ChemMedChem

Cover image for Vol. 9 Issue 8

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (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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July 05, 2014

Six Outstanding Posters!

Six Outstanding Posters!Congratulations to the six poster prize winners at last month's Metals in Medicine Gordon Research Conference, Defining the Future of Medicinal Inorganic Chemistry (June 22–27, Andover, NH, USA): Stacy Barnaby (front left, Northwestern University) Probing the Inherent Stability of siRNA Immobilized on Nanoparticle Constructs; Insiya Fidai (front middle, The Ohio State University) Inactivation of Sortase A Mediated by Metal ATCUN Complexes; Steve Po-Yam Li (back left, City University of Hong Kong) Mitochondria-Targeting Cyclometalated Iridium(III) Poly(ethylene glycol) (PEG) Complexes with Tunable Photodynamic Activity; Martin Ross (front right, The Ohio State University) Insights into the Reactivity and Binding of Catalytic Metallodrugs Targeting the IRES RNA of HCV; Kevin Siters (back right, SUNY Buffalo) Targeting the Human Telomeric G-Quadruplex Using Modified ZnII Macrocycles; and Lindsey van Gemeren (back middle, University of Birmingham) Multimodal Imaging Agents for in vivo Cell Tracking.

The poster prizes were sponsored by ChemMedChem and EurJIC; thanks to conference co-chairs Alan B. Packard and Michael J. Hannon, and vice co-chairs Katherine J. Franz and Nils Metzler-Nolte. For more outstanding inorganic medicinal chemistry, see ChemMedChemIssue 06!

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    Article first published online: 19 AUG 2014 | DOI: 10.1002/cmdc.201402252

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    JAK of all trades: A library of tofacitinib bioisosteres was prepared and tested against Janus kinases (JAKs). The hinge binding motif in all of the studied compounds was replaced by a variety of heterocycles mimicking the 7H-pyrrolo[2,3-d]pyrimidine pharmacophore. In view of the promising expectations obtained from molecular modeling, most of the compounds proved to be poorly active, yet crucial structure–activity relationships were deduced.

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    Inhibitors that compete! Carboxymethylsulfonyl-modified nucleosides with xylo and arabino configurations were synthesized in order to assess their inhibitory properties against RNase A. Experimental and theoretical studies established the arabinocytidine analogue as the most effective competitive inhibitor due to proper recognition of the B1 and P1 subsites of the enzyme.

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    A key target: Fungal infections, parasitic diseases, and cancers remain three major global health problems. N-Myristoyltransferase (NMT) has been identified as a novel and promising target for antifungal, antiparasitic, and anticancer agents. This review highlights recent advances in the discovery of NMT inhibitors, with particular focus on their activities, structure–activity relationships, and mechanisms.

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