Editorial
| Revision of Purity Criteria for Tested Compounds Philip S. Portoghese 1-1 |
| Full: PDF (40 K) |
Perspectives
| Discovery of Innovative Small Molecule Therapeutics Magid Abou-Gharbia 2-9  |
| Full: PDF (1461 K) |
Letters
| Short Antisense Oligonucleotides with Novel 2′−4′ Conformationaly Restricted Nucleoside Analogues Show Improved Potency without Increased Toxicity in Animals Punit P. Seth, Andrew Siwkowski, Charles R. Allerson, Guillermo Vasquez, Sam Lee, Thazha P. Prakash, Edward V. Wancewicz, Donna Witchell and Eric E. Swayze 10-13  |
| Full: PDF (451 K) |
Articles
| Selectively Targeting T- and B-Cell Lymphomas: A Benzothiazole Antagonist of α4β1 Integrin Richard D. Carpenter, Mirela Andrei, Olulanu H. Aina, Edmond Y. Lau, Felice C. Lightstone, Ruiwu Liu, Kit S. Lam and Mark J. Kurth 14-19  |
| Full: PDF (1081 K) |
| Pharmacophore Guided Discovery of Small-Molecule Human Apurinic/Apyrimidinic Endonuclease 1 Inhibitors Zahrah Zawahir, Raveendra Dayam, Jinxia Deng, Cherelene Pereira and Nouri Neamati 20-32  |
| Full: PDF (2033 K) |
| Antagonists of the Human A2A Adenosine Receptor. 4. Design, Synthesis, and Preclinical Evaluation of 7-Aryltriazolo[4,5-d]pyrimidines Roger J. Gillespie, Samantha J. Bamford, Ruth Botting, Mike Comer, Sarah Denny, Suneel Gaur, Michael Griffin, Allan M. Jordan, Anthony R. Knight, Joanne Lerpiniere, Stefania Leonardi, Sean Lightowler, Steven McAteer, Angela Merrett, Anil Misra, Antony Padfield, Mark Reece, Mona Saadi, Daniel L. Selwood, Gemma C. Stratton, Dominic Surry, Richard Todd, Xin Tong, Vicki Ruston, Rebecca Upton and Scott M. Weiss 33-47  |
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| Discovery of Potent Thermolysin Inhibitors Using Structure Based Virtual Screening and Binding Assays Mahmud Tareq Hassan Khan, Ole-Martin Fuskevåg and Ingebrigt Sylte 48-61  |
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| Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Fluorine-18 Labeled Reboxetine Analogues: Potential Positron Emission Tomography Radioligands for in Vivo Imaging of the Norepinephrine Transporter Fanxing Zeng, Jiyoung Mun, Nachwa Jarkas, Jeffrey S. Stehouwer, Ronald J. Voll, Gilles D. Tamagnan, Leonard Howell, John R. Votaw, Clinton D. Kilts, Charles B. Nemeroff and Mark M. Goodman 62-73  |
| Full: PDF (392 K) |
| Synthesis and Evaluation of Novel Inhibitors of Pim-1 and Pim-2 Protein Kinases Zuping Xia, Christian Knaak, Jian Ma, Zanna M. Beharry, Campbell McInnes, Wenxue Wang, Andrew S. Kraft and Charles D. Smith 74-86  |
| Full: PDF (539 K) |
| New Uracil Dimers Showing Erythroid Differentiation Inducing Activities Alessandro Accetta, Roberto Corradini, Stefano Sforza, Tullia Tedeschi, Eleonora Brognara, Monica Borgatti, Roberto Gambari and Rosangela Marchelli 87-94  |
| Full: PDF (668 K) |
| Highly Potent 4-Amino-indolo[2,3-c]azepin-3-one-Containing Somatostatin Mimetics with a Range of sst Receptor Selectivities Debby Feytens, Magali De Vlaeminck, Renzo Cescato, Dirk Tourwé and Jean Claude Reubi 95-104  |
| Full: PDF (696 K) |
| Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides William J. Moore, Jeffrey C. Kern, Ramesh Bhat, Thomas J. Commons, Shoichi Fukayama, Igor Goljer, Girija Krishnamurthy, Ronald L. Magolda, Lisa Nogle, Keith Pitts, Barb Stauffer, Eugene J. Trybulski, Gregory S. Welmaker, Matthew Wilson and Peter V. N. Bodine 105-116  |
| Full: PDF (401 K) |
| Total Synthesis and Cytoprotective Properties of Dykellic Acid Christina M. Thompson, Catherine A. Quinn and Paul J. Hergenrother 117-125  |
| Full: PDF (521 K) |
| Discovery of Targeting Ligands for Breast Cancer Cells Using the One-Bead One-Compound Combinatorial Method Nianhuan Yao, Wenwu Xiao, Xiaobing Wang, Jan Marik, See Hyoung Park, Yoshikazu Takada and Kit S. Lam 126-133  |
| Full: PDF (500 K) |
| Synthesis and Biological Evaluation of Vinca Alkaloids and Phomopsin Hybrids Quoc Anh Ngo, Fanny Roussi, Anthony Cormier, Sylviane Thoret, Marcel Knossow, Daniel Guénard and Françoise Guéritte 134-142  |
