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COMMUNICATIONS
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3815-3819
| Structure-Based Design of Novel Bicyclic Nonpeptide Inhibitors for the Src SH2 Domain
William C. Shakespeare,
Regine S. Bohacek,
Mihai D. Azimioara,
Karina J. Macek,
George P. Luke,
David C. Dalgarno,
Marcos H. Hatada,
Xiaode Lu,
Shelia M. Violette,
Catherine Bartlett, and
Tomi K. Sawyer[Full Article -
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3820-3823
| Hunting the Emesis and Efficacy Targets of PDE4 Inhibitors: Identification of the Photoaffinity Probe 8-(3-Azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ)
Dwight Macdonald,
Hélène Perrier,
Susana Liu,
France Laliberté,
Roberta Rasori,
Annette Robichaud,
Paul Masson, and
Zheng Huang[Full Article -
PDF] | |
3824-3826
| 7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)- 4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2- carboxylates as Novel Highly Selective AMPA Receptor Antagonists
Daniela Catarzi,
Vittoria Colotta,
Flavia Varano,
Lucia Cecchi,
Guido Filacchioni,
Alessandro Galli,
Chiara Costagli, and
Vincenzo Carlà[Full Article -
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3827-3831
| Synthesis of a Substance P Antagonist with a Somatostatin Scaffold: Factors Affecting Agonism/Antagonism at GPCRs and the Role of Pseudosymmetry
Josephine Liu,
Dennis J. Underwood,
Margaret A. Cascieri,
Susan P. Rohrer,
Louis-David Cantin,
Gary Chicchi,
Amos B. Smith, III, and
Ralph Hirschmann[Full Article -
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EXPEDITED ARTICLES
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3832-3836
Discovery of a Potent, Orally Bioavailable  3 Adrenergic Receptor Agonist, (R)-N-[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide
Robert J. Mathvink,
J. Samuel Tolman,
Dawn Chitty,
Mari R. Candelore,
Margaret A. Cascieri,
Lawrence F. Colwell, Jr.,
Liping Deng,
William P. Feeney,
Michael J. Forrest,
Gary J. Hom,
D. Euan MacIntyre,
Randall R. Miller,
Ralph A. Stearns,
Laurie Tota,
Matthew J. Wyvratt,
Michael H. Fisher, and
Ann E. Weber
[Full Article -
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ARTICLES
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3837-3851
| Design, Synthesis, and X-ray Crystal Structure of a Potent Dual Inhibitor of Thymidylate Synthase and Dihydrofolate Reductase as an Antitumor Agent
Aleem Gangjee,
Jianming Yu,
John J. McGuire,
Vivian Cody,
Nikolai Galitsky,
Roy L. Kisliuk, and
Sherry F. Queener
[Full Article -
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3852-3861
| Computational Predictions of Binding Affinities to Dihydrofolate Reductase: Synthesis and Biological Evaluation of Methotrexate Analogues
Malin Graffner-Nordberg,
John Marelius,
Sofie Ohlsson,
Åsa Persson,
Göte Swedberg,
Paul Andersson,
Sven E. Andersson,
Johan Åqvist, and
Anders Hallberg
[Full Article -
PDF] | |
3862-3866
| Identification of Novel Inhibitors of Urokinase via NMR-Based Screening
Philip J. Hajduk,
Steven Boyd,
David Nettesheim,
Vicki Nienaber,
Jean Severin,
Richard Smith,
Don Davidson,
Todd Rockway, and
Stephen W. Fesik
[Full Article -
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3867-3877
| Prediction of Drug Absorption Using Multivariate Statistics
William J. Egan,
Kenneth M. Merz, Jr., and
