Cover image for Vol. 10 Issue 10

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/255 (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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September 26, 2015

Editor's Picks: Issue 10/2015

Editor's Picks: Issue 10/2015The Editor's picks for issue 10 are focused on positron emission tomography (PET). See the Full Paper by Gilmour and colleagues and the Communication by Wuest and co-workers for the latest-breaking advances in this important technology for clinical imaging and medicinal chemistry research. Read more...

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Recently Published Articles

  1. Synthesis and Pharmacological Properties of Silicon-Containing GPR81 and GPR109A Agonists

    Marcel Geyer, Johannes A. Baus, Dr. Ola Fjellström, Dr. Eric Wellner, Linda Gustafsson and Prof. Dr. Reinhold Tacke

    Article first published online: 13 OCT 2015 | DOI: 10.1002/cmdc.201500343

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    Quaternary silicon atoms: Compounds 1a1 f and 2a2f were synthesized as part of a systematic SAR analysis within a new GPR81 agonist lead series (with activities also on the GPR109A receptor) and were studied for their physicochemical properties [octanol/water distribution coefficient (pH 7.4), solubility in HBSS buffer (pH 7.4)], agonistic potency at rat GPR81 and GPR109A receptors, and intrinsic clearance in human liver microsomes and rat hepatocytes.

  2. Design, Synthesis, and Evaluation of Novel Ferroquine and Phenylequine Analogues as Potential Antiplasmodial Agents

    Leon Jacobs, Dr. Carmen de Kock, Dr. Katherine A. de Villiers, Prof. Peter J. Smith, Dr. Vincent J. Smith, Prof. Willem A. L. van Otterlo and Dr. Margaret A. L. Blackie

    Article first published online: 8 OCT 2015 | DOI: 10.1002/cmdc.201500349

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    Mind your FQs and PQs: Novel ferrocenyl and phenyl derivatives of 7-chloroquinolines were found to have good in vitro efficacy toward both chloroquine-sensitive (CQS) NF54 (IC50: 4.2 nM) and chloroquine-resistant (CQR) Dd2 (IC50: 33.7 nM) strains of P. falciparum, as well as good inhibitory activity against β-hematin formation in a NP-40 detergent assay, with IC50 values ranging between 10.4 and 19.2 μM.

  3. Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues

    Prof. Dr. K. C. Nicolaou, Derek Rhoades, Dr. Yanping Wang, Dr. Sotirios Totokotsopoulos, Dr. Ruoli Bai and Dr. Ernest Hamel

    Article first published online: 8 OCT 2015 | DOI: 10.1002/cmdc.201500401

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    Ready for delivery: The design, synthesis and biological evaluation of several new epothilone analogues with regard to their tubulin binding affinities and their capacity to inhibit cancer cell growth are reported. The biological activities of these analogues fall within existing SARs for the epothilone family and will help guide future work toward higher potencies and conjugation with cancer-cell-specific antibodies and other delivery systems for targeted cancer chemotherapy.

  4. Design, Synthesis, and Photophysical Properties of Pyrroloquinoline-Based Compounds Showing Strong Blue Fluorescence as Potential Dyes for Biomedical Applications

    Dr. Davide Carta, Dr. Anna Balasso, Prof. Paolo Caliceti and Prof. Maria Grazia Ferlin

    Article first published online: 8 OCT 2015 | DOI: 10.1002/cmdc.201500366

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    New and blue: A series of pyrroloquinoline-based fluorochromes that emit in the blue wavelength region were synthesized, and their spectral properties were exhaustively evaluated. Some of them showed characteristics similar to or even better than those of AMCA, the known coumarinic scaffold of commercial dyes. The amino-reactive compound 38 coupled to pullulan was found to have very promising potential as a labeling agent for biological applications.

  5. Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9-Epipolygodial against Drug-Resistant Cancer Cells

    Dr. Ramesh Dasari, Annelise De Carvalho, Derek C. Medellin, Kelsey N. Middleton, Dr. Frédéric Hague, Marie N. M. Volmar, Prof. Liliya V. Frolova, Dr. Mateus F. Rossato, Jorge J. De La Chapa, Nicholas F. Dybdal-Hargreaves, Akshita Pillai, Prof. Véronique Mathieu, Prof. Snezna Rogelj, Prof. Cara B. Gonzales, Prof. João B. Calixto, Prof. Antonio Evidente, Dr. Mathieu Gautier, Dr. Gnanasekar Munirathinam, Prof. Rainer Glass, Prof. Patricia Burth, Dr. Stephen C. Pelly, Prof. Willem A. L. van Otterlo, Prof. Robert Kiss and Prof. Alexander Kornienko

    Article first published online: 5 OCT 2015 | DOI: 10.1002/cmdc.201500360

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    Inverting one stereocenter turns the inactive sesquiterpenoid polygodial into a potent anticancer agent with promising activity against drug-resistant cancer cells. Polygodial and 9-epipolygodial undergo a Paal–Knorr reaction with electron-deficient primary amines to form a stable pyrrole derivative, a process of possible biological relevance. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives.