Table of Contents
December 19, 2002
Volume 45, Issue 26
Pages 5609-5819
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Perspectives
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural Products and Design: Interrelated Approaches in Drug Discovery
Arthur A. Patchett
pp 5609–5616Publication Date (Web): November 23, 2002 (Perspective)
DOI: 10.1021/jm020424z
Hi-Res PDFIdentification of Arodyn, a Novel Acetylated Dynorphin A-(1−11) Analogue, as a κ Opioid Receptor Antagonist
Marco A. Bennett, Thomas F. Murray, and Jane V. Aldrich
pp 5617–5619Publication Date (Web): November 22, 2002 (Letter)
DOI: 10.1021/jm025575g
Tumor-Specific Novel Taxoid−Monoclonal Antibody Conjugates
Iwao Ojima, Xudong Geng, Xinyuan Wu, Chuanxing Qu, Christopher P. Borella, Hongsheng Xie, Sharon D. Wilhelm, Barbara A. Leece, Laura M. Bartle, Victor S. Goldmacher, and Ravi V. J. Chari
pp 5620–5623Publication Date (Web): November 20, 2002 (Letter)
DOI: 10.1021/jm025540g
AutoDocking Dinucleotides to the HIV-1 Integrase Core Domain: Exploring Possible Binding Sites for Viral and Genomic DNA
Alexander L. Perryman and J. Andrew McCammon
pp 5624–5627Publication Date (Web): November 14, 2002 (Letter)
DOI: 10.1021/jm025554m
Articles
NMR-Based Modification of Matrix Metalloproteinase Inhibitors with Improved Bioavailability
Philip J. Hajduk, Suzanne B. Shuker, David G. Nettesheim, Richard Craig, David J. Augeri, David Betebenner, Daniel H. Albert, Yan Guo, Robert P. Meadows, Lianhong Xu, Michael Michaelides, Steven K. Davidsen, and Stephen W. Fesik
pp 5628–5639Publication Date (Web): November 20, 2002 (Article)
DOI: 10.1021/jm020160g
Binding Model for Nonpeptide Antagonists of αvβ3 Integrin
Bradley P. Feuston, J. Chris Culberson, Mark E. Duggan, George D. Hartman, Chih-Tai Leu, and Sevgi B. Rodan
pp 5640–5648Publication Date (Web): November 07, 2002 (Article)
DOI: 10.1021/jm0203130
Automated Analysis of Large Sets of Heteronuclear Correlation Spectra in NMR-Based Drug Discovery
Charlotta S. Damberg, Vladislav Yu. Orekhov, and Martin Billeter
pp 5649–5654Publication Date (Web): November 14, 2002 (Article)
DOI: 10.1021/jm020866a
In Silico and NMR Identification of Inhibitors of the IGF-I and IGF-Binding Protein-5 Interaction
Mariusz Kamionka, Till Rehm, Hans-Georg Beisel, Kurt Lang, Richard A. Engh, and Tad A. Holak
pp 5655–5660Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm0208828
Metal-Dependent Inhibition of HIV-1 Integrase
Nouri Neamati, Zhaiwei Lin, Rajeshri G. Karki, Ann Orr, Kiriana Cowansage, Dirk Strumberg, Godwin C. G. Pais, Johannes H. Voigt, Marc C. Nicklaus, Heather E. Winslow, He Zhao, Jim A. Turpin, Jizu Yi, Anna Marie Skalka, Terrence R. Burke, Jr., and Yves Pommier
pp 5661–5670Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm0201417
Pharmacophore Model of Drugs Involved in P-Glycoprotein Multidrug Resistance: Explanation of Structural Variety (Hypothesis)
Ilza K. Pajeva and Michael Wiese
pp 5671–5686Publication Date (Web): November 14, 2002 (Article)
DOI: 10.1021/jm020941h
Anthranilic Acid Amides: A Novel Class of Antiangiogenic VEGF Receptor Kinase Inhibitors
