Table of Contents
June 6, 2002
Volume 45, Issue 12
Pages 2349-2674
Letters
A New Type of Prodrug of Catecholamines: An Opportunity to Improve the Treatment of Parkinson's Disease
Bastiaan J. Venhuis, Håkan V. Wikström, Nienke Rodenhuis, Staffan Sundell, and Durk Dijkstra
pp 2349–2351Publication Date (Web): May 10, 2002 (Letter)
DOI: 10.1021/jm025508m
Hi-Res PDFArylaminoethyl Amides as Novel Non-Covalent Cathepsin K Inhibitors
Eva Altmann, Johanne Renaud, Jonathan Green, David Farley, Brian Cutting, and Wolfgang Jahnke
pp 2352–2354Publication Date (Web): May 10, 2002 (Letter)
DOI: 10.1021/jm010801s
Synthesis of 3,4-Dihydro-2H-1,2,4-benzo- thiadiazine 1,1-Dioxide Derivatives as Potential Allosteric Modulators of AMPA/Kainate Receptors
Daniela Braghiroli, Giulia Puia, Giuseppe Cannazza, Annalisa Tait, Carlo Parenti, Gabriele Losi, and Mario Baraldi
pp 2355–2357Publication Date (Web): May 09, 2002 (Letter)
DOI: 10.1021/jm025510d
Synthesis and Antiproliferative Activity of a New Compound Containing an α-Methylene-γ-Lactone Group
Antonio G. González, Margarita Hernández Silva, Juan I. Padrón, Francisco León, Eduardo Reyes, Melchor Álvarez-Mon, Juan P. Pivel, José Quintana, Francisco Estévez, and Jaime Bermejo
pp 2358–2361Publication Date (Web): May 11, 2002 (Letter)
DOI: 10.1021/jm025518n
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties
Edwin B. Villhauer, John A. Brinkman, Goli B. Naderi, Beth E. Dunning, Bonnie L. Mangold, Manisha D. Mone, Mary E. Russell, Stephen C. Weldon, and Thomas E. Hughes
pp 2362–2365Publication Date (Web): May 09, 2002 (Letter)
DOI: 10.1021/jm025522z
Articles
Structural Classification of Protein Kinases Using 3D Molecular Interaction Field Analysis of Their Ligand Binding Sites: Target Family Landscapes
Thorsten Naumann and Hans Matter
pp 2366–2378Publication Date (Web): May 07, 2002 (Article)
DOI: 10.1021/jm011002c
SAR and X-ray. A New Approach Combining Fragment-Based Screening and Rational Drug Design: Application to the Discovery of Nanomolar Inhibitors of Src SH2
Dominique Lesuisse, Gudrun Lange, Pierre Deprez, Didier Bénard, Bernard Schoot, Georges Delettre, Jean-Pierre Marquette, Pierre Broto, Véronique Jean-Baptiste, Paulette Bichet, Edoardo Sarubbi, and Eliane Mandine
pp 2379–2387Publication Date (Web): May 02, 2002 (Article)
DOI: 10.1021/jm010927p
3-Aminopyrrolidinone Farnesyltransferase Inhibitors: Design of Macrocyclic Compounds with Improved Pharmacokinetics and Excellent Cell Potency
Ian M. Bell, Steven N. Gallicchio, Marc Abrams, Lorena S. Beese, Douglas C. Beshore, Hema Bhimnathwala, Michael J. Bogusky, Carolyn A. Buser, J. Christopher Culberson, Joseph Davide, Michelle Ellis-Hutchings, Christine Fernandes, Jackson B. Gibbs, Samuel L. Graham, Kelly A. Hamilton, George D. Hartman, David C. Heimbrook, Carl F. Homnick, Hans E. Huber, Joel R. Huff, Kelem Kassahun, Kenneth S. Koblan, Nancy E. Kohl, Robert B. Lobell, Joseph J. Lynch, Jr., Ronald Robinson, A. David Rodrigues, Jeffrey S. Taylor, Eileen S. Walsh, Theresa M. Williams, and C. Blair Zartman
pp 2388–2409Publication Date (Web): May 03, 2002 (Article)
DOI: 10.1021/jm010531d
Inhibition of MIF Bioactivity by Rational Design of Pharmacological Inhibitors of MIF Tautomerase Activity
Angeles Dios, Robert A. Mitchell, Bayan Aljabari, Jodi Lubetsky, KerryAnn O'Connor, Hong Liao, Peter D. Senter, Kirk R. Manogue, Elias Lolis, Christine Metz, Richard Bucala, David J. E. Callaway, and Yousef Al-Abed
