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PERSPECTIVES
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2609-2645
| Ligands for Glutamate Receptors: Design and Therapeutic Prospects
Hans Bräuner-Osborne,
Jan Egebjerg,
Elsebet Ø. Nielsen,
Ulf Madsen, and
Povl Krogsgaard-Larsen
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ARTICLES
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2646-2654
Antimalarial, Antitrypanosomal, and Antileishmanial Activities and Cytotoxicity of Bis(9-amino-6-chloro-2-methoxyacridines): Influence of the Linker
Sophie Girault,
Philippe Grellier,
Amaya Berecibar, ,
Louis Maes,
Elisabeth Mouray,
Pascal Lemière,
Marie-Ange Debreu,
Elisabeth Davioud-Charvet, and
Christian Sergheraert
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2655-2663
Identification of Substituted 3-[(4,5,6,7-Tetrahydro-1H-indol-2-yl)methylene]- 1,3-dihydroindol-2-ones as Growth Factor Receptor Inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-R Tyrosine Kinases
Li Sun,
Ngoc Tran,
Congxing Liang,
Steve Hubbard,
Flora Tang,
Kenneth Lipson,
Randall Schreck,
Yong Zhou,
Gerald McMahon, and
Cho Tang
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2664-2674
Novel Inhibitors of DNA Gyrase: 3D Structure Based Biased Needle Screening, Hit Validation by Biophysical Methods, and 3D Guided Optimization. A Promising Alternative to Random Screening
Hans-Joachim Boehm,
Markus Boehringer,
Daniel Bur,
Hans Gmuender,
Walter Huber,
Werner Klaus,
Dirk Kostrewa,
Holger Kuehne,
Thomas Luebbers,
Nathalie Meunier-Keller, and
Francis Mueller
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2675-2684
Synthesis and Antitumor Activity of New Benzoheterocyclic Derivatives of Distamycin A
Pier Giovanni Baraldi,
Romeo Romagnoli,
Italo Beria,
Paolo Cozzi,
Cristina Geroni,
Nicola Mongelli,
Nicoletta Bianchi,
Carlo Mischiati, and
Roberto Gambari
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2685-2697
Synthesis and Pharmacological Evaluation of New Pyrazolidine-3,5-diones as AT1 Angiotensin II Receptor Antagonists
Bertrand Le Bourdonnec,
Emmanuelle Meulon,
Saïd Yous,
Jean-François Goossens,
Raymond Houssin, and
Jean-Pierre Hénichart
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2698-2702
[Pro3]Dyn A(1-11)-NH2: A Dynorphin Analogue with High Selectivity for the Opioid Receptor
Georg Schlechtingen,
Li Zhang,
Alan Maycock,
Robert N. DeHaven,
Jeffrey D. Daubert,
Joel Cassel,
Nga N. Chung,
Peter W. Schiller, and
Murray Goodman
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2703-2718
In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective 1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia
James C. Barrow,
Philippe G. Nantermet,
Harold G. Selnick,
Kristen L. Glass,
Kenneth E. Rittle,
Kevin F. Gilbert,
Thomas G. Steele,
Carl F. Homnick,
Roger M. Freidinger,
Rick W. Ransom,
Paul Kling,
Duane Reiss,
Theodore P. Broten,
Terry W. Schorn,
Raymond S. L. Chang,
Stacey S. O'Malley,
Timothy V. Olah,
Joan D. Ellis,
Andrea Barrish,
Kelem Kassahun,
Paula Leppert,
Dhanapalan Nagarathnam, and
Carlos Forray
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2719-2730
Characterization of a Novel Analogue of 1 ,25(OH)2-Vitamin D3 with Two Side Chains: Interaction with Its Nuclear Receptor and Cellular Actions
Anthony W. Norman,
Percy S. Manchand,
Milan R. Uskokovic,
William H. Okamura,
Janet A. Takeuchi,
June E. Bishop,
Jun-Iichi Hisatake,
H. Phillip Koeffler, and
Sara Peleg
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2731-2737
Antineoplastic Agents. 443. Synthesis of the Cancer Cell Growth Inhibitor Hydroxyphenstatin and Its Sodium Diphosphate Prodrug
George R. Pettit,
Matthew P. Grealish,
Delbert L. Herald,
Michael R. Boyd,
Ernest Hamel, and
Robin K. Pettit
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2738-2744
Development of a Lead Inhibitor for the A16V+S108T Mutant of Dihydrofolate Reductase from the Cycloguanil-Resistant Strain (T9/94) of Plasmodium falciparum
Yongyuth Yuthavong,
Tirayut Vilaivan,
Netnapa Chareonsethakul,
Sumalee Kamchonwongpaisan,
Worachart Sirawaraporn,
Rachel Quarrell, and
Gordon Lowe
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2745-2752
'3+1' Mixed-Ligand Oxotechnetium(V) Complexes with Affinity for Melanoma: Synthesis and Evaluation in Vitro and in Vivo
Matthias Friebe,
Ashfaq Mahmood,
Hartmut Spies,
Ralf Berger,
Bernd Johannsen,
Ashour Mohammed,
Michael Eisenhut,
Cristina Bolzati,
Alan Davison, and
Alun G. Jones
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2753-2758
Synthesis and Antimalarial Activity of Sixteen Dispiro-1,2,4,5-tetraoxanes: Alkyl-Substituted 7,8,15,16-Tetraoxadispiro[5.2.5.2]hexadecanes
Jonathan L. Vennerstrom,
Yuxiang Dong,
Steven L. Andersen,
Arba L. Ager, Jr.,
Hong-ning Fu,
Robert E. Miller,
David L. Wesche,
Dennis E. Kyle,
Lucia Gerena,
Sheri M. Walters,
James K. Wood,
Geoffrey Edwards,
Alexandra D. Holme,
W. Graham McLean, and
Wilbur K. Milhous
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2759-2769
Potent and Selective Indolomorphinan Antagonists of the Kappa-Opioid Receptor
William C. Stevens, Jr.,
Robert M. Jones,
Govindan Subramanian,
Thomas G. Metzger,
David M. Ferguson, and
Philip S. Portoghese
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BRIEF ARTICLES
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2770-2774
A Rapid Computational Method for Lead Evolution: Description and Application to 1-Adrenergic Antagonists
Erin K. Bradley,
Paul Beroza,
Julie E. Penzotti,
Peter D. J. Grootenhuis,
David C. Spellmeyer, and
Jennifer L. Miller
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