Paul W. Manley, Pascal Furet, Guido Bold, Josef Brüggen, Jürgen Mestan, Thomas Meyer, Christian R. Schnell, and Jeanette WoodMartin Haberey, Andreas Huth, Martin Krüger, Andreas Menrad, Eckhard Ottow, Dieter Seidelmann, Gerhard Siemeister, and Karl-Heinz Thierauch
pp 5687–5693Publication Date (Web): November 20, 2002 (Article)
DOI: 10.1021/jm020899q
Acyclic Analogues of Adenosine Bisphosphates as P2Y Receptor Antagonists: Phosphate Substitution Leads to Multiple Pathways of Inhibition of Platelet Aggregation
Bin Xu, Andrew Stephens, Gary Kirschenheuter, Arthur F. Greslin, Xiaoquin Cheng, Joe Sennelo, Marco Cattaneo, Maddalena L. Zighetti, Aishe Chen, Soon-Ai Kim, Hak Sung Kim, Norbert Bischofberger, Gary Cook, and Kenneth A. Jacobson
pp 5694–5709Publication Date (Web): November 22, 2002 (Article)
DOI: 10.1021/jm020173u
Benzodiazepine Receptor Ligands. 7. Synthesis and Pharmacological Evaluation of New 3-Esters of the 8-Chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) Derivative: An Anxioselective Agent in Rodents
Annarella Costanzo, Gabriella Guerrini, Giovanna Ciciani, Fabrizio Bruni, Camilla Costagli, Silvia Selleri, François Besnard, Barbara Costa, Claudia Martini, and Petra Malmberg-Aiello
pp 5710–5720Publication Date (Web): November 21, 2002 (Article)
DOI: 10.1021/jm020944u
Synthesis of Novel N-1 (Allyloxymethyl) Analogues of 6-Benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, Emivirine) with Improved Activity Against HIV-1 and Its Mutants
Nasser R. El-Brollosy, Per T. Jørgensen, Berit Dahan, Anne Marie Boel, Erik B. Pedersen, and Claus Nielsen
pp 5721–5726Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm020949r
Structure−Affinity Relationship Study on N-[4-(4-Arylpiperazin-1-yl)butyl]arylcarboxamides as Potent and Selective Dopamine D3 Receptor Ligands
Marcello Leopoldo, Francesco Berardi, Nicola A. Colabufo, Paola De Giorgio, Enza Lacivita, Roberto Perrone, and Vincenzo Tortorella
pp 5727–5735Publication Date (Web): November 22, 2002 (Article)
DOI: 10.1021/jm020952a
Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors. 4. Modifications at the Trp Position
Jerry Ryan Holder, Zhimin Xiang, Rayna M. Bauzo, and Carrie Haskell-Luevano
pp 5736–5744Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm020296e
Solid-Phase Synthesis of Polyamine Toxin Analogues: Potent and Selective Antagonists of Ca2+-Permeable AMPA Receptors
Hasse Kromann, Sonata Krikstolaityte, Anne J. Andersen, Kim Andersen, Povl Krogsgaard-Larsen, Jerzy W. Jaroszewski, Jan Egebjerg, and Kristian Strømgaard
pp 5745–5754Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm020314s
Optimization of Alkylidene Hydrazide Based Human Glucagon Receptor Antagonists. Discovery of the Highly Potent and Orally Available 3-Cyano-4-hydroxybenzoic Acid [1-(2,3,5,6-Tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide
Peter Madsen, Anthony Ling, Michael Plewe, Christian K. Sams, Lotte B. Knudsen, Ulla G. Sidelmann, Lars Ynddal, Christian L. Brand, Birgitte Andersen, Douglas Murphy, Min Teng, Larry Truesdale, Dan Kiel, John May, Atsuo Kuki, Shenghua Shi, Michael D. Johnson, Kimberly Ann Teston, Jun Feng, James Lakis, Kenna Anderes, Vlad Gregor, and Jesper Lau
