Perspectives
| Discovery and Development of Fatty Acid Amide Hydrolase (FAAH) Inhibitors Mark Seierstad and J. Guy Breitenbucher 7327-7343  |
| Full: PDF (822 K) |
Letters
| In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as Novel Antileishmanial Chemotypes Suresh K. Tipparaju, Sipak Joyasawal, Marco Pieroni, Marcel Kaiser, Reto Brun and Alan P. Kozikowski 7344-7347  |
| Full: PDF (653 K) |
| Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease Scott C. Mayer, Anthony F. Kreft, Boyd Harrison, Magid Abou-Gharbia, Madelene Antane, Suzan Aschmies, Kevin Atchison, Michael Chlenov, Derek C. Cole, Thomas Comery, George Diamantidis, John Ellingboe, Kristi Fan, Rocco Galante, Cathleen Gonzales, Douglas M. Ho, Molly E. Hoke, Yun Hu, Donna Huryn, Uday Jain, Mei Jin, Kenneth Kremer, Dennis Kubrak, Melissa Lin, Peimin Lu, Ron Magolda, Robert Martone, William Moore, Aram Oganesian, Menelas N. Pangalos, Alex Porte, Peter Reinhart, Lynn Resnick, David R. Riddell, June Sonnenberg-Reines, Joseph R. Stock, Shaiu-Ching Sun, Erik Wagner, Ting Wang, Kevin Woller, Zheng Xu, Margaret M. Zaleska, Joseph Zeldis, Minsheng Zhang, Hua Zhou and J. Steven Jacobsen 7348-7351  |
| Full: PDF (175 K) |
| Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases Bin Zhang, Zaneta Nikolovska-Coleska, Yan Zhang, Longchuan Bai, Su Qiu, Chao-Yie Yang, Haiying Sun, Shaomeng Wang and Yikang Wu 7352-7355  |
| Full: PDF (361 K) |
Articles
| Novel Multifunctional Acyloxyalkyl Ester Prodrugs of 5-Aminolevulinic Acid Display Improved Anticancer Activity Independent and Dependent on Photoactivation Gili Berkovitch, Dvir Doron, Abraham Nudelman, Zvi Malik and Ada Rephaeli 7356-7369  |
| Full: PDF (1576 K) |
| Synthesis and Pharmacological Characterization of Novel Druglike Corticotropin-Releasing Factor 1 Antagonists Romano Di Fabio, Yves St-Denis, Fabio M. Sabbatini, Daniele Andreotti, Roberto Arban, Giovanni Bernasconi, Simone Braggio, Frank E. Blaney, Anna M. Capelli, Emiliano Castiglioni, Enza Di Modugno, Daniele Donati, Elettra Fazzolari, Emiliangelo Ratti, Aldo Feriani, Stefania Contini, Gabriella Gentile, Damiano Ghirlanda, Stefano Provera, Carla Marchioro, Karen L. Roberts, Anna Mingardi, Mario Mattioli, Arnaldo Nalin, Francesca Pavone, Simone Spada, David G. Trist and Angela Worby 7370-7379  |
| Full: PDF (517 K) |
| Novel Acetylcholine and Carbamoylcholine Analogues: Development of a Functionally Selective α4β2 Nicotinic Acetylcholine Receptor Agonist Camilla P. Hansen, Anders A. Jensen, Jeppe K. Christensen, Thomas Balle, Tommy Liljefors and Bente Frølund 7380-7395  |
| Full: PDF (1479 K) |
| Identification of Small Molecular Weight Inhibitors of Src Homology 2 Domain-Containing Tyrosine Phosphatase 2 (SHP-2) via in Silico Database Screening Combined with Experimental Assay Wen-Mei Yu, Olgun Guvench, Alexander D. MacKerell, and Cheng-Kui Qu 7396-7404  |
| Full: PDF (1307 K) |
| A Small Molecule Inhibitor, 1,2,4,5-Benzenetetraamine Tetrahydrochloride, Targeting the Y397 Site of Focal Adhesion Kinase Decreases Tumor Growth Vita M. Golubovskaya, Carl Nyberg, Min Zheng, Frederick Kweh, Andrew Magis, David Ostrov and William G. Cance 7405-7416  |
| Full: PDF (3393 K) |
| Histone Deacetylase Inhibitors through Click Chemistry Jie Shen, Robert Woodward, James Patrick Kedenburg, Xianwei Liu, Min Chen, Lanyan Fang, Duxin Sun and Peng George Wang 7417-7427  |
| Full: PDF (413 K) |
| Targeting the Delivery of Glycan-Based Paclitaxel Prodrugs to Cancer Cells via Glucose Transporters Yih-Shyan Lin, Rudeewan Tungpradit, Supachok Sinchaikul, Feng-Ming An, Der-Zen Liu, Suree Phutrakul and Shui-Tein Chen 7428-7441  |
| Full: PDF (1239 K) |
| Discovery of New Inhibitors of d-Alanine:d-Alanine Ligase by Structure-Based Virtual Screening Andreja Kovač, Janez Konc, Blaž Vehar, Julieanne M. Bostock, Ian Chopra, Dušanka Janežič and Stanislav Gobec 7442-7448  |
