© WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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
July 30, 2015
Gutenberg Research Award Goes to Kataoka
In recognition of his outstanding research accomplishments, ChemMedChem International Advisory Board member Kazunori Kataoka (University of Tokyo) has been awarded the 2015 Gutenberg Research Award by the Gutenberg Research School at the University of Mainz. Read more...
Recently Published Articles
- Exploring the Effects of Glycosylation and Etherification of the Side Chains of the Anticancer Drug Mitoxantrone
Pazit Shaul, Kfir B. Steinbuch, Eran Blacher, Prof. Reuven Stein and Dr. Micha Fridman
Article first published online: 31 JUL 2015 | DOI: 10.1002/cmdc.201500274
Sweets on the side: Derivatization of the antitumor drug mitoxantrone trough symmetric and asymmetric O-glycosylation or methyl etherification of the drugs’ side chains can improve DNA affinity, affects both in vitro and in vivo activity, and can inhibit the formation of potentially toxic metabolites.
- Application of MS Transport Assays to the Four Human γ-Aminobutyric Acid Transporters
Dr. Sebastian Schmitt, Dr. Georg Höfner and Prof. Dr. Klaus T. Wanner
Article first published online: 27 JUL 2015 | DOI: 10.1002/cmdc.201500254
MS Transport Assays: We describe the application of mass spectrometry based MS Transport Assays toward all four human γ-aminobutyric acid (GABA) transporters. Data for several inhibitors are presented and compared with state-of-the-art radiometric uptake assays. Moreover, a method to evaluate the inhibition curves by taking nonspecific transport into account is discussed in detail.
- Perspectives on Inhibiting β-Amyloid Aggregation through Structure-Based Drug Design
Pankaj Mishra, Dr. Senthil R. Ayyannan and Dr. Gautam Panda
Article first published online: 24 JUL 2015 | DOI: 10.1002/cmdc.201500215
New horizons in biospace: Although the utility of structure-based drug design principles in devising ways to inhibit β-amyloid aggregation with small molecules is still in its early stages, there are unexplored avenues that can be taken in this regard. Herein we discuss the current state of the art in this field of developing drugs to combat Alzheimer′s disease.
- Synthesis and Antiplasmodial Activity of Novel Chloroquine Analogues with Bulky Basic Side Chains
Dr. Bruno Tasso, Dr. Federica Novelli, Dr. Michele Tonelli, Dr. Anna Barteselli, Dr. Nicoletta Basilico, Dr. Silvia Parapini, Prof. Donatella Taramelli, Prof. Anna Sparatore and Prof. Fabio Sparatore
Article first published online: 24 JUL 2015 | DOI: 10.1002/cmdc.201500195
Where the action is: We synthesized a new series of chloroquine (CQ) analogues characterized by a side chain terminated with a bulky basic head group. Most compounds were found to be active against the D-10 (CQ-susceptible) and W-2 (CQ-resistant) strains of Plasmodium falciparum, with nanomolar and sub-micromolar IC50 values. Four derivatives appear to be of particular interest in terms of their high potency and low cytotoxicity.
- N′-Alkylaminosulfonyl Analogues of 6-Fluorobenzylideneindolinones with Desirable Physicochemical Profiles and Potent Growth Inhibitory Activities on Hepatocellular Carcinoma
Dr. Xiao Chen, Dr. Tianming Yang, Amudha Deivasigamani, Dr. Muthu K. Shanmugam, Prof. Kam-Man Hui, Prof. Gautam Sethi and Prof. Mei-Lin Go
Article first published online: 21 JUL 2015 | DOI: 10.1002/cmdc.201500235
The importance of being drug-like: When inserted into the benzylideneindolinone scaffold, the N′-alkylsulfonylamino group was found to improve aqueous solubility, PAMPA permeability, and growth inhibitory potency toward malignant cells. The most promising compound in this class, 3-12, is apoptogenic and inhibits the phosphorylation of several receptor tyrosine kinases, most prominently FGFR4 and HER3.