ChemMedChem

Cover image for Vol. 7 Issue 4

April 2012

Volume 7, Issue 4

Pages 537–743

  1. Cover Picture

    1. Top of page
    2. Cover Picture
    3. Inside Cover
    4. Back Cover
    5. Graphical Abstract
    6. Corrigendum
    7. News
    8. Author Profile
    9. Highlights
    10. Communications
    11. Full Papers
    12. Book Reviews
    13. Preview
    1. Cover Picture: Fluorogenic Peptide-Based Substrates for Monitoring Thrombin Activity (ChemMedChem 4/2012) (page 537)

      Dr. Sander S. van Berkel, Bas van der Lee, Dr. Floris L. van Delft, Dr. Rob Wagenvoord, Prof. Dr. H. Coenraad Hemker and Prof. Dr. Floris P. J. T. Rutjes

      Version of Record online: 27 MAR 2012 | DOI: 10.1002/cmdc.201290012

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      The cover picture shows thrombin-specific substrates bound in the active site of thrombin. In the background, the intact fluorogenic conjugate (shown in yellow) of thrombin-specific tripeptide H-Gly-Gly-Arg and 7-amino-4-methylcoumarin (AMC) bound to thrombin is displayed. Prior to thrombin-mediate hydrolysis, this substrate displays only weak fluorescence. Upon cleavage of the Arg[BOND]AMC bond, strongly fluorescent AMC (shown in bright blue) is liberated. Quantification of the increase in fluorescence over time provides a direct measure for the amount of thrombin present in plasma. Moreover, from these data, the specific thrombin activity can be calculated, which is a direct measure of the coagulability of a clotting sample. These substrates have potential application in microfluidic devices for point-of-care tests, allowing the rapid diagnosis of blood or plasma samples. For more details, see the Full Paper by Floris P. J. T. Rutjes et al. on p. 606 ff.

  2. Inside Cover

    1. Top of page
    2. Cover Picture
    3. Inside Cover
    4. Back Cover
    5. Graphical Abstract
    6. Corrigendum
    7. News
    8. Author Profile
    9. Highlights
    10. Communications
    11. Full Papers
    12. Book Reviews
    13. Preview
    1. Inside Cover: Preliminary Study of the Anticancer Applications of Mesoporous Materials Functionalized with the Natural Product Betulinic Acid (ChemMedChem 4/2012) (page 538)

      Sergio Sánchez-Muñoz, Dr. Santiago Gómez-Ruiz, Dr. Damián Pérez-Quintanilla, Dr. Sonia Morante-Zarcero, Dr. Isabel Sierra, Dr. Sanjiv Prashar, Dr. Reinhard Paschke and Dr. Goran N. Kaluđerović

      Version of Record online: 27 MAR 2012 | DOI: 10.1002/cmdc.201290013

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      The inside cover picture shows that a combination of functionalized mesoporous materials such as MCM-41 and cytotoxic agents, in this case the natural product betulinic acid, gives a drug delivery system with potential application as an adjuvant for local implantation to prevent the recurrence of bone tumors. For more details, see the Full Paper by Santiago Gómez-Ruiz, Damián Pérez-Quintanilla, Goran N. Kaluđerović et al. on p. 670 ff.

  3. Back Cover

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    4. Back Cover
    5. Graphical Abstract
    6. Corrigendum
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    10. Communications
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    1. Inside Back Cover: Fluorescein Analogues Inhibit SecA ATPase: The First Sub-micromolar Inhibitor of Bacterial Protein Translocation (ChemMedChem 4/2012) (page 744)

      Ying-Ju Huang, Dr. Hongyun Wang, Prof. Fen-Biao Gao, Prof. Minyong Li, Dr. Hsiuchin Yang, Prof. Binghe Wang and Prof. Phang C. Tai

      Version of Record online: 27 MAR 2012 | DOI: 10.1002/cmdc.201290017

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      The back cover picture shows the inhibition of SecA, a key enzyme in the bacterial general secretion (Sec) pathway. SecA is essential for bacterial growth and as such represents an ideal target for antibacterial agents. The fluorescein derivatives shown represent the first sub-micromolar inhibitors of SecA's ATPase activity. For more details, see the Full Paper by Binghe Wang, Phang C. Tai et al. on p. 571 ff.