| Full: PDF (970 K) |
| Design of Annulated Pyrazoles as Inhibitors of HIV-1 Reverse Transcriptase Zachary K. Sweeney, Seth F. Harris, Nidhi Arora, Hassan Javanbakht, Yu Li, Jennifer Fretland, James P. Davidson, J. Roland Billedeau, Shelley K. Gleason, Donald Hirschfeld, Joshua J. Kennedy-Smith, Taraneh Mirzadegan, Ralf Roetz, Mark Smith, Sarah Sperry, Judy M. Suh, Jeffrey Wu, Stan Tsing, Armando G. Villaseñor, Amber Paul, Guoping Su, Gabrielle Heilek, Julie Q. Hang, Amy S. Zhou, Jesper A. Jernelius, Fang-Jie Zhang and Klaus Klumpp 7449-7458  |
| Full: PDF (707 K) |
| Selectivity and Mechanism of Action of a Growth Factor Receptor-Bound Protein 2 Src Homology 2 Domain Binding Antagonist Alessio Giubellino, Zhen-Dan Shi, Lisa M. Miller Jenkins, Karen M. Worthy, Lakshman K. Bindu, Gagani Athauda, Benedetta Peruzzi, Robert J. Fisher, Ettore Appella, Terrence R. Burke, and Donald P. Bottaro 7459-7468  |
| Full: PDF (900 K) |
| Impact of Plasticity and Flexibility on Docking Results for Cytochrome P450 2D6: A Combined Approach of Molecular Dynamics and Ligand Docking Jozef Hritz, Anita de Ruiter and Chris Oostenbrink 7469-7477  |
| Full: PDF (1060 K) |
| Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor Chen Chen, Dongpei Wu, Zhiqiang Guo, Qiu Xie, Greg J. Reinhart, Ajay Madan, Jenny Wen, Takung Chen, Charles Q. Huang, Mi Chen, Yongsheng Chen, Fabio C. Tucci, Martin Rowbottom, Joseph Pontillo, Yun-Fei Zhu, Warren Wade, John Saunders, Haig Bozigian and R. Scott Struthers 7478-7485  |
| Full: PDF (197 K) |
| Novel Naphthalene-N-sulfonyl-d-glutamic Acid Derivatives as Inhibitors of MurD, a Key Peptidoglycan Biosynthesis Enzyme, Jan Humljan, Miha Kotnik, Carlos Contreras-Martel, Didier Blanot, Uroš Urleb, Andréa Dessen, Tom Šolmajer and Stanislav Gobec 7486-7494  |
| Full: PDF (1014 K) |
| Inhibition of Siderophore Biosynthesis by 2-Triazole Substituted Analogues of 5′-O-[N-(Salicyl)sulfamoyl]adenosine: Antibacterial Nucleosides Effective against Mycobacterium tuberculosis Amol Gupte, Helena I. Boshoff, Daniel J. Wilson, João Neres, Nicholas P. Labello, Ravindranadh V. Somu, Chengguo Xing, Clifton E. Barry, and Courtney C. Aldrich 7495-7507  |
| Full: PDF (1470 K) |
| Antitumor Activity of New Substituted 3-(5-Imidazo[2,1-b]thiazolylmethylene)-2-indolinones and 3-(5-Imidazo[2,1-b]thiadiazolylmethylene)-2-indolinones: Selectivity against Colon Tumor Cells and Effect on Cell Cycle-Related Events(1) Aldo Andreani, Silvia Burnelli, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Lucilla Varoli, Natalia Calonghi, Concettina Cappadone, Manuela Voltattorni, Maddalena Zini, Claudio Stefanelli, Lanfranco Masotti and Robert H. Shoemaker 7508-7513  |
| Full: PDF (228 K) |
| Prolyl Oligopeptidase Inhibition by N-Acyl-pro-pyrrolidine-type Molecules Károly Kánai, Péter Arányi, Zsolt Böcskei, György Ferenczy, Veronika Harmat, Kálmán Simon, Sándor Bátori, Gábor Náray-Szabó and István Hermecz 7514-7522  |
| Full: PDF (728 K) |
| Novel 4-(4-Aryl)cyclohexyl-1-(2-pyridyl)piperazines as Δ8−Δ7 Sterol Isomerase (Emopamil Binding Protein) Selective Ligands with Antiproliferative Activity Francesco Berardi, Carmen Abate, Savina Ferorelli, Anna F. de Robertis, Marcello Leopoldo, Nicola A. Colabufo, Mauro Niso and Roberto Perrone 7523-7531  |
| Full: PDF (335 K) |
| Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase Jennifer M. Beierlein, Kathleen M. Frey, David B. Bolstad, Phillip M. Pelphrey, Tammy M. Joska, Adrienne E. Smith, Nigel D. Priestley, Dennis L. Wright and Amy C. Anderson 7532-7540  |
| Full: PDF (1937 K) |