pp 2410–2416Publication Date (Web): May 09, 2002 (Article)
DOI: 10.1021/jm010534q
Discovery of Potent, Nonsteroidal, and Highly Selective Glucocorticoid Receptor Antagonists
Bradley P. Morgan, Andrew G. Swick, Diane M. Hargrove, Janet A. LaFlamme, Melinda S. Moynihan, Richard S. Carroll, Kelly A. Martin, Eunsun Lee, Debra Decosta, and Jon Bordner
pp 2417–2424Publication Date (Web): May 10, 2002 (Article)
DOI: 10.1021/jm0105530
Discovery and Biological Evaluation of a New Family of Potent Modulators of Multidrug Resistance: Reversal of Multidrug Resistance of Mouse Lymphoma Cells by New Natural Jatrophane Diterpenoids Isolated from Euphorbia Species
Judit Hohmann, Joseph Molnár, Dóra Rédei, Ferenc Evanics, Peter Forgo, Alajos Kálmán, Gyula Argay, and Pál Szabó
pp 2425–2431Publication Date (Web): May 14, 2002 (Article)
DOI: 10.1021/jm0111301
Design of Selective Thrombin Inhibitors Based on the (R)-Phe-Pro-Arg Sequence
John C. Danilewicz, Stuart M. Abel, Alan D. Brown, Paul V. Fish, Edward Hawkeswood, Stephen J. Holland, Keith James, Andrew B. McElroy, John Overington, Michael J. Powling, and David J. Rance
pp 2432–2453Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm011133d
Novel Class of Potent 4-Arylalkyl Substituted 3-Isoxazolol GABAA Antagonists: Synthesis, Pharmacology, and Molecular Modeling
Bente Frølund, Anne T. Jørgensen, Lena Tagmose, Tine B. Stensbøl, Henrik T. Vestergaard, Christine Engblom, Uffe Kristiansen, Connie Sanchez, Povl Krogsgaard-Larsen, and Tommy Liljefors
pp 2454–2468Publication Date (Web): May 04, 2002 (Article)
DOI: 10.1021/jm020027o
Simple, Intuitive Calculations of Free Energy of Binding for Protein−Ligand Complexes. 1. Models without Explicit Constrained Water
Pietro Cozzini, Micaela Fornabaio, Anna Marabotti, Donald J. Abraham, Glen E. Kellogg, and Andrea Mozzarelli
pp 2469–2483Publication Date (Web): May 04, 2002 (Article)
DOI: 10.1021/jm0200299
Design, Synthesis, and Activity of a Novel Series of Factor Xa Inhibitors: Optimization of Arylamidine Groups1,2
Gary Phillips, William J. Guilford, Brad O. Buckman, David D. Davey, Keith A. Eagen, Sunil Koovakkat, Amy Liang, Meg McCarrick, Raju Mohan, Howard P. Ng, Michael Pinkerton, Babu Subramanyam, Elena Ho, Lan Trinh, Marc Whitlow, Shung Wu, Wei Xu, and Michael M. Morrissey
pp 2484–2493Publication Date (Web): May 02, 2002 (Article)
DOI: 10.1021/jm0200660
Evaluation of a Novel Shape-Based Computational Filter for Lead Evolution: Application to Thrombin Inhibitors
Jayashree Srinivasan, Angelo Castellino, Erin K. Bradley, John E. Eksterowicz, Peter D. J. Grootenhuis, Santosh Putta, and Robert V. Stanton
pp 2494–2500Publication Date (Web): May 07, 2002 (Article)
DOI: 10.1021/jm010494q
Conformations and Receptor Activity of Desmopressin Analogues, Which Contain γ-Turn Mimetics or a Ψ[CH2O] Isostere
Mattias Hedenström, ZhongQing Yuan, Kay Brickmann, Jolanta Carlsson, Kjell Ekholm, Birgitta Johansson, Eva Kreutz, Anders Nilsson, Ingmar Sethson, and Jan Kihlberg
pp 2501–2511Publication Date (Web): May 04, 2002 (Article)
DOI: 10.1021/jm011073b
Synthesis and Pharmacological Evaluation of an Analogue of the Peptide Hormone Oxytocin That Contains a Mimetic of an Inverse γ-Turn
ZhongQing Yuan, David Blomberg, Ingmar Sethson, Kay Brickmann, Kjell Ekholm, Birgitta Johansson, Anders Nilsson, and Jan Kihlberg
pp 2512–2519Publication Date (Web): May 04, 2002 (Article)
DOI: 10.1021/jm0110744
Novel Selective PDE4 Inhibitors. 3. In Vivo Antiinflammatory Activity of a New Series of N-Substituted cis-Tetra- and cis-Hexahydrophthalazinones
