Journal of Medicinal Chemistry
Volume 44, Issue 11 (May 24, 2001)
Copyright © 2001 American Chemical Society

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PERSPECTIVES

1627-1653

Recent Developments in the Biology and Medicinal Chemistry of Potassium Channel Modulators: Update from a Decade of Progress Michael J. Coghlan, William A. Carroll, and Murali Gopalakrishnan [Full Article - PDF]

LETTERS

1654-1657

Design, Synthesis, and Preclinical Characterization of Novel, Highly Selective Indole Estrogens Chris P. Miller, Michael D. Collini, Bach D. Tran, Heather A. Harris, Yogendra P. Kharode, James T. Marzolf, Robert A. Moran, Ruth A. Henderson, Reinhold H. W. Bender, Rayomond J. Unwalla, Lee M. Greenberger, John P. Yardley, Magid A. Abou-Gharbia, C. Richard Lyttle, and Barry S. Komm [Full Article - PDF]

EXPEDITED ARTICLES

1658-1665

Antiplasmodial Activity and Cytotoxicity of Bis-, Tris-, and Tetraquinolines with Linear or Cyclic Amino Linkers Sophie Girault, Philippe Grellier, Amaya Berecibar, Louis Maes, Pascal Lemière, Elisabeth Mouray, Elisabeth Davioud-Charvet, and Christian Sergheraert [Full Article - PDF]

ARTICLES

1666-1674

Development of a Pharmacophore Model for Histamine H3 Receptor Antagonists, Using the Newly Developed Molecular Modeling Program SLATE Iwan J. P. De Esch, James E. J. Mills, Tim D. J. Perkins, Giuseppe Romeo, Marcel Hoffmann, Kerstin Wieland, Rob Leurs, Wiro M. P. B. Menge, Paul H. J. Nederkoorn, Philip M. Dean, and Henk Timmerman [Full Article - PDF]

1675-1689

Stepwise Modulation of Neurokinin-3 and Neurokinin-2 Receptor Affinity and Selectivity in Quinoline Tachykinin Receptor Antagonists Frank E. Blaney, Luca F. Raveglia, Marco Artico, Stefano Cavagnera, Catherine Dartois, Carlo Farina, Mario Grugni, Stefania Gagliardi, Mark A. Luttmann, Marisa Martinelli, Guy M. M. G. Nadler, Carlo Parini, Paola Petrillo, Henry M. Sarau, Mark A. Scheideler, Douglas W. P. Hay, and Giuseppe A. M. Giardina [Full Article - PDF]

1690-1701

Structural Basis of Binding of High-Affinity Ligands to Protein Kinase C: Prediction of the Binding Modes through a New Molecular Dynamics Method and Evaluation by Site-Directed Mutagenesis Youngshang Pak, Istvan J. Enyedy, Judith Varady, Justin W. Kung, Patricia S. Lorenzo, Peter M. Blumberg, and Shaomeng Wang [Full Article - PDF]

1702-1709

Ether Phospholipid-AZT Conjugates Possessing Anti-HIV and Antitumor Cell Activity. Synthesis, Conformational Analysis, and Study of Their Thermal Effects on Membrane Bilayers Thomas Mavromoustakos, Theodora Calogeropoulou, Maria Koufaki, Antonios Kolocouris, Ioanna Daliani, Costas Demetzos, Zhaoxing Meng, Alexandros Makriyannis, Jan Balzarini, and Erik De Clercq [Full Article - PDF]

1710-1717

Quinazolin-4-one -Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonists: Structure-Activity Relationship of the C-2 Side Chain Tether Bertrand L. Chenard, Willard M. Welch, James F. Blake, Todd W. Butler, Anthony Reinhold, Frank E. Ewing, Frank S. Menniti, and Martin J. Pagnozzi [Full Article - PDF]