| Design, Structure−Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors Yan Shi, Doree Sitkoff, Jing Zhang, Herbert E. Klei, Kevin Kish, Eddie C.-K. Liu, Karen S. Hartl, Steve M. Seiler, Ming Chang, Christine Huang, Sonia Youssef, Thomas E. Steinbacher, William A. Schumacher, Nyeemah Grazier, Andrew Pudzianowski, Atsu Apedo, Lorell Discenza, Joseph Yanchunas, , Philip D. Stein and Karnail S. Atwal 7541-7551  |
| Full: PDF (984 K) |
| Assessment of Additive/Nonadditive Effects in Structure−Activity Relationships: Implications for Iterative Drug Design Yogendra Patel, Valerie J. Gillet, Trevor Howe, Joaquin Pastor, Julen Oyarzabal and Peter Willett 7552-7562  |
| Full: PDF (2305 K) |
| Surprising Alteration of Antibacterial Activity of 5′′-Modified Neomycin against Resistant Bacteria Jianjun Zhang, Fang-I. Chiang, Long Wu, Przemyslaw Greg Czyryca, Ding Li and Cheng-Wei Tom Chang 7563-7573  |
| Full: PDF (589 K) |
| A Non-Cross-Linking Platinum−Acridine Agent with Potent Activity in Non-Small-Cell Lung Cancer Zhidong Ma, Jayati Roy Choudhury, Marcus W. Wright, Cynthia S. Day, Gilda Saluta, Gregory L. Kucera and Ulrich Bierbach 7574-7580  |
| Full: PDF (475 K) |
| Novel Bis- and Tris-1,2,4-trioxanes: Synthesis and Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii in Swiss Mice(1) Chandan Singh, Ved Prakash Verma, Niraj Krishna Naikade, Ajit Shankar Singh, Mohammad Hassam and Sunil K. Puri 7581-7592  |
| Full: PDF (289 K) |
| Activation of p16 Gene Silenced by DNA Methylation in Cancer Cells by Phosphoramidate Derivatives of 2′-Deoxyzebularine Christine B. Yoo, Rocco Valente, Costantino Congiatu, Federica Gavazza, Annette Angel, Maqbool A. Siddiqui, Peter A. Jones, Christopher McGuigan and Victor E. Marquez 7593-7601  |
| Full: PDF (165 K) |
| 2-[(3-Methoxyphenylethyl)phenoxy]-Based ABCB1 Inhibitors: Effect of Different Basic Side-Chains on Their Biological Properties Nicola Antonio Colabufo, Francesco Berardi, Roberto Perrone, Simona Rapposelli, Maria Digiacomo, Michael Vanni and Aldo Balsamo 7602-7613  |
| Full: PDF (209 K) |
| Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin Gersande Lena, Joseph A. Trapani, Vivien R. Sutton, Annette Ciccone, Kylie A. Browne, Mark J. Smyth, William A. Denny and Julie A. Spicer 7614-7624  |
| Full: PDF (154 K) |
| Synthesis and Structure−Activity Relationship Studies of 2-(N-Substituted)-aminobenzimidazoles as Potent Negative Gating Modulators of Small Conductance Ca2+-Activated K+ Channels Ulrik S. Sørensen, Dorte Strøbæk, Palle Christophersen, Charlotte Hougaard, Marianne L. Jensen, Elsebet Ø. Nielsen, Dan Peters and Lene Teuber 7625-7634  |
| Full: PDF (288 K) |
Brief Articles
| Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors Gianfranco Balboni, Ilaria Lazzari, Claudio Trapella, Lucia Negri, Roberta Lattanzi, Elisa Giannini, Annalisa Nicotra, Pietro Melchiorri, Sergio Visentin, Chiara De Nuccio and Severo Salvadori 7635-7639  |
| Full: PDF (478 K) |
| Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists Takayoshi Suzuki, Sou-ichi Igari, Akira Hirasawa, Mie Hata, Masaji Ishiguro, Hiroki Fujieda, Yukihiro Itoh, Tatsuya Hirano, Hidehiko Nakagawa, Michitaka Ogura, Makoto Makishima, Gozoh Tsujimoto and Naoki Miyata 7640-7644  |
| Full: PDF (504 K) |
| Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase Kenji Tomita, Shinya Oishi, Hiroaki Ohno, Stephen C. Peiper and Nobutaka Fujii 7645-7649  |
| Full: PDF (115 K) |
Book Reviews
| Book Review of High-Throughput Lead Optimization in Drug Discovery Jan W. F. Wasley 7650-7650 |
| Full: PDF (33 K) |
| Book Review of Annual Review of Biochemistry. Volume 77 Jonathan A. Doorn 7650-7651 |
| Full: PDF (33 K) |
Additions and Corrections
| New Selective Inhibitors of Steroid 11β-Hydroxylation in the Adrenal Cortex. Synthesis and Structure−Activity Relationship of Potent Etomidate Analogues Ilse M. Zolle, Michael L. Berger, Friedrich Hammerschmidt, Stefanie Hahner, Andreas Schirbel and Biljana Peric-Simov 7652-7652 |
| Full: PDF (24 K) |