Cover image for Vol. 9 Issue 12

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

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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November 22, 2014

The Most Accessed Are More Accessible

The Most Accessed Are More AccessibleChemMedChem's top-24 most-accessed articles of the last 12 months are now free to access! The diverse topics covered by these articles reflect the broad scope of the journal. Read more...

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Recently Published Articles

  1. Optimization of Diarylthiazole B-Raf Inhibitors: Identification of a Compound Endowed with High Oral Antitumor Activity, Mitigated hERG Inhibition, and Low Paradoxical Effect

    Dr. Maurizio Pulici, Dr. Gabriella Traquandi, Dr. Chiara Marchionni, Dr. Michele Modugno, Dr. Rosita Lupi, Nadia Amboldi, Dr. Elena Casale, Dr. Nicoletta Colombo, Luca Corti, Dr. Marina Fasolini, Dr. Fabio Gasparri, Wilma Pastori, Dr. Alessandra Scolaro, Dr. Daniele Donati, Dr. Eduard Felder, Dr. Arturo Galvani, Dr. Antonella Isacchi, Dr. Enrico Pesenti and Dr. Marina Ciomei

    Article first published online: 27 NOV 2014 | DOI: 10.1002/cmdc.201402424

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    Curb the paradoxical effect! Optimization of the potent B-Raf inhibitor 1 led to the identification of compound 20, which preserves the favorable in vitro and in vivo properties of 1, but is devoid of hERG liability. Intriguingly, compound 20 shows a markedly decreased “paradoxical” effect.

  2. Carborane-Derived Local Anesthetics are Isomer Dependent

    Dr. George R. Kracke, Dr. Monika R. VanGordon, Dr. Yulia V. Sevryugina, Dr. Peter J. Kueffer, Dr. Kuanysh Kabytaev, Dr. Satish S. Jalisatgi and Dr. M. Frederick Hawthorne

    Article first published online: 24 NOV 2014 | DOI: 10.1002/cmdc.201402369

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    Cage anesthetics: In a new local anesthetic, ortho-boronicaine, the phenyl ring of lidocaine was replaced with a highly symmetric, ortho-carborane cage. Hindlimb plantar injections in mice resulted in longer analgesic effects compared with lidocaine. ortho-Boronicaine exhibited greater analgesic efficacy compared with lidocaine or the meta- and para-carborane or adamantane derivatives.

  3. Design, Synthesis, and Biological Evaluation of Unconventional Aminopyrimidine, Aminopurine, and Amino-1,3,5-triazine Methyloxynucleosides

    Gloria Fernández-Cureses, Sonia de Castro, María-Luisa Jimeno, Jan Balzarini and Prof. María-José Camarasa

    Article first published online: 24 NOV 2014 | DOI: 10.1002/cmdc.201402465

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    Bucking convention: Herein we describe unconventional nucleosides that combine methyloxy-bound pyrimidines or purines with D-allitolyl, D-altritolyl groups as unusual ribofuranosyl mimics or 2,5-bis-hydroxymethyltetrahydrofuran as their dideoxy analogues. The pyrimidine nucleotides act as adenine nucleotide mimics. This class of unconventional nucleosides represents a new family of potential antiproliferative agents.

  4. The Discovery of a Highly Selective 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 Inhibitor that is Neuroprotective in an in vitro Parkinson’s Disease Model

    Dr. Paolo Di Fruscia, Emmanouil Zacharioudakis, Chang Liu, Dr. Sébastien Moniot, Sasiwan Laohasinnarong, Mattaka Khongkow, Ian F. Harrison, Konstantina Koltsida, Dr. Christopher R. Reynolds, Karin Schmidtkunz, Prof. Dr. Manfred Jung, Dr. Kathryn L. Chapman, Prof. Dr. Clemens Steegborn, Prof. David T. Dexter, Prof. Michael J. E. Sternberg, Prof. Eric W.-F. Lam and Dr. Matthew J. Fuchter

    Article first published online: 13 NOV 2014 | DOI: 10.1002/cmdc.201402431

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    Hit discovery: Through ligand-based virtual screening validation, ICL-SIRT078, a cell-active substrate-competitive SIRT2 inhibitor with a Ki value of 0.62±0.15 μM and more than 50-fold selectivity against SIRT1, 3 and 5 was identified. In addition, ICL-SIRT078 shows a significant neuroprotective effect in a lactacystin-induced model of Parkinsonian neuronal cell death in the N27 cell line. ICL-SIRT078, or an optimised derivative thereof, warrants further investigation as a neuroprotective agent in in vivo models of Parkinson’s disease.

  5. From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy

    Dr. Yves P. Auberson, Dr. Thomas Troxler, Dr. Xuechun Zhang, Dr. Charles R. Yang, Dr. Dominik Feuerbach, Dr. Yu-Chih Liu, Dr. Bharat Lagu, Dr. Mark Perrone, Dr. Lijun Lei, Dr. Xiaoxia Shen, Dr. Dushan Zhang, Dr. Chunxiu Wang, Dr. Tie-Lin Wang, Dr. Karin Briner and Dr. Mark G. Bock

    Article first published online: 12 NOV 2014 | DOI: 10.1002/cmdc.201402418

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    Better than caffeine! Simplification of the ergoline scaffold of the H3 receptor antagonist 1 led to a series of indoles with improved pharmacological properties and better chemical accessibility. A combined pharmacodynamic, pharmacokinetic, and receptor occupancy evaluation led to the selection of 15 m, the wakefulness-enhancing properties of which were demonstrated by EEG measurements in rats.