John J. Baldwin
[Full Article -
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3878-3894
New Diarylmethylpiperazines as Potent and Selective Nonpeptidic  Opioid Receptor Agonists with Increased In Vitro Metabolic Stability
Niklas Plobeck,
Daniel Delorme,
Zhong-Yong Wei,
Hua Yang,
Fei Zhou,
Peter Schwarz,
Lars Gawell,
Hélène Gagnon,
Benjamin Pelcman,
Ralf Schmidt,
Shi Yi Yue,
Christopher Walpole,
William Brown,
Edward Zhou,
Maryse Labarre,
Kemal Payza,
Stephane St-Onge,
Augustus Kamassah,
Pierre-Emmanuel Morin,
Denis Projean,
Julie Ducharme, and
Edward Roberts
[Full Article -
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3895-3905
| N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: A Novel, Exceptionally Selective, Potent Opioid Receptor Agonist with Oral Bioavailability and Its Analogues
Zhong-Yong Wei,
William Brown,
Bryan Takasaki,
Niklas Plobeck,
Daniel Delorme,
Fei Zhou,
Hua Yang,
Paul Jones,
Lars Gawell,
Helene Gagnon,
Ralf Schmidt,
Shi-Yi Yue,
Chris Walpole,
Kemal Payza,
Stephane St-Onge,
Maryse Labarre,
Claude Godbout,
Andrea Jakob,
Joanne Butterworth,
Augustus Kamassah,
Pierre-Emmanuel Morin,
Denis Projean,
Julie Ducharme, and
Edward Roberts
[Full Article -
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3906-3912
| Synthesis and Antiviral Activity of Oxaselenolane Nucleosides
Chung K. Chu,
Li Ma,
Sureyya Olgen,
Claire Pierra,
Jinfa Du,
Giuseppe Gumina,
Elizabeth Gullen,
Yung-Chi Cheng, and
Raymond F. Schinazi
[Full Article -
PDF] | |
3913-3922
| Radioiodinated N-(2-Diethylaminoethyl)benzamide Derivatives with High Melanoma Uptake: Structure-Affinity Relationships, Metabolic Fate, and Intracellular Localization
Michael Eisenhut,
William E. Hull,
Ashour Mohammed,
Walter Mier,
Dorothee Lay,
Wilhelm Just,
Karin Gorgas,#
Wolf D. Lehmann, and
Uwe Haberkorn
[Full Article -
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3923-3932
| trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: Mixed Dopamine D2/D4 Receptor Antagonists as Potential Antipsychotic Agents
Xiaoyan Zhang,
Kevin Hodgetts,
Stanislaw Rachwal,
He Zhao,
Jan W. F. Wasley,
Kimberly Craven,
Robbin Brodbeck,
Andrzej Kieltyka,
Diane Hoffman,
Maria D. Bacolod,
Brian Girard,
Jennifer Tran, and
Andrew Thurkauf
[Full Article -
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3933-3940
| Sequential Cytotoxicity: A Theory Evaluated Using Novel 2-[4-(3-Aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and Related Compounds
Jonathan R. Dimmock,
N. Murthi Kandepu,
Adil J. Nazarali,
Narasimhan L. Motaganahalli,
Travis P. Kowalchuk,
Uma Pugazhenthi,
Jared S. Prisciak,
J. Wilson Quail,
Theresa M. Allen,
Renée LeClerc,
Cheryl L. Santos,
Erik De Clercq, and
Jan Balzarini
[Full Article -
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3941-3948
| Synthesis and Evaluation of N,N-Dialkyl Enkephalin-Based Affinity Labels for Opioid Receptors
Dean Y. Maeda,
Jane E. Ishmael,
Thomas F. Murray, and
Jane V. Aldrich
[Full Article -
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3949-3962
| Synthesis and Antiviral Activity of 4-Benzyl Pyridinone Derivatives as Potent and Selective Non-Nucleoside Human Immunodeficiency Virus Type 1 Reverse Transcriptase Inhibitors
Valérie Dollé,
Chi Hung Nguyen,
Michel Legraverend,
Anne-Marie Aubertin,
André Kirn,
Marie Line Andreola,
Michel Ventura,
