 0.01) 0.02 (0.01, 0.02)
Bortezomib Proteasome inhibitor (oncology) 0.02 (0.01, 0.04) 0.08 (0.07, 0.09)
Thiothixene Post-synaptic receptor agonista (anti-psychotic) 0.04 (0, 233.71) 0.02 (0.01, 0.05)
Dequalinium Anti-septic 0.06 (0.002, 1.53) 0.06 (0.03, 0.12)
Doxorubicin Topoisomerase II inhibitor, DNA intercalating agent (oncology) 0.21 (0.16, 0.27) 0.20 (0.14, 0.30)
Pentamidine Inhibition of DNA, RNA, phospholipid and protein synthesisb (anti-infective) 0.22 (0.18, 0.27) 0.05 (0.04, 0.06)
Bosutinib Tyrosine kinase inhibitor (oncology) 0.22 (0.016, 3.11) 0.65 (0.36, 1.19)
Aminopterin Dihydrofolate reductase inhibitor (oncology) 0.32 (0.30, 0.33) 1.25 (1.11, 1.41)
Midostaurin Multi-kinase inhibitor (oncology) 0.35 (0.17, 0.71) 0.15 (0.13, 0.17)
Lestaurtinib FMS-like tyrosine kinase 3 inhibitor (oncology) 0.49 (0.28, 0.84) 0.34 (0.29, 0.41)
Demecarium Cholinesterase inhibitor (ophthalmology) 0.51 (0.45, 0.57) 0.30 (0.26, 0.36)
Cyproterone Steroidal anti-androgen (oncology) 0.56 (0.54, 0.58) 0.89 (0, 1501.50)
Lapatinib Tyrosine kinase inhibitor (oncology) 0.56 (0.39, 0.80) >7.37 (NA)
Pimozide Dopamine receptor blocker (anti-psychotic) 0.70 (0.44, 1.11) >12.76 (NA)
Pravastatin HMG-CoA reductase inhibitor (anti-cholesterol) 0.75 (0.51, 1.09) 0.12 (0.10, 0.15)
Dipyrone NSAIDb (pain) 0.84 (0.71, 0.98) 0.50 (0.21, 1.16)
Mitomycin Inhibition of DNA synthesis (oncology) 0.97 (0.81, 1.17) 0.51 (0.45, 0.57)
Propafenone Sodium channel modulator (cardiology) 1.22 (0.58, 2.55) 0.33 (0.31, 0.34)
Cyclosporin A Immune suppressant (oncology) 1.23 (1.06, 1.44) 0.87 (0.62, 1.23)
Vorinostat Histone deacetylase inhibitor (oncology) 1.47 (1.17, 1.84) 0.84 (0.76, 0.93)
Sorafenib Multi-kinase inhibitor (oncology) 2.71 (2.4, 3.1) 0.88 (0.7, 1.1)
  1. NA, not available. EC50 values are shown as mean (95% CI). Compounds with an EC50 < 1 μM against either P. falciparum strain are shown. Relevant results from all compound sets tested at SJCRH are shown. Where compounds were duplicated across the consolidated test set, the results with the most potent in vitro activity are shown. Known anti-malarial drugs have been excluded.
  2. aAgonist of dopaminergic-receptors, serotonergic-receptors, histaminergic-receptors, alpha1/alpha2-receptors, and muscarinic (cholinergic) M1/M2-receptors.
  3. bMechanism unknown.
  4. SYBR®I fluorescence assay for activity against P. falciparum strains 3D7 and K1.