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Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/254 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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October 03, 2015

VIP: Small-Molecule T. brucei NMT Inhibitors

VIP: Small-Molecule T. brucei NMT InhibitorsHuman African trypanosomiasis (sleeping sickness) is endemic in sub-Saharan Africa. There are very few well-validated drug targets in the parasite Trypanosoma brucei, which causes the illness. Research groups from the University of Dundee (UK) played a substantial part in the validation of the enzyme N-myristoyltransferase (NMT) as a drug target in the parasite. Read more...

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    Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode

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    HATs off to diversity! Screening a diverse library against Trypanosoma brucei N-myristoyltransferase (NMT) identified hits based on thiazolidinone and benzomorpholine scaffolds. X-ray crystallography of these compounds bound to Leishmania major NMT revealed novel active site binding conformations. Using the structural information, the benzomorpholine scaffold was optimised to a blood–brain barrier penetrant compound with activity against TbNMT of <0.002 μM.

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    Article first published online: 21 SEP 2015 | DOI: 10.1002/cmdc.201500341

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    Quinolines against cancer: Quinoline-derived trifluoromethylated alcohols were synthesized by a C[BOND]H functionalization strategy. Three structurally diverse compounds (13) were evaluated for toxicity and anticancer activity. Compounds 2 and 3 were found to be effective anticancer agents in a zebrafish embryo model and in an in vitro cell proliferation assay. This study demonstrates the promising role of organofluorine compounds as potential therapeutic agents to treat cancer.