Cover image for Vol. 10 Issue 5

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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April 29, 2015

Editor's Picks: Issue 05/2015

Editor's Picks: Issue 05/2015Editor's picks for issue 05: This month, two Full Papers by Dennis C. Waalboer et al. and David Böhme and Annette G. Beck-Sickinger describe methods of targeted drug delivery using molecular conjugation. Read more...

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  1. Multitarget-Directed Tricyclic Pyridazinones as G Protein-Coupled Receptor Ligands and Cholinesterase Inhibitors

    Prof. Amedeo Pau, Dr. Marco Catto, Dr. Giovanni Pinna, Dr. Simona Frau, Dr. Gabriele Murineddu, Dr. Battistina Asproni, Prof. Maria M. Curzu, Dr. Leonardo Pisani, Dr. Francesco Leonetti, Prof. Maria Isabel Loza, Dr. José Brea, Prof. Gérard A. Pinna and Prof. Angelo Carotti

    Article first published online: 29 APR 2015 | DOI: 10.1002/cmdc.201500124

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    So many targets, so little time: Following a multitarget ligand design approach, 47 pyridazinone-based tricyclic compounds were prepared and tested as ligands of selected GPCRs (5-HT1A, α1A, and D2) and as cholinesterase inhibitors. Several compounds showed nanomolar affinity for the GPCRs tested, acting preferentially as dual antagonist ligands of α1A and 5-HT1A receptors, as well as good cholinesterase inhibitory activities.

  2. MS565: A SPECT Tracer for Evaluating the Brain Penetration of BAF312 (Siponimod)

    Dr. Emmanuelle Briard, Dr. Bettina Rudolph, Dr. Sandrine Desrayaud, Dr. Joel A. Krauser and Dr. Yves P. Auberson

    Article first published online: 29 APR 2015 | DOI: 10.1002/cmdc.201500115

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    Exposing siponimod: BAF312 is a drug candidate for the treatment of multiple sclerosis. Replacement of its trifluoromethyl group by iodine did not affect organ/tissue distribution or pharmacokinetics, and led to the prospective single-photon emission computed tomography (SPECT) imaging agent MS565. The ability of MS565 to mimic BAF312 was confirmed by whole-body autoradiography, using their 14C isotopomers.

  3. Multitarget Therapeutic Leads for Alzheimer’s Disease: Quinolizidinyl Derivatives of Bi- and Tricyclic Systems as Dual Inhibitors of Cholinesterases and β-Amyloid (Aβ) Aggregation

    Dr. Michele Tonelli, Dr. Marco Catto, Dr. Bruno Tasso, Dr. Federica Novelli, Dr. Caterina Canu, Dr. Giovanna Iusco, Dr. Leonardo Pisani, Dr. Angelo De Stradis, Dr. Nunzio Denora, Prof. Anna Sparatore, Prof. Vito Boido, Prof. Angelo Carotti and Prof. Fabio Sparatore

    Article first published online: 29 APR 2015 | DOI: 10.1002/cmdc.201500104

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    “Dualing” with Alzheimer’s! Thioxanthen-9-one (red), xanthen-9-one, naphtho- (green) and anthraquinone (blue) derivatives were identified as leads for the development of Alzheimer’s disease therapeutics. Evaluation identified thioxanthenones 2 (R=CH3, W=(CH2)2) and 4 (R=CH3, W=(CH2)3SCH2), and naphthoquinone 28 as the most potent inhibitors of Aβ aggregation, butyrylcholinesterase, and acetylcholinesterase, respectively.

  4. Aryloxyethyl Thiocyanates Are Potent Growth Inhibitors of Trypanosoma cruzi and Toxoplasma gondii

    María N. Chao, Carolina Exeni Matiuzzi, Melissa Storey, Catherine Li, Dr. Sergio H. Szajnman, Prof. Dr. Roberto Docampo, Prof. Dr. Silvia N. J. Moreno and Prof. Dr. Juan B. Rodriguez

    Article first published online: 27 APR 2015 | DOI: 10.1002/cmdc.201500100

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    Finding the WC: WC-9 is a well-known antichagasic agent targeting squalene synthase. We describe the design, synthesis, and biological evaluation of WC-9 analogues bearing the aryloxy moiety bonded either at the C-4′ or the C-3′ position of the A ring. Some of the analogues are effective growth inhibitors of both Trypanosoma cruzi and Toxoplasma gondii, the etiologic agents of Chagas disease and toxoplasmosis, respectively.

  5. Rational Design of Ruthenium Complexes Containing 2,6-Bis(benzimidazolyl)pyridine Derivatives with Radiosensitization Activity by Enhancing p53 Activation

    Zhiqin Deng, Lianling Yu, Dr. Wenqiang Cao, Prof. Wenjie Zheng and Prof. Tianfeng Chen

    Article first published online: 27 APR 2015 | DOI: 10.1002/cmdc.201500127

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    Oh, 2 b a super sensitizer! A novel Ru complex Ru(bnbp)2Cl2 (bnbp=2,6-bis- (6-nitrobenzimidazol-2-yl)pyridine) was synthesized and was found to enhance radiation-induced DNA damage through the overproduction of reactive oxygen species. Studies into its mechanism of action revealed it to cause G2M cell-cycle arrest and apoptosis by activating the p53 pathway. This study provides a rational design strategy for the development of benzimidazole-containing Ru complexes as potential radiosensitizers.