  4. Graphical Abstract

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    5. Graphical Abstract
    6. Corrigendum
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    9. Highlights
    10. Communications
    11. Full Papers
    12. Book Reviews
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  5. Corrigendum

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      Corrigendum: A Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase in Inhibition Potency (page 546)

      Dr. Wataru Nomura, Chie Hashimoto, Aki Ohya, Dr. Kosuke Miyauchi, Dr. Emiko Urano, Dr. Tomohiro Tanaka, Dr. Tetsuo Narumi, Toru Nakahara, Dr. Jun A. Komano, Prof. Dr. Naoki Yamamoto and Prof. Dr. Hirokazu Tamamura

      Version of Record online: 27 MAR 2012 | DOI: 10.1002/cmdc.201200114

      This article corrects:

      A Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase in Inhibition Potency

      Vol. 7, Issue 2, 205–208, Version of Record online: 13 JAN 2012

  6. News

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  7. Author Profile

    1. Top of page
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    3. Inside Cover
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    5. Graphical Abstract
    6. Corrigendum
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    8. Author Profile
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    1. G. Klebe (page 553)

      Version of Record online: 22 FEB 2012 | DOI: 10.1002/cmdc.201200029

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      “If I could be anyone for a day … I would be a water molecule to understand my role in drug–protein binding. In ten years time I will be … just as ignorant about the driving forces responsible for protein–ligand interactions as today, but on a much, much higher level …” This and more about Gerhard Klebe can be found on page 553

  8. Highlights

    1. Top of page
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    6. Corrigendum
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    10. Communications
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    1. In Silico Identification of an Interferon Inhibitor (pages 555–557)

      Prof. Dr. Markus Kaiser and Dr. Christian Ottmann

      Version of Record online: 20 JAN 2012 | DOI: 10.1002/cmdc.201100579

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      Inhibition of IFNα–IFNR: Interferon (IFN) is an important signaling molecule and antiviral therapeutic agent. However, in certain diseases like type I diabetes, IFN action can be harmful. Schneider and co-workers recently reported the identification of the first IFNα–IFNR inhibitor via in silico screening, which binds to IFNα and impedes interferon signaling in cells.

    2. Pyrazinamide: A Frontline Drug Used for Tuberculosis. Molecular Mechanism of Action Resolved after 50 Years? (pages 558–560)

      Alvin S. Kalinda and Prof. Courtney C. Aldrich

      Version of Record online: 13 JAN 2012 | DOI: 10.1002/cmdc.201100587

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      Target acquired! After 50 years of use, has the molecular mode of action finally been identified for pyrazinamide? Recently, inhibition of trans-translation in Mycobacterium tuberculosis was suggested as a novel mode of action for this important TB drug. The results of the study by Zhang et al., reported in Science, are highlighted here.

  9. Communications

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    1. Dual Dehydrosqualene/Squalene Synthase Inhibitors: Leads for Innate Immune System-Based Therapeutics (pages 561–564)

      Dr. Fu-Yang Lin, Dr. Yonghui Zhang, Dr. Mary Hensler, Yi-Liang Liu, Dr. Ohn A. Chow, Wei Zhu, Dr. Ke Wang, Ran Pang, Wdee Thienphrapa, Prof. Victor Nizet and Prof. Eric Oldfield

      Version of Record online: 30 JAN 2012 | DOI: 10.1002/cmdc.201100589

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      Double whammy! Small molecules that inhibit Staphylococcus aureus dehydrosqualene synthase (CrtM) or host squalene synthase (SQS) are of interest as novel, innate immunity-based therapeutics, blocking virulence or stimulating antibacterial neutrophil extracellular trap (NET) formation. The discovery of leads that do both represents a new route to treating staph infections.

