Table of Contents
September 11, 2003
Volume 46, Issue 19
Pages 3953-4213
About the Cover: Connolly surface map of the X-ray structure of the α-thrombin-cyclopentenedicarboxylic acid derivative complex (yellow) at 1.9 Å resolution superimposed on the X-ray structure of the α-thrombin-PPACK complex (magenta) (Thorstensson, F.; et al. J. Med. Chem. 2003, 46, 1165-1179).
Letters
Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain
J. Scott Sawyer, Bryan D. Anderson, Douglas W. Beight, Robert M. Campbell, Michael L. Jones, David K. Herron, John W. Lampe, Jefferson R. McCowan, William T. McMillen, Nicholas Mort, Stephen Parsons, Edward C. R. Smith, Michal Vieth, Leonard C. Weir, Lei Yan, Faming Zhang, and Jonathan M. Yingling
pp 3953–3956Publication Date (Web): August 12, 2003 (Letter)
DOI: 10.1021/jm0205705
Hi-Res PDFThe First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists
Jill A. Jablonowski, Cheryl A. Grice, Wenying Chai, Curt A. Dvorak, Jennifer D. Venable, Annette K. Kwok, Kiev S. Ly, Jianmei Wei, Sherry M. Baker, Pragnya J. Desai, Wen Jiang, Sandy J. Wilson, Robin L. Thurmond, Lars Karlsson, James P. Edwards, Timothy W. Lovenberg, and Nicholas I. Carruthers
pp 3957–3960Publication Date (Web): July 24, 2003 (Letter)
DOI: 10.1021/jm0341047
Discovery and Preclinical Characterization of (+)-3-[4-(1- Piperidinoethoxy)phenyl]spiro[indene- 1,1‘-indane]-5,5‘-diol Hydrochloride: A Promising Nonsteroidal Estrogen Receptor Agonist for Hot Flush
Nobuhide Watanabe, Akihisa Ikeno, Hisao Minato, Hiroshi Nakagawa, Chie Kohayakawa, and Jun-ichi Tsuji
pp 3961–3964Publication Date (Web): August 13, 2003 (Letter)
DOI: 10.1021/jm034134+
Full Text HTML Articles
Receptor-Mediated Targeting of a Photosensitizer by Its Conjugation to Gonadotropin-Releasing Hormone Analogues
Shai Rahimipour, Nurit Ben-Aroya, Keren Ziv, Alon Chen, Mati Fridkin, and Yitzhak Koch
pp 3965–3974Publication Date (Web): August 12, 2003 (Article)
DOI: 10.1021/jm020535y
Synthesis and Cyclooxygenase-2 Inhibiting Property of 1,5-Diarylpyrazoles with Substituted Benzenesulfonamide Moiety as Pharmacophore: Preparation of Sodium Salt for Injectable Formulation†
Manojit Pal, Manjula Madan, Srinivas Padakanti, Vijaya R. Pattabiraman, Srinivas Kalleda, Akhila Vanguri, Ramesh Mullangi, N. V. S. Rao Mamidi, Seshagiri R. Casturi, Alpeshkumar Malde, B. Gopalakrishnan, and Koteswar R. Yeleswarapu
pp 3975–3984Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm020563g
Synthesis and SAR of Thrombin Inhibitors Incorporating a Novel 4-Amino-Morpholinone Scaffold: Analysis of X-ray Crystal Structure of Enzyme Inhibitor Complex
Jonas W. Nilsson, Ingemar Kvarnström, Djordje Musil, Ingemar Nilsson, and Bertil Samulesson
pp 3985–4001Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm0307990
Effects of the Substitution of Phe4 in the Opioid Peptide [d-Ala8]Dynorphin A-(1−11)NH2
Balvinder S. Vig, Mike Q. Zheng, Thomas F. Murray, and Jane V. Aldrich
pp 4002–4008Publication Date (Web): August 16, 2003 (Article)
DOI: 10.1021/jm030075o
Studies on the Nitroreductase Prodrug-Activating System. Crystal Structures of Complexes with the Inhibitor Dicoumarol and Dinitrobenzamide Prodrugs and of the Enzyme Active Form
Eric Johansson, Gary N. Parkinson, William A. Denny, and Stephen Neidle
pp 4009–4020Publication Date (Web): August 07, 2003 (Article)
DOI: 10.1021/jm030843b
Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors
Gee-Hong Kuo, Catherine Prouty, Alan DeAngelis, Lan Shen, David J. O'Neill, Chandra Shah, Peter J. Connolly, William V. Murray, Bruce R. Conway, Peter Cheung, Lori Westover, Jun Z. Xu, Richard A. Look, Keith T. Demarest, Stuart Emanuel, Steven A. Middleton, Linda Jolliffe, Mary Pat Beavers, and Xin Chen
pp 4021–4031Publication Date (Web): August 12, 2003 (Article)