| Full: PDF (967 K) |
| Fast Three Dimensional Pharmacophore Virtual Screening of New Potent Non-Steroid Aromatase Inhibitors Marco A. C. Neves, Teresa C. P. Dinis, Giorgio Colombo and M. Luisa Sá e Melo 143-150  |
| Full: PDF (624 K) |
| Discovery of a New Class of Potential Multifunctional Atypical Antipsychotic Agents Targeting Dopamine D3 and Serotonin 5-HT1A and 5-HT2A Receptors: Design, Synthesis, and Effects on Behavior Stefania Butini, Sandra Gemma, Giuseppe Campiani, Silvia Franceschini, Francesco Trotta, Marianna Borriello, Nicoletta Ceres, Sindu Ros, Salvatore Sanna Coccone, Matteo Bernetti, Meri De Angelis, Margherita Brindisi, Vito Nacci, Isabella Fiorini, Ettore Novellino, Alfredo Cagnotto, Tiziana Mennini, Karin Sandager-Nielsen, Jesper Tobias Andreasen, Jorgen Scheel-Kruger, Jens D. Mikkelsen and Caterina Fattorusso 151-169  |
| Full: PDF (1024 K) |
| Synthesis and Evaluation of Benzothiazole-Based Analogues as Novel, Potent, and Selective Fatty Acid Amide Hydrolase Inhibitors Xueqing Wang, Katerina Sarris, Karen Kage, Di Zhang, Scott P. Brown, Teodozyi Kolasa, Carol Surowy, Odile F. El Kouhen, Steven W. Muchmore, Jorge D. Brioni and Andrew O. Stewart 170-180  |
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| Identification and Optimization of a Novel Inhibitor of Mitochondrial Calpain 10 Kyle A. Rasbach, David D. Arrington, Sina Odejinmi, Chris Giguere, Craig C. Beeson and Rick G. Schnellmann 181-188  |
| Full: PDF (882 K) |
| Chemical Modification and Biological Evaluation of New Semisynthetic Derivatives of 28,29-Didehydronystatin A1 (S44HP), a Genetically Engineered Antifungal Polyene Macrolide Antibiotic Maria N. Preobrazhenskaya, Evgenia N. Olsufyeva, Svetlana E. Solovieva, Anna N. Tevyashova, Marina I. Reznikova, Yuryi N. Luzikov, Larisa P. Terekhova, Aleksei S. Trenin, Olga A. Galatenko, Ivan D. Treshalin, Elena P. Mirchink, Vladimir M. Bukhman, Håvard Sletta and Sergey B. Zotchev 189-196  |
| Full: PDF (329 K) |
| New Derivatives of Farnesylthiosalicylic Acid (Salirasib) for Cancer Treatment: Farnesylthiosalicylamide Inhibits Tumor Growth in Nude Mice Models Liat Goldberg, Roni Haklai, Victor Bauer, Aaron Heiss and Yoel Kloog 197-205  |
| Full: PDF (341 K) |
| Synthesis and Anti-Hepatitis B Virus and Anti-Hepatitis C Virus Activities of 7-Deazaneplanocin A Analogues in Vitro Hyo-Joong Kim, Ashoke Sharon, Chandralata Bal, Jianing Wang, Madhan Allu, Zhuhui Huang, Michael G. Murray, Leda Bassit, Raymond F. Schinazi, Brent Korba and Chung K. Chu 206-213  |
| Full: PDF (153 K) |
Brief Articles
| Design and Synthesis of a Cyclic Double Mutant Peptide (cyclo(87−99)[A91,A96]MBP87−99) Induces Altered Responses in Mice after Conjugation to Mannan: Implications in the Immunotherapy of Multiple Sclerosis Maria Katsara, George Deraos, Theodore Tselios, Minos-Timotheos Matsoukas, Irene Friligou, John Matsoukas and Vasso Apostolopoulos 214-218  |
| Full: PDF (451 K) |
| The Design, Synthesis, and Antiviral Activity of 4′-Azidocytidine Analogues against Hepatitis C Virus Replication: The Discovery of 4′-Azidoarabinocytidine David B. Smith, Genadiy Kalayanov, Christian Sund, Anna Winqvist, Pedro Pinho, Tatiana Maltseva, Veronique Morisson, Vincent Leveque, Sonal Rajyaguru, Sophie Le Pogam, Isabel Najera, Kurt Benkestock, Xiao-Xiong Zhou, Hans Maag, Nick Cammack, Joseph A. Martin, Steven Swallow, Nils Gunnar Johansson, Klaus Klumpp and Mark Smith 219-223  |
| Full: PDF (111 K) |
Additions and Corrections
| Synthesis and Quantitative Structure−Activity Relationship of Fatty Acid Amide Hydrolase Inhibitors: Modulation at the N-Portion of Biphenyl-3-yl Alkylcarbamates Marco Mor, Alessio Lodola, Silvia Rivara, Federica Vacondio, Andrea Duranti, Andrea Tontini, Silvano Sanchini, Giovanni Piersanti, Jason R. Clapper, Alvin R. King, Giorgio Tarzia and Daniele Piomelli 224-224 |
| Full: PDF (17 K) |