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); 75/256 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
January 22, 2015
Editor's Picks: Issue 02/2015
Editor's picks for issue 02: A Communication by Denny, Cobb and colleagues, and a Full Paper by Champy and co-workers report the latest discoveries for combating two different forms of leishmaniasis. Read more...
Recently Published Articles
- Synthesis and Biological Evaluation of Ferrocenylquinoline as a Potential Antileishmanial Agent
Md Yousuf, Debarati Mukherjee, Abhishek Pal, Somaditya Dey, Supratim Mandal, Dr. Chiranjib Pal and Dr. Susanta Adhikari
Article first published online: 23 JAN 2015 | DOI: 10.1002/cmdc.201402537
Ironing out leishmaniasis! Ferrocenylquinoline is a unique metallocene drug candidate that exhibits promising activity against Leismania donovani promastigotes (IC50: 15.26 μM) without cytotoxicity against host splenocytes. Treatment with this compound generated substantial amounts of reactive oxygen species followed by a depletion of reduced glutathione (GSH) and loss of membrane potential, leading to cell death. It inhibits intracellular amastigotes and also increases the levels of nitric oxide in infected macrophages.
- Drug Discovery Summit: 11th Swiss Course on Medicinal Chemistry
Priska Frei, Giulio Navarra, Christoph P. Sager, Marleen Silbermann, Dr. Norbert Varga and Eike-Christian Wamhoff
Article first published online: 14 JAN 2015 | DOI: 10.1002/cmdc.201402543
A summit amongst the summits: The 11th Swiss Course on Medicinal Chemistry was held in October 2014, again in the scenic setting of the Alps in Leysin, Switzerland. One hundred participants, mostly from industry, experienced a week of expert talks about numerous aspects of drug discovery and medicinal chemistry. In this conference report, we briefly summarize the essential topics of this event, while the most inspiring lectures are described in greater detail.
- Synthesis, Bioactivity, Docking and Molecular Dynamics Studies of Furan-Based Peptides as 20S Proteasome Inhibitors
Dr. Qi Sun, Dr. Bo Xu, Dr. Yan Niu, Fengrong Xu, Dr. Lei Liang, Dr. Chao Wang, Jiapei Yu, Gang Yan, Wei Wang, Dr. Hongwei Jin and Prof. Ping Xu
Article first published online: 13 JAN 2015 | DOI: 10.1002/cmdc.201402484
Sweet 17 vs. 20S: Seventeen furan-based peptidic molecules were designed and synthesized as 20S proteasome inhibitors, some of which showed potency and selectivity for the β5 subunit in both enzymatic and cell-based assays. Good antineoplastic activities were observed in multiple tumor cell lines. Docking and molecular dynamics simulations were also used to confirm a noncovalent binding mode.
- Natural Products as Zinc-Dependent Histone Deacetylase Inhibitors
Shuai Tan and Prof. Dr. Zhao-Peng Liu
Article first published online: 7 JAN 2015 | DOI: 10.1002/cmdc.201402460
As an inexhaustible source of novel chemotypes and pharmacophores, natural products play an invaluable role in the discovery of histone deacetylase (HDAC) inhibitors. Herein we provide a systematic introduction of natural HDAC inhibitors, with emphasis on their inhibitory potency, selectivity, biological activities, and their typical binding modes with HDACs.
- Novel Tacrine-Grafted Ugi Adducts as Multipotent Anti-Alzheimer Drugs: A Synthetic Renewal in Tacrine–Ferulic Acid Hybrids
Mohamed Benchekroun, Dr. Manuela Bartolini, Dr. Javier Egea, Dr. Alejandro Romero, Dr. Elena Soriano, Dr. Marc Pudlo, Vincent Luzet, Prof. Vincenza Andrisano, Dr. María-Luisa Jimeno, Dr. Manuela G. López, Sarah Wehle, Prof. Tijani Gharbi, Prof. Bernard Refouvelet, Lucía de Andrés, Clara Herrera-Arozamena, Prof. Barbara Monti, Prof. Maria Laura Bolognesi, Prof. María Isabel Rodríguez-Franco, Prof. Dr. Michael Decker, Prof. José Marco-Contelles and Dr. Lhassane Ismaili
Article first published online: 23 DEC 2014 | DOI: 10.1002/cmdc.201402409
Multicomponent reaction for a multifactorial disease: new multipotent tacrine–ferulic acid hybrids (TFAHs) were synthesized by the Ugi four-component reaction and evaluated in vitro for the treatment of Alzheimer’s disease. Among them, TFAH 10 n was found to selectively inhibit human butyrylcholinesterase. It also demonstrated good profiles in terms of toxicity, neuroprotection, antioxidant, and blood–brain barrier penetration.