DOI: 10.1021/jm030115o
Novel Estrogen Receptor Ligands Based on an Anthranylaldoxime Structure: Role of the Phenol-Type Pseudocycle in the Binding Process
Filippo Minutolo, Michela Antonello, Simone Bertini, Gabriella Ortore, Giorgio Placanica, Simona Rapposelli, Shubin Sheng, Kathryn E. Carlson, Benita S. Katzenellenbogen, John A. Katzenellenbogen, and Marco Macchia
pp 4032–4042Publication Date (Web): August 16, 2003 (Article)
DOI: 10.1021/jm0308390
Polymer-Assisted Solution-Phase Library Synthesis and Crystal Structure of α-Ketothiazoles as Tissue Factor VIIa Inhibitors
John J. Parlow, Thomas A. Dice, Rhonda M. Lachance, Thomas J. Girard, Anna M. Stevens, Roderick A. Stegeman, William C. Stallings, Ravi G. Kurumbail, and Michael S. South
pp 4043–4049Publication Date (Web): August 09, 2003 (Article)
DOI: 10.1021/jm030130t
Design, Parallel Synthesis, and Crystal Structures of Pyrazinone Antithrombotics as Selective Inhibitors of the Tissue Factor VIIa Complex
John J. Parlow, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Michael J. Hayes, Darin E. Jones, William L. Neumann, Rhonda S. Wood, Rhonda M. Lachance, Thomas J. Girard, Nancy S. Nicholson, Michael Clare, Roderick A. Stegeman, Anna M. Stevens, William C. Stallings, Ravi G. Kurumbail, and Michael S. South
pp 4050–4062Publication Date (Web): August 09, 2003 (Article)
DOI: 10.1021/jm030131l
Selectivity Fields: Comparative Molecular Field Analysis (CoMFA) of the Glycine/NMDA and AMPA Receptors
Igor I. Baskin, Irina G. Tikhonova, Vladimir A. Palyulin, and Nikolai S. Zefirov
pp 4063–4069Publication Date (Web): August 09, 2003 (Article)
DOI: 10.1021/jm030833a
CCR2: Characterization of the Antagonist Binding Site from a Combined Receptor Modeling/Mutagenesis Approach
Theo A. Berkhout, Frank E. Blaney, Angela M. Bridges, David G. Cooper, Ian T. Forbes, Andrew D. Gribble, Pieter H. E. Groot, Adam Hardy, Robert J. Ife, Rejbinder Kaur, Kitty E. Moores, Helen Shillito, Jennifer Willetts, and Jason Witherington
pp 4070–4086Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm030862l
Design, Synthesis, and Structure−Activity Relationship Studies of Novel 6,7-Locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic Acids
Pierre-Yves Michellys, Robert J. Ardecky, Jyun-Hung Chen, Jennifer D'Arrigo, Timothy A. Grese, Donald S. Karanewsky, Mark D. Leibowitz, Sha Liu, Dale A. Mais, Christopher M. Mapes, Chahrzad Montrose-Rafizadeh, Katheen M. Ogilvie Anne Reifel-Miller, Deepa Rungta, Anthony W. Thompson, John S. Tyhonas, and Marcus F. Boehm
pp 4087–4103Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm020401k
5-Benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as Selective Progesterone Receptor Modulators
Lin Zhi, Christopher M. Tegley, Barbara Pio, James P. Edwards, Mehrnouch Motamedi, Todd K. Jones, Keith B. Marschke, Dale E. Mais, Boris Risek, and William T. Schrader
pp 4104–4112Publication Date (Web): August 14, 2003 (Article)
DOI: 10.1021/jm020477g
Ascochlorin Derivatives as Ligands for Nuclear Hormone Receptors
Marie Togashi, Satoshi Ozawa, Shoko Abe, Tomoyuki Nishimura, Mie Tsuruga, Kunio Ando, Gakuzo Tamura, Shigefumi Kuwahara, Makoto Ubukata, and Junji Magae
pp 4113–4123Publication Date (Web): August 19, 2003 (Article)
DOI: 10.1021/jm0205649
Development of Water-Soluble Prodrugs of the HIV-1 Protease Inhibitor KNI-727: Importance of the Conversion Time for Higher Gastrointestinal Absorption of Prodrugs Based on Spontaneous Chemical Cleavage
Youhei Sohma, Yoshio Hayashi, Tomoko Ito, Hikaru Matsumoto, Tooru Kimura, and Yoshiaki Kiso
pp 4124–4135Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm030009m
Orally Active Oxime Derivatives of the Dopaminergic Prodrug 6-(N,N-Di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and Pharmacological Activity