    2. Truncated Reverse Isoxazolidinyl Nucleosides: A New Class of Allosteric HIV-1 Reverse Transcriptase Inhibitors (pages 565–569)

      Prof. Roberto Romeo, Dr. Salvatore V. Giofrè, Dr. Beatrice Macchi, Dr. Emanuela Balestrieri, Prof. Antonio Mastino, Pedro Merino, Dr. Caterina Carnovale, Prof. Giovanni Romeo and Prof. Ugo Chiacchio

      Version of Record online: 9 FEB 2012 | DOI: 10.1002/cmdc.201200022

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      Affairs of the HAART! The synthesis of HEPT-derived, truncated reverse isoxazolidinyl nucleosides (shown) is reported. These compounds represent the first examples of isoxazolidines bearing a pyrimidine scaffold at the C-3 position using a glycoside-type linkage. Biological evaluation showed that some of the derivatives act as non-nucleoside inhibitors of HIV-1 reverse transcriptase, with an efficacy comparable to that of Nevirapine but with reduced toxicity.

  10. Full Papers

    1. Top of page
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    3. Inside Cover
    4. Back Cover
    5. Graphical Abstract
    6. Corrigendum
    7. News
    8. Author Profile
    9. Highlights
    10. Communications
    11. Full Papers
    12. Book Reviews
    13. Preview
    1. Fluorescein Analogues Inhibit SecA ATPase: The First Sub-micromolar Inhibitor of Bacterial Protein Translocation (pages 571–577)

      Ying-Ju Huang, Dr. Hongyun Wang, Prof. Fen-Biao Gao, Prof. Minyong Li, Dr. Hsiuchin Yang, Prof. Binghe Wang and Prof. Phang C. Tai

      Version of Record online: 22 FEB 2012 | DOI: 10.1002/cmdc.201100594

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      Battling bugs! As an essential component for bacterial growth, SecA is an ideal target for antimicrobial agents. Two fluorescein analogues rose bengal (RB) and erythrosin B (EB) were found to be potent inhibitors of SecA ATPase with IC50 values of 0.5 and 0.2 μM, respectively. RB and EB also exhibit inhibitory effects on cell growth and in vitro protein translocation.

    2. Synthesis and Evaluation of 1-Amino-6-halo-β-carbolines as Antimalarial and Antiprion Agents (pages 578–586)

      Dr. Mark J. Thompson, Jennifer C. Louth, Susan M. Little, Matthew P. Jackson, Dr. Yohan Boursereau, Dr. Beining Chen and Prof. Iain Coldham

      Version of Record online: 24 JAN 2012 | DOI: 10.1002/cmdc.201200002

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      Parasites and problem proteins! Malaria and Creutzfeldt–Jakob disease (CJD), two very different conditions, may have a common therapeutic agent class in the 6-halo-β-carbolines. Synthesis of a compound library and screening against two strains of Plasmodium falciparum and in an in vitro model of prion disease revealed these agents as potential candidates for further development as both antiprion and antimalarial drugs.

    3. Synthesis and Biological Evaluation of Acridine Derivatives as Antimalarial Agents (pages 587–605)

      Dr. Xiao-Min Yu, Dr. Florence Ramiandrasoa, Dr. Lucie Guetzoyan, Dr. Bruno Pradines, Edgar Quintino, Dr. Daniele Gadelle, Dr. Patrick Forterre, Dr. Thierry Cresteil, Prof. Jean-Pierre Mahy and Dr. Stéphanie Pethe

      Version of Record online: 13 FEB 2012 | DOI: 10.1002/cmdc.201100554

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      Bad news forP. fal.: 28 new N-alkylaminoacridine derivatives attached to nitrogen heterocycles were synthesized, and their antimalarial potency was examined. The best among these have nanomolar IC50 values toward parasite proliferation on chloroquine (CQ)-susceptible and CQ-resistant strains. The activity of these new acridine derivatives can be explained by inhibition of heme biocrystallization and DNA intercalation, thus inhibiting topoisomerase IIB.

