Cover image for Vol. 9 Issue 10

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (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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October 20, 2014

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  1. Pramipexole Derivatives as Potent and Selective Dopamine D3 Receptor Agonists with Improved Human Microsomal Stability

    Dr. Jianyong Chen, Dr. Cheng Jiang, Prof. Beth Levant, Dr. Xiaoqin Li, Dr. Ting Zhao, Dr. Bo Wen, Dr. Ruijuan Luo, Prof. Duxin Sun and Prof. Shaomeng Wang

    Article first published online: 22 OCT 2014 | DOI: 10.1002/cmdc.201402398

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    Fully stable: A series of novel pramipexole derivatives were synthesized by modification of previously reported D3 ligands. These compounds are much more stable in human microsomes. They retain high affinities for the D3 receptor and excellent selectivity for D3 over the D2 and D1 receptors. These compounds were determined to be full agonists for the human D3 receptor.

  2. Receptor-Mediated Uptake of Boron-Rich Neuropeptide Y Analogues for Boron Neutron Capture Therapy

    Dr. Verena M. Ahrens, Dr. René Frank, Solveig Boehnke, Dr. Christian L. Schütz, Dr. Gabriele Hampel, Dorothée S. Iffland, Prof. Dr. Nicolas H. Bings, Prof. Dr. Evamarie Hey-Hawkins and Prof. Dr. Annette G. Beck-Sickinger

    Article first published online: 22 OCT 2014 | DOI: 10.1002/cmdc.201402368

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    NPY for BNCT: Neuropeptide Y (NPY) derivatives selective for only one receptor subtype are internalized into tumor cells that express these specific surface receptors. The cellular uptake of highly boron-loaded NPY analogues and their application as an efficient shuttle system for successful boron neutron capture therapy (BNCT) are demonstrated.

  3. O-(Triazolyl)methyl Carbamates as a Novel and Potent Class of Fatty Acid Amide Hydrolase (FAAH) Inhibitors

    Dr. Giampiero Colombano, Clara Albani, Dr. Giuliana Ottonello, Dr. Alison Ribeiro, Dr. Rita Scarpelli, Dr. Glauco Tarozzo, Jennifer Daglian, Dr. Kwang-Mook Jung, Prof. Daniele Piomelli and Dr. Tiziano Bandiera

    Article first published online: 22 OCT 2014 | DOI: 10.1002/cmdc.201402374

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    Searching FAAH and wide:­ O-(Triazolyl)methyl carbamates were designed and synthesized via click chemistry to investigate their inhibitory activity against fatty acid amide hydrolase (FAAH), a validated target in the treatment of several disorders, including pain and drug addiction. The results highlighted the importance of 1,4-disubstituted-1,2,3-triazoles for activity.

  4. Molecular-Target-Based Anticancer Photosensitizer: Synthesis and in vitro Photodynamic Activity of Erlotinib–Zinc(II) Phthalocyanine Conjugates

    Dr. Feng-Ling Zhang, Qi Huang, Prof. Jian-Yong Liu, Prof. Ming-Dong Huang and Prof. Jin-Ping Xue

    Article first published online: 21 OCT 2014 | DOI: 10.1002/cmdc.201402373

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    Waging war on cancer: Herein we report a series of conjugates with phthalocyanine as the “warhead” and erlotinib, a molecular-target-based anticancer drug, as the “guidance system”. These conjugates combine the high activity of photodynamic therapy with the highly effective targeting capacity of molecular-target-based anticancer therapy, thereby acting as “missile-style” target-directed photosensitizers for potential use in cancer treatments.

  5. Design of gem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological Evaluation

    Prof. Dr. Arun K. Ghosh, Sofiya Yashchuk, Akira Mizuno, Nilanjana Chakraborty, Johnson Agniswamy, Yuan-Fang Wang, Manabu Aoki, Pedro Miguel Salcedo Gomez, Masayuki Amano, Prof. Irene T. Weber and Dr. Hiroaki Mitsuya

    Article first published online: 21 OCT 2014 | DOI: 10.1002/cmdc.201402358

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    High-performance fluoros: We report the design, synthesis, biological, and X-ray structural studies of HIV-1 protease inhibitors (PIs) containing gem-difluoro-bis-THF as the P2 ligand. These PIs exhibited much better lipophilicity profiles and blood–brain barrier permeability than darunavir in an in vitro model. A high-resolution structure of a PI–HIV-1 protease complex shows ligand fluorine atoms involved in interesting interactions in the S2 subsite. The PIs also maintained excellent activity against multi-PI-resistant clinical HIV-1 variants.