Bastiaan J. Venhuis, Durk Dijkstra, David Wustrow, Len T. Meltzer, Lawrence D. Wise, Stephen J. Johnson, and Håkan V. Wikström
pp 4136–4140Publication Date (Web): August 19, 2003 (Article)
DOI: 10.1021/jm0307786
In Vitro Analysis of Stable, Receptor-Selective Neurotensin[8−13] Analogues
Kyle P. Kokko, M. Kyle Hadden, Kevin S. Orwig, Jean Mazella, and Thomas A. Dix
pp 4141–4148Publication Date (Web): August 12, 2003 (Article)
DOI: 10.1021/jm0300633
Ring-Expanded (“Fat”) Nucleoside and Nucleotide Analogues Exhibit Potent in Vitro Activity against Flaviviridae NTPases/Helicases, Including Those of the West Nile Virus, Hepatitis C Virus, and Japanese Encephalitis Virus
Ning Zhang, Huan-Ming Chen, Verena Koch, Herbert Schmitz, Ching-Len Liao, Maria Bretner, Vishweshwar S. Bhadti, Ali I. Fattom, Robert B. Naso, Ramachandra S. Hosmane, and Peter Borowski
pp 4149–4164Publication Date (Web): August 13, 2003 (Article)
DOI: 10.1021/jm030842j
Studies on the Structure−Activity Relationship of Endostatin: Synthesis of Human Endostatin Peptides Exhibiting Potent Antiangiogenic Activities
Francesco Chillemi and Pierangelo FrancescatoEnzio RaggMaria Grazia Cattaneo, Sandra Pola, and Lucia Vicentini
pp 4165–4172Publication Date (Web): August 07, 2003 (Article)
DOI: 10.1021/jm0308287
Soft Antimicrobial Agents: Synthesis and Activity of Labile Environmentally Friendly Long Chain Quaternary Ammonium Compounds
Thorsteinn Thorsteinsson, Már Másson, Karl G. Kristinsson, Martha A. Hjálmarsdóttir, Hilmar Hilmarsson, and Thorsteinn Loftsson
pp 4173–4181Publication Date (Web): August 05, 2003 (Article)
DOI: 10.1021/jm030829z
Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 20.1 14-Phenylpropoxymetopon: An Extremely Powerful Analgesic
Johannes Schütz, Mariana Spetea, Martin Koch, Mario D. Aceto, Louis S. Harris, Andrew Coop, and Helmut Schmidhammer
pp 4182–4187Publication Date (Web): August 14, 2003 (Article)
DOI: 10.1021/jm030878b
A Novel and Selective 5-HT2 Receptor Agonist with Ocular Hypotensive Activity: (S)-(+)-1-(2-Aminopropyl)-8,9-dihydropyrano[3,2-e]indole
Jesse A. May, Hwang-Hsing Chen, Andrew Rusinko, Vincent M. Lynch, Najam A. Sharif, and Marsha A. McLaughlin
pp 4188–4195Publication Date (Web): August 08, 2003 (Article)
DOI: 10.1021/jm030205t
New Bivalent PKC Ligands Linked by a Carbon Spacer: Enhancement in Binding Affinity
Jayalakshmi Sridhar, Zhi-Liang Wei, Ireneusz Nowak, Nancy E. Lewin, Jolene A. Ayres, Larry V. Pearce, Peter M. Blumberg, and Alan P. Kozikowski
pp 4196–4204Publication Date (Web): August 09, 2003 (Article)
DOI: 10.1021/jm0302041
Brief Articles
Synthesis and Cytotoxic Activity of Two Novel 1-Dodecylthio-2-decyloxypropyl-3-phosphatidic Acid Conjugates with Gemcitabine and Cytosine Arabinoside
Richard L. Alexander, Susan L. Morris-Natschke, Khalid S. Ishaq, Ronald A. Fleming, and Gregory L. Kucera
pp 4205–4208Publication Date (Web): August 09, 2003 (Brief Article)
DOI: 10.1021/jm020571x
Biosynthetic Origin of a Branched Chain Analogue of the Lipase Inhibitor, Lipstatin
Wolfgang Eisenreich, Ernst Kupfer, Peter Stohler, Wolfgang Weber, and Adelbert Bacher
pp 4209–4212Publication Date (Web): August 06, 2003 (Brief Article)
DOI: 10.1021/jm030780x
Book Reviews
Annual Review of Pharmacology and Toxicology. Volume 43 Edited by A. K. Cho, T. F. Blaschke, P. A. Insel, and H. H. Loh. Annual Reviews, Palo Alto, CA. 2003. vii + 710 pp. 15.5 × 23.5 cm. ISBN 0-8243-0443-8. $70.00.
S. J. Enna
p 4213Publication Date (Web): August 13, 2003 (Book Review)
DOI: 10.1021/jm0303249
Handbook of Aqueous Solubility Data By Samuel H. Yalkowsky and Yan He. CRC Press, Boca Raton, FL. 2003. xii + 1496 pp. 18 × 26 cm. ISBN 0-89493-1532-8. $299.95.
J. Keith Guillory
p 4213Publication Date (Web): August 09, 2003 (Book Review)
DOI: 10.1021/jm0303251