    4. Fluorogenic Peptide-Based Substrates for Monitoring Thrombin Activity (pages 606–617)

      Dr. Sander S. van Berkel, Bas van der Lee, Dr. Floris L. van Delft, Dr. Rob Wagenvoord, Prof. Dr. H. Coenraad Hemker and Prof. Dr. Floris P. J. T. Rutjes

      Version of Record online: 31 JAN 2012 | DOI: 10.1002/cmdc.201100560

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      An eye on thrombin: A series of fluorogenic peptidyl-AMC substrates were synthesized and subjected to a biological evaluation to determine their suitability in the thrombin generation test (TGT). Evaluation of the acquired thrombin generation curves showed that several of these substrates have excellent potential for replacement of the substrate in current use.

    5. Dipeptidyl Peptidase IV (DPPIV/CD26)-Based Prodrugs of Hydroxy-Containing Drugs (pages 618–628)

      Dr. Alberto Diez-Torrubia, Dr. Silvia Cabrera, Dr. Anne-Marie Lambeir, Prof. Jan Balzarini, Prof. María-José Camarasa and Dr. Sonsoles Velázquez

      Version of Record online: 3 FEB 2012 | DOI: 10.1002/cmdc.201100504

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      Improve stability and solubility! Tripeptide prodrugs of a variety of hydroxy-containing drugs exhibiting fair chemical stability are efficiently hydrolyzed by DPPIV/CD26 to ester valyl intermediates, which spontaneously release the parent drug. A number of these prodrugs have significantly higher water solubility than their poorly soluble parent compounds.

    6. Diarylheterocycle Core Ring Features Effect in Selective COX-1 Inhibition (pages 629–641)

      Dr. Maria Grazia Perrone, Dr. Paola Vitale, Dr. Paola Malerba, Dr. Angela Altomare, Dr. Rosanna Rizzi, Prof. Antonio Lavecchia, Dr. Carmen Di Giovanni, Prof. Ettore Novellino and Prof. Antonio Scilimati

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/cmdc.201100530

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      Getting to the core: The role of the central nucleus in the diarylheterocycle COX-1 inhibitor class was investigated. We identified 5-(furan-2-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole (17) as a selective inhibitor of COX-1 activity. The results of molecular docking studies shed light the binding mode of 17 into the catalytic site of COX-1.

    7. Synthesis, in vitro Cytotoxicity, and Interaction with DNA of Platinum(II) Complexes with N-Monocycloalkyl Derivatives of 1R,2R-Diaminocyclohexane as Carrier Ligands (pages 642–649)

      Yanyan Sun, Prof. Shaohua Gou, Fei Liu, Dr. Runting Yin and Dr. Lei Fang

      Version of Record online: 13 JAN 2012 | DOI: 10.1002/cmdc.201100467

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      Platinum(II) complexes: Oxaliplatin derivatives, especially 1 f and 2 f, show similar or superior cytotoxicity to oxaliplatin. The apoptotic mechanism of complex 2 f and its ability to cause S-phase cell-cycle arrest were determined by flow cytometry. This compound has the capacity to distort DNA through a binding mode distinct from that of oxaliplatin.

    8. Tyrosine Kinase Inhibitors Influence ABCG2 Expression in EGFR-Positive MDCK BCRP Cells via the PI3K/Akt Signaling Pathway (pages 650–662)

      Dr. Anne Pick and Prof. Dr. Michael Wiese

      Version of Record online: 22 FEB 2012 | DOI: 10.1002/cmdc.201100543

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      Resisting resistance! The interaction of known tyrosine kinase inhibitors (TKIs) with ABC transporter ABCG2 was investigated in detail. Insight was gained into the signal transduction cascade that regulates ABCG2. And the results suggest that combining a modulator of drug resistance with an EGFR inhibitor might be an ideal way to combat multidrug resistance in cancer cells in the future.