1718-1728

Discovery of Novel Aldose Reductase Inhibitors Using a Protein Structure-Based Approach: 3D-Database Search Followed by Design and Synthesis Yoriko Iwata, Mitsuhiro Arisawa, Ryuji Hamada, Yasuyuki Kita, Miho Y. Mizutani, Nobuo Tomioka, Akiko Itai, and Shuichi Miyamoto [Full Article - PDF]

1729-1740

Homology Modeling Using Multiple Molecular Dynamics Simulations and Docking Studies of the Human Androgen Receptor Ligand Binding Domain Bound to Testosterone and Nonsteroidal Ligands Craig A. Marhefka, Bob M. Moore II, Thomas C. Bishop, Leonid Kirkovsky, Arnab Mukherjee, James T. Dalton, and Duane D. Miller [Full Article - PDF]

1741-1748

Diguanidino and "Reversed" Diamidino 2,5-Diarylfurans as Antimicrobial Agents Chad E. Stephens, Farial Tanious, Susan Kim, W. David Wilson, Wiley A. Schell, John R. Perfect, Scott G. Franzblau, and David W. Boykin [Full Article - PDF]

1749-1757

Synthesis and Biological Evaluation of Purine-Containing Butenolides Gholam H. Hakimelahi, Nai-Wen Mei, Ali A. Moosavi-Movahedi, Hady Davari, Shahram Hakimelahi, Ke-Yung King, Jih Ru Hwu, and Yuh-Sheng Wen [Full Article - PDF]

1758-1776

Design, Synthesis, and Biological Evaluation of Analogues of the Antitumor Agent, 2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic Acid (XK469) Stuart T. Hazeldine, Lisa Polin, Juiwanna Kushner, Jennifer Paluch, Kathryn White, Matthew Edelstein, Eduardo Palomino, Thomas H. Corbett, and Jerome P. Horwitz [Full Article - PDF]

1777-1793

Potent Reversible Inhibitors of the Protein Tyrosine Phosphatase CD45 Rebecca A. Urbanek, Suzanne J. Suchard, Gary B. Steelman, Katharine S. Knappenberger, Linda A. Sygowski, Chris A. Veale, and Marc J. Chapdelaine [Full Article - PDF]

1794-1801

Enantioselective Syntheses of Dopaminergic (R)- and (S)-Benzyltetrahydroisoquinolines Nuria Cabedo, Inmaculada Andreu, M. Carmen Ramírez de Arellano, Abdeslam Chagraoui, Angel Serrano, Almudena Bermejo, Philippe Protais, and Diego Cortes [Full Article - PDF]

1802-1814

Estradiol-16-carboxylic Acid Esters as Locally Active Estrogens David C. Labaree, Toni Y. Reynolds, and Richard B. Hochberg [Full Article - PDF]

1815-1826

Synthesis and Structure-Activity Relationships of Naphthamides as Dopamine D3 Receptor Ligands Yunsheng Huang, Robert R. Luedtke, Rebekah A. Freeman, Li Wu, and Robert H. Mach [Full Article - PDF]

1827-1832

QSAR and Molecular Modeling Studies of Baclofen Analogues as GABAB Agonists. Insights into the Role of the Aromatic Moiety in GABAB Binding and Activation Gabriele Costantino, Antonio Macchiarulo, Antonio Entrena Guadix, and Roberto Pellicciari [Full Article - PDF]

BRIEF ARTICLES

1833-1836

Phenanthroindolizidine Alkaloids as Cytotoxic Substances in a Danaid Butterfly, Ideopsis similis, against Human Cancer Cells Hajime Komatsu, Masahiko Watanabe, Masayoshi Ohyama, Takeji Enya, Kotaro Koyama, Takashi Kanazawa, Nobuo Kawahara, Takashi Sugimura, and Keiji Wakabayashi [Full Article - PDF]

1837-1840

The Role of Sugar Residues in Molecular Recognition by Vancomycin Jeffrey Kaplan, Brian D. Korty, Paul H. Axelsen, and Patrick J. Loll [Full Article - PDF]