Margaretha Van der Mey, Hildegard Boss, Armin Hatzelmann, Ivonne J. Van der Laan, Geert J. Sterk, and Hendrik Timmerman
pp 2520–2525Publication Date (Web): May 14, 2002 (Article)
DOI: 10.1021/jm0110340
Novel Selective Phosphodiesterase (PDE4) Inhibitors. 4. Resolution, Absolute Configuration, and PDE4 Inhibitory Activity of cis-Tetra- and cis-Hexahydrophthalazinones
Margaretha Van der Mey, Hildegard Boss, Dennis Couwenberg, Armin Hatzelmann, Geert J. Sterk, Kees Goubitz, Henk Schenk, and Hendrik Timmerman
pp 2526–2533Publication Date (Web): February 26, 2002 (Article)
DOI: 10.1021/jm0110338
Antineoplastic Agents. 465. Structural Modification of Resveratrol: Sodium Resverastatin Phosphate1
George R. Pettit, Matthew P. Grealish, M. Katherine Jung, Ernest Hamel, Robin K. Pettit, J.-Charles Chapuis, and Jean M. Schmidt
pp 2534–2542Publication Date (Web): May 10, 2002 (Article)
DOI: 10.1021/jm010119y
3-Aryl-2-Quinolone Derivatives: Synthesis and Characterization of In Vitro and In Vivo Antitumor Effects with Emphasis on a New Therapeutical Target Connected with Cell Migration
Benoît Joseph, Francis Darro, Aurélie Béhard, Brigitte Lesur, Françoise Collignon, Christine Decaestecker, Armand Frydman, Gérald Guillaumet, and Robert Kiss
pp 2543–2555Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm010978m
Synthesis and Structure−Activity Relationship of 2-Aminobenzophenone Derivatives as Antimitotic Agents
Jing-Ping Liou, Chun-Wei Chang, Jeng-Shin Song, Yung-Ning Yang, Ching-Fang Yeh, Huan-Yi Tseng, Yu-Kang Lo, Yi-Ling Chang, Chung-Ming Chang, and Hsing-Pang Hsieh
pp 2556–2562Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm010365+
Full Text HTMLPotent Antimalarial Febrifugine Analogues against the Plasmodium Malaria Parasite
Haruhisa Kikuchi, Hidehisa Tasaka, Shingo Hirai, Yoshiaki Takaya, Yoshiharu Iwabuchi, Hidenori Ooi, Susumi Hatakeyama, Hye-Sook Kim, Yusuke Wataya, and Yoshiteru Oshima
pp 2563–2570Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm010448q
Endomorphin-1 Analogues Containing β-Proline Are μ-Opioid Receptor Agonists and Display Enhanced Enzymatic Hydrolysis Resistance
Giuliana Cardillo, Luca Gentilucci, Ahmed R. Qasem, Fabio Sgarzi, and Santi Spampinato
pp 2571–2578Publication Date (Web): May 09, 2002 (Article)
DOI: 10.1021/jm011059z
Synthesis and Characterization of Fluorescent Antagonists and Agonists for Human Oxytocin and Vasopressin V1a Receptors
Sonia Terrillon, Ling Ling Cheng, Stoytcho Stoev, Bernard Mouillac, Claude Barberis, Maurice Manning, and Thierry Durroux
pp 2579–2588Publication Date (Web): May 09, 2002 (Article)
DOI: 10.1021/jm010526+
Synthesis and Pharmacological Evaluation of 5-(4-Biphenyl)-3-methyl-4-phenyl-1,2,4-triazole Derivatives as a Novel Class of Selective Antagonists for the Human Vasopressin V1A Receptor
Akio Kakefuda, Takeshi Suzuki, Takahiko Tobe, Junko Tsukada, Atsuo Tahara, Shuichi Sakamoto, and Shin-ichi Tsukamoto
pp 2589–2598Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm010544r
Design, Synthesis, and Antiproliferative Activity of Some New Pyrazole-Fused Amino Derivatives of the Pyranoxanthenone, Pyranothioxanthenone, and Pyranoacridone Ring Systems: A New Class of Cytotoxic Agents
Ioannis K. Kostakis, Prokopios Magiatis, Nicole Pouli, Panagiotis Marakos, Alexios-Leandros Skaltsounis, Harris Pratsinis, Stephane Léonce, and Alain Pierré
pp 2599–2609Publication Date (Web): May 10, 2002 (Article)