Laura Tarrago-Litvak, and
Emile Bisagni
[Full Article -
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3963-3969
| Novel 7-Substituted Camptothecins with Potent Antitumor Activity
Sabrina Dallavalle,
Tatiana Delsoldato,
Anna Ferrari,
Lucio Merlini,
Sergio Penco,
Nives Carenini,
Paola Perego,
Michelandrea De Cesare,
Graziella Pratesi, and
Franco Zunino
[Full Article -
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3970-3980
| The Novel Silatecan 7-tert-Butyldimethylsilyl-10-hydroxycamptothecin Displays High Lipophilicity, Improved Human Blood Stability, and Potent Anticancer Activity
David Bom,
Dennis P. Curran,
Stefan Kruszewski,
Stephen G. Zimmer,
J. Thompson Strode,
Glenda Kohlhagen,
Wu Du,
Ashok J. Chavan,
Kimberly A. Fraley,
Alex L. Bingcang,
Lori J. Latus,
Yves Pommier, and
Thomas G. Burke
[Full Article -
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3981-3986
| Role of Hydrophobic Interactions in Binding S-(N-Aryl/Alkyl-N-hydroxy- carbamoyl)glutathiones to the Active Site of the Antitumor Target Enzyme Glyoxalase I
Avinash Kalsi,
Malcolm J. Kavarana,
Tianfen Lu,
Dale L. Whalen,
Diana S. Hamilton, and
Donald J. Creighton
[Full Article -
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3987-3994
| Novel Histamine H3-Receptor Antagonists with Carbonyl-Substituted 4-(3-(Phenoxy)propyl)-1H-imidazole Structures like Ciproxifan and Related Compounds
Holger Stark,
Bassem Sadek,
Michael Krause,
Annette Hüls,
Xavier Ligneau,
C. Robin Ganellin,
Jean-Michel Arrang,
Jean-Charles Schwartz, and
Walter Schunack
[Full Article -
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3995-4004
Inhibitors of NF- B and AP-1 Gene Expression: SAR Studies on the Pyrimidine Portion of 2-Chloro-4-trifluoromethylpyrimidine-5-[N-(3',5'-bis(trifluoromethyl)phenyl)carboxamide]
Moorthy S. S. Palanki,
Paul E. Erdman,
Leah M. Gayo-Fung,
Graziella I. Shevlin,
Robert W. Sullivan,
Mark J. Suto,
Mark E. Goldman,
Lynn J. Ransone,
Brydon L. Bennett, and
Anthony M. Manning
[Full Article -
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4005-4016
| Nitrosothiol Esters of Diclofenac: Synthesis and Pharmacological Characterization as Gastrointestinal-Sparing Prodrugs
Upul K. Bandarage,
Liqing Chen,
Xinqin Fang,
David S. Garvey,
Alicia Glavin,
David R. Janero,
L. Gordon Letts,
Gregory J. Mercer,
Joy K. Saha,
Joseph D. Schroeder,
Matthew J. Shumway, and
S. William Tam
[Full Article -
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4017-4024
| [GdPCP2A(H2O)2]-: A Paramagnetic Contrast Agent Designed for Improved Applications in Magnetic Resonance Imaging
Silvio Aime,
Mauro Botta,
Luca Frullano,
Simonetta Geninatti Crich,
Giovanni Giovenzana,
Roberto Pagliarin,
Giovanni Palmisano,
Federico Riccardi Sirtori, and
Massimo Sisti
[Full Article -
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4025-4040
| Discovery of Novel p-Arylthio Cinnamides as Antagonists of Leukocyte Function-Associated Antigen-1/Intracellular Adhesion Molecule-1 Interaction. 1. Identification of an Additional Binding Pocket Based on an Anilino Diaryl Sulfide Lead
Gang Liu,
J. T. Link,
Zhonghua Pei,
Edward B. Reilly,
Sandra Leitza,
Bach Nguyen,
Kennan C. Marsh,
Gregory F. Okasinski,
Thomas W. von Geldern,
Mark Ormes,
Kerry Fowler, and
Mike Gallatin
[Full Article -
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