Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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
September 23, 2014
Diederich to Give Bohlmann Lecture
Congratulations to François Diederich (ETH Zürich), who will be giving this year's Bohlmann Lecture at the Technische Universität Berlin in November. Diederich is a member of ChemMedChem's International Advisory Board, and recently reported on small-molecule inhibitors of trypanothione reductase.
Recently Published Articles
- Structure–Activity Relationship Study of Spider Polyamine Toxins as Inhibitors of Ionotropic Glutamate Receptors
Dr. Xiao-Feng Xiong, Dr. Mette H. Poulsen, Rama A. Hussein, Dr. Niels G. Nørager and Prof. Kristian Strømgaard
Article first published online: 29 SEP 2014 | DOI: 10.1002/cmdc.201402278
Selectivity woven in: Polyamine spider toxins from the orb-weaver spider Nephila clavata (Joro spider) were used as templates for a structure–activity relationship study. Compounds were evaluated at AMPA and NMDA subtypes of glutamate receptors, providing novel compounds with selectivity for AMPA receptors.
- Design and Synthesis of N-Acylated Aza-Goniothalamin Derivatives and Evaluation of Their in vitro and in vivo Antitumor Activity
Dr. Rosimeire Coura Barcelos, Dr. Julio Cezar Pastre, Dr. Débora Barbosa Vendramini-Costa, Vanessa Caixeta, Giovanna Barbarini Longato, Paula Araújo Monteiro, Prof. João Ernesto de Carvalho and Prof. Ronaldo Aloise Pilli
Article first published online: 26 SEP 2014 | DOI: 10.1002/cmdc.201402292
In vivo l′importance! We conducted antiproliferation assays of a library of aza derivatives of goniothalamin (1) against a panel of tumor cell lines. The most potent compound, 18, led to reactive oxygen species generation, apoptosis, and G2/M cell-cycle arrest in prostate PC-3 cells, but it failed to inhibit tumor growth. Surprisingly, aza-goniothalamin (2), which was shown to be much less toxic in vitro, inhibited Ehrlich tumor development in mice.
- Benzofuran–Chalcone Hybrids as Potential Multifunctional Agents against Alzheimer’s Disease: Synthesis and in vivo Studies with Transgenic Caenorhabditis elegans
Dr. Koneni V. Sashidhara, Ram K. Modukuri, Pooja Jadiya, Ranga Prasad Dodda, Dr. Manoj Kumar, Dr. Balasubramaniam Sridhar, Vikash Kumar, Rizwanul Haque, Dr. Mohammad Imran Siddiqi and Dr. Aamir Nazir
Article first published online: 24 SEP 2014 | DOI: 10.1002/cmdc.201402291
See elegant conjugates! To arrest multifaceted Alzheimer’s disease, a series of multifunctional benzofuran–chalcone hybrids were synthesized and bio-evaluated using transgenic C. elegans. These hybrid compounds potently reduced the aggregation of β-amyloid peptide, increased the acetylcholine levels, and provided protection against neurodegeneration.
- Design and Structural Analysis of Aromatic Inhibitors of Type II Dehydroquinase from Mycobacterium tuberculosis
Dr. Nigel I. Howard, Dr. Marcio V. B. Dias, Dr. Fabienne Peyrot, Dr. Liuhong Chen, Dr. Marco F. Schmidt, Prof. Tom L. Blundell and Prof. Chris Abell
Article first published online: 18 SEP 2014 | DOI: 10.1002/cmdc.201402298
Flattening the ring: A range of synthetically tractable biaryl inhibitors of type II dehydroquinase are described. They were designed with aromatic mimetics of the substrate’s non-aromatic six-membered ring. The compounds were used to investigate hydrogen bond acceptor/donor interaction patterns, aided with protein crystallographic studies.
- Structure–Activity Relationship of Tumor-Selective 5-Substituted 2-Amino-3-carboxymethylthiophene Derivatives
Dr. Joice Thomas, Dr. Alenka Jejcic, Peter Vervaeke, Prof. Romeo Romagnoli, Prof. Sandra Liekens, Prof. Jan Balzarini and Prof. Wim Dehaen
Article first published online: 18 SEP 2014 | DOI: 10.1002/cmdc.201402274
Cytostatic potential & tumor selectivity (TS) of a prototype 2-aminothiophene is retained by replacing the ethyl linker between the thiophene and the substituted aryl by a thioalkyl moiety. A SAR of this class of compounds revealed that the 4-alkylphenyl derivatives are more potent and selective anti-T-lymphoma/leukemia agents than the prototype.