    9. Novel 4-Amino Bis-pyridinium and Bis-quinolinium Derivatives as Choline Kinase Inhibitors with Antiproliferative Activity against the Human Breast Cancer SKBR-3 Cell Line (pages 663–669)

      Verónica Gómez-Pérez, Dr. Theresa McSorley, Dr. Wei Cun See Too, Dr. Manfred Konrad and Dr. Joaquín M. Campos

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/cmdc.201100505

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      Hitting the spot! There is significant interest in the development of selective and potent choline kinase (ChoK) inhibitors for use as pharmacological tools. ChoK inhibitors with either bis-pyridinium or bis-quinolinium scaffolds exhibit mixed inhibition with a predominantly competitive component. The most active compounds have antiproliferative activities of ∼1 μM against the SKBR3 cell line and are much more potent than the choline homologue hemicholinium-3.

    10. Preliminary Study of the Anticancer Applications of Mesoporous Materials Functionalized with the Natural Product Betulinic Acid (pages 670–679)

      Sergio Sánchez-Muñoz, Dr. Santiago Gómez-Ruiz, Dr. Damián Pérez-Quintanilla, Dr. Sonia Morante-Zarcero, Dr. Isabel Sierra, Dr. Sanjiv Prashar, Dr. Reinhard Paschke and Dr. Goran N. Kaluđerović

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/cmdc.201100588

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      The perfect combination: The combination of functionalized mesoporous materials such as MCM-41 with betulinic acid, a potent anticancer drug, led to novel drug delivery systems which may be useful in the future as adjuvant agents to avoid the recurrence of bone tumors on local implantations.

    11. Discovery of Novel 2-N-Aryl-Substituted Benzenesulfonamidoacetamides: Orally Bioavailable Tubulin Polymerization Inhibitors with Marked Antitumor Activities (pages 680–693)

      Dr. Zulong Liu, Dr. Zuyu Zhou, Dr. Wei Tian, Dr. Xing Fan, Ding Xue, Prof. Long Yu, Prof. Qiang Yu and Prof. Ya-Qiu Long

      Version of Record online: 6 FEB 2012 | DOI: 10.1002/cmdc.201100529

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      The latest and greatest: Structural optimization of an in-house screening hit afforded a novel class of benzenesulfonamides as orally bioavailable and potent tubulin polymerization inhibitors. These compounds act as antimitotic agents and exhibit a tubulin binding mechanism similar to that of colchicine. The most potent analogues have in vivo antitumor efficacy and are able to circumvent P-glycoprotein-mediated multidrug resistance in tumor cells.

    12. Design, Synthesis, and Biological Activity of Hydroxamic Tertiary Amines as Histone Deacetylase Inhibitors (pages 694–702)

      Dr. Stefania Terracciano, Dr. Maria Giovanna Chini, Prof. Raffaele Riccio, Prof. Ines Bruno and Prof. Giuseppe Bifulco

      Version of Record online: 25 JAN 2012 | DOI: 10.1002/cmdc.201100531

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      Linear thought process: Non-peptide linear compounds equipped with hydroxamic groups as the metal binder were explored for their effect on histone deacetylase activity. Herein we report docking studies, synthesis, and biological evaluation of this new generation of hydroxamic tertiary amines.

    13. Cytotoxic Salan–Titanium(IV) Complexes: High Activity Toward a Range of Sensitive and Drug-Resistant Cell Lines, and Mechanistic Insights (pages 703–708)

      Dr. Cesar M. Manna, Dr. Ori Braitbard, Esther Weiss, Prof. Jacob Hochman and Prof. Edit Y. Tshuva

      Version of Record online: 20 JAN 2012 | DOI: 10.1002/cmdc.201100593

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      Titanic strength: Salan–TiIV complexes demonstrate high cytotoxicity toward a wide range of cancer cell lines, including cisplatin- and multi-drug-resistant lines, with marked selectivity for tumor tissue. These complexes are also highly robust; they retain activity after long-term pre-incubation in cell culture medium, and appear to induce p53-mediated cell-cycle arrest.