DOI: 10.1021/jm011117g
NMR-Based Screening with Competition Water−Ligand Observed via Gradient Spectroscopy Experiments: Detection of High-Affinity Ligands
Claudio Dalvit, Marina Fasolini, Maria Flocco, Stefan Knapp, Paolo Pevarello, and Marina Veronesi
pp 2610–2614Publication Date (Web): May 10, 2002 (Article)
DOI: 10.1021/jm011122k
Molecular Properties That Influence the Oral Bioavailability of Drug Candidates
Daniel F. Veber, Stephen R. Johnson, Hung-Yuan Cheng, Brian R. Smith, Keith W. Ward, and Kenneth D. Kopple
pp 2615–2623Publication Date (Web): May 11, 2002 (Article)
DOI: 10.1021/jm020017n
Synthesis and Protein Kinase Inhibitory Activity of Balanol Analogues with Modified Benzophenone Subunits
John W. Lampe, Christopher K. Biggers, Jean M. Defauw, Robert J. Foglesong, Steven E. Hall, Julia M. Heerding, Sean P. Hollinshead, Hong Hu, Philip F. Hughes, G. Erik Jagdmann, Jr., Mary George Johnson, Yen-Shi Lai, Christopher T. Lowden, Michael P. Lynch, José S. Mendoza, Marcia M. Murphy, Joseph W. Wilson, Lawrence M. Ballas, Kiyomi Carter, James W. Darges, Jefferson E. Davis, Frederick R. Hubbard, and Mark L. Stamper
pp 2624–2643Publication Date (Web): May 02, 2002 (Article)
DOI: 10.1021/jm020018f
Novel Cyclic Templates of α-MSH Give Highly Selective and Potent Antagonists/Agonists for Human Melanocortin-3/4 Receptors
Malcolm J. Kavarana, Dev Trivedi, Minying Cai, Jinfa Ying, Matthew Hammer, Christopher Cabello, Paolo Grieco, Guoxia Han, and Victor J. Hruby
pp 2644–2650Publication Date (Web): May 14, 2002 (Article)
DOI: 10.1021/jm020021z
Sugar-Modified Conjugated Diene Analogues of Adenosine and Uridine: Synthesis, Interaction with S-Adenosyl-l-homocysteine Hydrolase, and Antiviral and Cytostatic Effects
Stanislaw F. Wnuk, Bong-Oh Ro, Carlos A. Valdez, Elzbieta Lewandowska, Neida X. Valdez, Pablo R. Sacasa, Dan Yin, Jinsong Zhang, Ronald T. Borchardt, and Erik De Clercq
pp 2651–2658Publication Date (Web): April 24, 2002 (Article)
DOI: 10.1021/jm020064f
Brief Articles
Structure−Activity Relationship Studies of Nordihydroguaiaretic Acid Inhibitors toward Soybean, 12-Human, and 15-Human Lipoxygenase
Stephanie Whitman, Mikail Gezginci, Barbara N. Timmermann, and Theodore R. Holman
pp 2659–2661Publication Date (Web): May 04, 2002 (Brief Article)
DOI: 10.1021/jm0201262
Synthesis of (+)-cis-N-(4-Isothiocyanatobenzyl)-N-normetazocine, an Isothiocyanate Derivative of N-Benzylnormetazocine as Acylant Agent for the σ1 Receptor
Giuseppe Ronsisvalle, Orazio Prezzavento, Agostino Marrazzo, Franco Vittorio, Michele Massimino, Giovanna Murari, and Santi Spampinato
pp 2662–2665Publication Date (Web): May 02, 2002 (Brief Article)
DOI: 10.1021/jm010501a
Synthesis and Antitumor Activity of 1,5,6-Substituted E-3-(2-Chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones1
Aldo Andreani, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, and Vida Garaliene
pp 2666–2669Publication Date (Web): May 09, 2002 (Brief Article)
DOI: 10.1021/jm011123c
One-Pot Synthesis of Benzo[b]furan and Indole Inhibitors of Tubulin Polymerization
Bernard L. Flynn, Ernest Hamel, and M. Katherine Jung
pp 2670–2673Publication Date (Web): May 04, 2002 (Brief Article)
DOI: 10.1021/jm020077t
Book Reviews
Handbook of GC/MS Fundamentals and Applications By Hans-Joachim Hübschmann. Wiley-VCH, Weinheim, Germany. 2001. xvi + 591 pp. 17.5 × 24.5 cm. ISBN 3-529-30170-4. $150.00.
Rickey P. Hicks
p 2674Publication Date (Web): May 02, 2002 (Book Review)
DOI: 10.1021/jm0201363