pp 5755–5775Publication Date (Web): November 20, 2002 (Article)
DOI: 10.1021/jm0208572
Design, Synthesis, and Physicochemical and Biological Characterization of a New Iron Chelator of the Family of Hydroxychromenes
Marco Ferrali, Sabrina Bambagioni, Antonio Ceccanti, Donato Donati, Gianluca Giorgi, Marco Fontani, Franco Laschi, Piero Zanello, Mario Casolaro, and Antonello Pietrangelo
pp 5776–5785Publication Date (Web): November 15, 2002 (Article)
DOI: 10.1021/jm021022u
Water Stability and Cytotoxic Activity Relationship of a Series of Ferrocenium Derivatives. ESR Insights on the Radical Production during the Degradation Process
Giovanni Tabbì, Claudio Cassino, Giorgio Cavigiolio, Donato Colangelo, Annalisa Ghiglia, Ilario Viano, and Domenico Osella
pp 5786–5796Publication Date (Web): November 22, 2002 (Article)
DOI: 10.1021/jm021003k
Immobilization of Aminothiols on Poly(oxyalkylene phosphates). Formation of Poly(oxyethylene phosphates)/Cysteamine Complexes and Their Radioprotective Efficiency
Radostina Georgieva, Raina Tsevi, Krassimir Kossev, Rossitsa Kusheva, Mariana Balgjiska, Radostina Petrova, Violeta Tenchova, Ivan Gitsov, and Kolio Troev
pp 5797–5801Publication Date (Web): November 23, 2002 (Article)
DOI: 10.1021/jm020309o
Brief Articles
Melanoma Uptake of 99mTc Complexes Containing the N-(2-Diethylaminoethyl)benzamide Structural Element
Michael Eisenhut, Ashour Mohammed, Walter Mier, Frank Schönsiegel, Matthias Friebe, Ashfaq Mahmood, Alun G. Jones, and Uwe Haberkorn
pp 5802–5805Publication Date (Web): November 23, 2002 (Brief Article)
DOI: 10.1021/jm021026z
Isotopic Effect Study of Propofol Deuteration on the Metabolism, Activity, and Toxicity of the Anesthetic
J. Helfenbein, C. Lartigue, E. Noirault, E. Azim, J. Legailliard, M. J. Galmier, and J. C. Madelmont
pp 5806–5808Publication Date (Web): November 20, 2002 (Brief Article)
DOI: 10.1021/jm020864q
Formaldehyde-Induced DNA Cross-Link of Indolizino[1,2-b]quinolines Derived from the A−D Rings of Camptothecin
Aurore Perzyna, Carine Marty, Michael Facompré, Jean-François Goossens, Nicole Pommery, Pierre Colson, Claude Houssier, Raymond Houssin, Jean-Pierre Hénichart, and Christian Bailly
pp 5809–5812Publication Date (Web): November 22, 2002 (Brief Article)
DOI: 10.1021/jm020235g
Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties of a New Series of Imidazonaphthalimides
Miguel F. Braña, Mónica Cacho, Mario A. García, Beatriz de Pascual-Teresa, Ana Ramos, Nuria Acero, Francisco Llinares, Dolores Muñoz-Mingarro, Cristina Abradelo, María Fernanda Rey-Stolle, and Mercedes Yuste
pp 5813–5816Publication Date (Web): November 22, 2002 (Brief Article)
DOI: 10.1021/jm020950q
Synthesis of (Aminoalkylamine)-N-aminoalkyl)azanonaborane(11) Derivatives for Boron Neutron Capture Therapy
Mohamed E. El-Zaria, Udo Dörfler, and Detlef Gabel
pp 5817–5819Publication Date (Web): November 15, 2002 (Brief Article)
DOI: 10.1021/jm020971k