    14. Spiro[chromane-2,4′-piperidine]-Based Histone Deacetylase Inhibitors with Improved in vivo Activity (pages 709–721)

      Dr. Florian Thaler, Dr. Mario Varasi, Dr. Giacomo Carenzi, Dr. Andrea Colombo, Dr. Agnese Abate, Dr. Chiara Bigogno, Dr. Roberto Boggio, Dr. Simone Carrara, Dr. Tiziana Cataudella, Dr. Roberto Dal Zuffo, Dr. Veronica Reali, Dr. Stefania Vultaggio, Dr. Giulio Dondio, Dr. Stefania Gagliardi, Prof. Dr. Saverio Minucci and Ciro Mercurio

      Version of Record online: 22 FEB 2012 | DOI: 10.1002/cmdc.201200024

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      Spiraling to new heights in HDAC inhibition: Herein we summarize the synthesis and biological evaluation of a series of spirochromane hydroxamic acid derivatives as novel inhibitors of human histone deacetylases. Selected compounds were studied for their in vivo pharmacokinetic behavior and for their antitumor activity in an HCT-116 xenograft model.

    15. The σ-Hole Phenomenon of Halogen Atoms Forms the Structural Basis of the Strong Inhibitory Potency of C5 Halogen Substituted Glucopyranosyl Nucleosides towards Glycogen Phosphorylase b (pages 722–732)

      Anastasia L. Kantsadi, Dr. Joseph M. Hayes, Dr. Stella Manta, Dr. Vicky T. Skamnaki, Christos Kiritsis, Dr. Anna-Maria G. Psarra, Zissis Koutsogiannis, Athina Dimopoulou, Stavroula Theofanous, Nikolaos Nikoleousakos, Dr. Panagiotis Zoumpoulakis, Dr. Maria Kontou, Dr. George Papadopoulos, Dr. Spyros E. Zographos, Prof. Dimitris Komiotis and Prof. Demetres D. Leonidas

      Version of Record online: 20 JAN 2012 | DOI: 10.1002/cmdc.201100533

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      On halogenated ground: C5 halogen substituted glucopyranosyl nucleosides have been discovered as some of the most potent inhibitors of glycogen phosphorylase. The ability of the halogen atom to form intermolecular electrostatic interactions through the σ-hole phenomenon rather than by steric effects alone is the structural basis behind their improved inhibitory potential over the unsubstituted ligand.

    16. A 2,6-Disubstituted 4-Anilinoquinazoline Derivative Facilitates Cardiomyogenesis of Embryonic Stem Cells (pages 733–740)

      Guofang Shen, Ying Hu, Jianwei Wu, Ke Jin, Danyan Zhu, Yandong Zhang, Prof. Dr. Yongping Yu and Prof. Dr. Yijia Lou

      Version of Record online: 2 FEB 2012 | DOI: 10.1002/cmdc.201100603

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      Cardiomyogenic agents: We explored the effects of EGFR inhibitors on cardiomyogenesis of embryonic stem (ES) cells and screened a quinazoline compound library for cardiomyogenic stimulators. Compound 62, a 2,6-disubstituted 4-anilinoquinazoline derivative, was found to be a potent cardiomyogenic inducer of ES cells with a mechanism distinct from that of iressa.

  11. Book Reviews

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    1. Drug Metabolism and Pharmacokinetics Quick Guide. By Siamak C. Khojasteh, Harvey Wong and Cornelis E. C. A. Hop. (pages 741–742)

      Dr. Andy Davis

      Version of Record online: 27 JAN 2012 | DOI: 10.1002/cmdc.201200027

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      Springer, Heidelberg 2011. xii+214 pp., softcover €42.75.—ISBN 978-1-4419-5628-6

    2. HIV-1 Integrase: Mechanism and Inhibitor Design. Edited by Nouri Neamati. (page 742)

      Prof. Maurizio Botta

      Version of Record online: 6 FEB 2012 | DOI: 10.1002/cmdc.201200047

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      John Wiley & Sons, Hoboken 2011. 384 pp., hardcover $ 119.99.—ISBN 978-0-47018-474-5

  12. Preview

    1. Top of page
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      Preview: ChemMedChem 5/2012 (page 743)

      Version of Record online: 27 MAR 2012 | DOI: 10.1002/cmdc.201290016

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