Copyright © 2015 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
March 24, 2015
2015 FMC in Marburg
The 2015 Frontiers in Medicinal Chemistry conference (www.gdch.de/medchem2015), organized by the German Chemical and Pharmaceutical Societies, together with the Swiss Chemical Society, was held last week at the Philipps University, Marburg (Germany). Read more...
Recently Published Articles
- New Approaches in the Design and Development of Cannabinoid Receptor Ligands: Multifunctional and Bivalent Compounds
Martin Nimczick and Prof. Dr. Michael Decker
Article first published online: 27 MAR 2015 | DOI: 10.1002/cmdc.201500041
Bivalent and multifunctional ligands acting at diverse biological targets were recently designed, synthesized and characterized for both cannabinoid receptor subtypes (CBRs). Due to their altered receptor binding and pharmacological profiles, they represent interesting tools to explore CBR functions and their interactions with other physiological systems. Moreover, this approach may bear therapeutic advantages in the therapy of CBR-related disorders, especially multifactorial diseases.
- Indanones As High-Potency Reversible Inhibitors of Monoamine Oxidase
Samantha Mostert, Prof. Anél Petzer and Prof. Jacobus P. Petzer
Article first published online: 27 MAR 2015 | DOI: 10.1002/cmdc.201500059
Location, location, location: C6-substituted indanones 3 are highly potent and selective MAO-B inhibitors, with IC50 values ranging from 0.001–0.030 μM. C5-substituted indanone (2) and indane (4) derivatives are comparatively weaker MAO-B inhibitors. C6-substituted indanones are thus promising leads for the design of therapies for Parkinson’s disease.
- Indolo[3,2-c]quinoline G-Quadruplex Stabilizers: a Structural Analysis of Binding to the Human Telomeric G-Quadruplex
Dr. João Lavrado, Dr. Stephan A. Ohnmacht, Dr. Isabel Correia, Clara Leitão, Sílvia Pisco, Dr. Mekala Gunaratnam, Prof. Rui Moreira, Prof. Stephen Neidle, Dr. Daniel J. V. A. dos Santos and Dr. Alexandra Paulo
Article first published online: 26 MAR 2015 | DOI: 10.1002/cmdc.201500067
A much higher IQ: We report indolo[3,2-c]quinoline (IQc) derivatives with two weak basic side chains as potent and selective human telomeric (HT) G-quadruplex (G4) stabilizers. Biophysical data show that stabilization involves the binding of two ligands which induces a conformational rearrangement of the HT G4 structure. Moreover, selected derivatives showed selective antiproliferative activity toward human malignant cell lines.
- Investigation of Structure–Activity Relationships of Synthetic Anti-Gonadotropin Releasing Hormone Vaccine Candidates
Chenghung Chang, Dr. Pegah Varamini, Ashwini Kumar Giddam, Dr. Friederike M. Mansfeld, Prof. Dr. Michael J. D'Occhio and Prof. Dr. Istvan Toth
Article first published online: 25 MAR 2015 | DOI: 10.1002/cmdc.201500036
Gonadotropin-releasing hormone (GnRH) vaccine candidates were found to produce effective anti-GnRH-specific antibodies, resulting in significant inhibition of folliculogenesis in mouse ovaries. The compounds were efficiently taken up by antigen-presenting cells with significant immunogenicity without the need for an external adjuvant.
- Platinum(II) as Bifunctional Linker in Antibody–Drug Conjugate Formation: Coupling of a 4-Nitrobenzo-2-oxa-1,3-diazole Fluorophore to Trastuzumab as a Model
Dr. Dennis C. J. Waalboer, Joey A. Muns, Dr. Niels J. Sijbrandi, Dr. Richard B. M. Schasfoort, Dr. Rob Haselberg, Prof. Dr. Govert W. Somsen, Dr. Hendrik-Jan Houthoff and Prof. Dr. Guus A. M. S. van Dongen
Article first published online: 25 MAR 2015 | DOI: 10.1002/cmdc.201402496
The missing link: [Pt(en)Cl2] was successfully used as a bifunctional linker in the conjugation of a variety of functionalized 4-nitrobenzo-2-oxa-1,3-diazole fluorophores to the model monoclonal antibody trastuzumab. The effect of ligand type, salt, and excipients on conjugation efficiency was explored. Conjugation was shown not to change the affinity of trastuzumab for its cognate antigen, Her2.