Cover image for Vol. 10 Issue 4

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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March 28, 2015

Editor's Picks: Issue 04/2015

Editor's Picks: Issue 04/2015Editor's picks for issue 04: This month, two Full Papers by Markus Pietsch and co-workers and Michael Wiese and colleagues describe various ways to overcome drug resistance in cancer using small-molecule therapeutics. Read more...

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  1. Protein Flexibility in Drug Discovery: From Theory to Computation

    Dr. Rosa Buonfiglio, Prof. Maurizio Recanatini and Dr. Matteo Masetti

    Article first published online: 17 APR 2015 | DOI: 10.1002/cmdc.201500086

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    Flex and stretch: The mechanisms of biomolecular recognition are strongly coupled to the intrinsic dynamic of proteins. Accounting for protein flexibility in structure-based drug discovery is still a challenging task. This review describes the most important computational methods to model protein flexibility in light of the recent advances in the theories of biomolecular recognition.

  2. 2-Substituted 6-(Het)aryl-7-deazapurine Ribonucleosides: Synthesis, Inhibition of Adenosine Kinases, and Antimycobacterial Activity

    Dr. Vincent Malnuit, Dr. Lenka Poštová Slavětínská, Dr. Petr Nauš, Dr. Petr Džubák, Prof. Marián Hajdúch, Dr. Jiřina Stolaříková, Dr. Jan Snášel, Dr. Iva Pichová and Prof. Dr. Michal Hocek

    Article first published online: 16 APR 2015 | DOI: 10.1002/cmdc.201500081

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    Specific for Mtb ADK: A series of diverse 2-substituted 6-heteroaryl-7-deazapurine ribonucleosides was prepared and the title compounds were found to be potent and selective inhibitors of Mycobacterium tuberculosis (but not human) adenosine kinase. Unfortunately, their antimycobacterial activity was observed to be weak, probably due to poor uptake or parallel biosynthesis.

  3. Toll-Like Receptor 7 Inactive Ligands Enhanced Cytokine Induction by Conjugation to Weak Antigens

    Dr. Dong Gao, Dr. Yuwen Diao, Wang Li, Dr. Ningning Gao, Dr. Yu Liu, Zhulin Wang, Prof. Wenqi Jiang and Prof. Guangyi Jin

    Article first published online: 16 APR 2015 | DOI: 10.1002/cmdc.201500088

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    Awakened by conjugation: We revealed that the conjugates between antigens and a series of inactive adenine analogues can trigger a profound induction of inflammatory cytokines. The free adenine analogues themselves lack such immunostimulatory activity and agonism toward toll-like receptors 7/8, making them better suited as inert adjuvants with decreased side effects.

  4. Oxidative Metabolism of Ferrocene Analogues of Tamoxifen: Characterization and Antiproliferative Activities of the Metabolites

    Dr. Marie-Aude Richard, Dr. Didier Hamels, Dr. Pascal Pigeon, Dr. Siden Top, Dr. Patrick M. Dansette, Hui Zhi Shirley Lee, Dr. Anne Vessières, Dr. Daniel Mansuy and Prof. Gérard Jaouen

    Article first published online: 16 APR 2015 | DOI: 10.1002/cmdc.201500075

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    Allez Paris FC! Ferrociphenols (FCs) show antitumor activities against estrogen-indepedent breast cancer cells. Their oxidation by rat and human liver microsomes leads to the formation of three main classes of metabolites: quinone methides (QMs), cyclic indene products (CPs), and allylic alcohols (AAs). Some of these ferrocene compounds were found to exhibit remarkable antiproliferative effects.

  5. Synthesis and Pharmacological Evaluation of α4β2 Nicotinic Ligands with a 3-Fluoropyrrolidine Nucleus

    Dr. Lucia Tamborini, Dr. Andrea Pinto, Dr. Roberta Ettari, Dr. Cecilia Gotti, Dr. Francesca Fasoli, Prof. Paola Conti and Prof. Carlo De Micheli

    Article first published online: 16 APR 2015 | DOI: 10.1002/cmdc.201500073

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    Basicity tuned by F: By combining structural features of niodene and compound B, we developed new α4β2 receptor ligands characterized by the 3-fluoropyrrolidine nucleus. Derivatives (2S,4R)-11 and (2S,4R)-12 were highlighted as the most promising ligands identified in this study, showing good affinity and selectivity for the α4β2 subtype and physicochemical properties predictive of good central nervous system penetration.