ChemMedChem
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim

Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.151
ISI Journal Citation Reports © Ranking: 2011: 17/59 (Chemistry Medicinal); 69/261 (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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June 13, 2013
The World's Most Influential Chemists
Peter Gölitz, Editor-in-Chief of Angewandte Chemie and former Editor for ChemMedChem, came up in discussions following a recent blog post listing some of history's most influential chemists. Check out the blog and discussion at ChemBark!
Recently Published Articles
- Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins
Dr. Reik Löser, Dr. Ralf Bergmann, Dr. Maxim Frizler, Dr. Birgit Mosch, Lilli Dombrowski, Manuela Kuchar, Prof. Dr. Jörg Steinbach, Prof. Dr. Michael Gütschow and Prof. Dr. Jens Pietzsch
Article first published online: 19 JUN 2013 | DOI: 10.1002/cmdc.201300135

Visualising cathepsins in tumours: Cysteine cathepsins are key players in tumour pathology. An azadipeptide nitrile with high affinity for cathepsins L, S, B, and K was labelled with fluorine-18 and investigated for its pharmacokinetic properties. PET imaging studies with tumour-bearing mice indicate the tumour accumulation of the probe and the potential of tumour targeting for this inhibitor class.
- Design of a Highly Selective and Potent Class of Non-planar Estrogen Receptor β Agonists
Dr. Henrik Sundén, Dr. Jian-Nong Ma, Prof. Lars K. Hansen, Dr. Anna-Lena Gustavsson, Dr. Ethan S. Burstein and Prof. Roger Olsson
Article first published online: 19 JUN 2013 | DOI: 10.1002/cmdc.201300175

Nothing flat about it: A T-shaped trans-SS diastereomer of 4-{3-fluoro-8-oxatricyclo[7.5.0.02,7]tetradeca-2,4,6-trien-1-yl}phenol (10) was found to be 1000-fold selective for ERβ over ERα. This compound exhibits ~10 nM potency and appears to be the first to take advantage of both conservative amino acid differences found in the α- and β-faces of the binding cavities of ERα and ERβ.
- Effect of Ester to Amide or N-Methylamide Substitution on Bacterial Membrane Depolarization and Antibacterial Activity of Novel Cyclic Lipopeptides
Dr. Nina Bionda, Renee M. Fleeman, Dr. Lindsey N. Shaw and Dr. Predrag Cudic
Article first published online: 18 JUN 2013 | DOI: 10.1002/cmdc.201300173

To be or not to be active: A cyclic lipodepsipeptide and its amide analogue can depolarize the cytoplasmic membranes of Gram-positive bacteria, whereas the N-methylamide analogue is inactive. Membrane depolarization does not correlate with bacterial cell lethality, suggesting that membrane-targeting activity is not the main mode of action for this class of antibacterial peptides.
- E-64c-Hydrazide: A Lead Structure for the Development of Irreversible Cathepsin C Inhibitors
Hanna Radzey, Markus Rethmeier, Dennis Klimpel, Maresa Grundhuber, Prof. Dr. Christian P. Sommerhoff and Priv.-Doz. Dr. Norbert Schaschke
Article first published online: 18 JUN 2013 | DOI: 10.1002/cmdc.201300093

Hitting the spot! Converting the carboxylic acid function of (2S,3S)-trans- epoxysuccinyl-L-leucylamido-3-methylbutane (E-64c), a synthetic broad-spectrum cysteine peptidase inhibitor, into the corresponding alkylhydrazide was identified as a key step to obtain potent irreversible cathepsin C inhibitors.
- Antiproliferative Activity, Cell Cycle, and Apoptosis Studies of a Series of 6-Substituted 9H-Purin-9-yl-pyridinium Derivatives on a Human Cervical Carcinoma Cell Line
Dr. Belén Rubio-Ruiz, Javier Ramos-Torrecillas, Fermín Capitán-Cañadas, Dr. Rosario Sánchez-Martín, Prof. Miguel Ángel Gallo, Prof. Antonio Espinosa, Prof. Concepción Ruiz, Dr. Ana Conejo-García and Prof. Antonio Entrena
Article first published online: 14 JUN 2013 | DOI: 10.1002/cmdc.201300171

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