Journal of Medicinal Chemistry
Volume 41, Issue 11 (May 21, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

1741-1744

Potent Antagonists of the SH2 Domain of Grb2: Optimization of the X+1 Position of 3-Amino-Z-Tyr(PO3H2)-X+1-Asn-NH2 Carlos García-Echeverría, Pascal Furet, Brigitte Gay, Heinz Fretz, Joseph Rahuel, Joseph Schoepfer, and Giorgio Caravatti [Full Article - PDF]

1745-1748

Design and Synthesis of Cyclic Inhibitors of Matrix Metalloproteinases and TNF- Production Chu-Biao Xue, Xiaohua He, John Roderick, William F. DeGrado,2 Robert J. Cherney, Karl D. Hardman, David J. Nelson, Robert A. Copeland, Bruce D. Jaffee, and Carl P. Decicco,3 [Full Article - PDF]

1749-1751

Macrocyclic Amino Carboxylates as Selective MMP-8 Inhibitors Robert J. Cherney, Li Wang, Dayton T. Meyer, Chu-Baio Xue, Zelda R. Wasserman, Karl D. Hardman, Patty K. Welch, Maryanne B. Covington, Robert A. Copeland, Elizabeth C. Arner, William F. DeGrado, and Carl P. Decicco [Full Article - PDF]

ARTICLES

1752-1763

Development of a Binding Model to Protein Tyrosine Kinases for Substituted Pyrido[2,3-d]pyrimidine Inhibitors Susanne Trumpp-Kallmeyer, J. Ronald Rubin, Christine Humblet, James M. Hamby, and H. D. Hollis Showalter [Full Article - PDF]

1764-1776

32-Ascomycinyloxyacetic Acid Derived Immunosuppressants. Independence of Immunophilin Binding and Immunosuppressive Potency Rolf Wagner, Teresa A. Rhoades, Yat Sun Or, Benjamin C. Lane, Gin Hsieh, Karl W. Mollison, and Jay R. Luly [Full Article - PDF]

1777-1788

Structure-Activity Relationship of 2-[[(2-Pyridyl)methyl]thio]-1H- benzimidazoles as Anti Helicobacter pylori Agents in Vitro and Evaluation of their in Vivo Efficacy Thomas C. Kühler, Marianne Swanson, Vladimir Shcherbuchin, Håkan Larsson, Björn Mellgård, and Jan-Eric Sjöström [Full Article - PDF]

1789-1802

Hydroxyphthalocyanines as Potential Photodynamic Agents for Cancer Therapy Mougang Hu, Nicole Brasseur, S. Zeki Yildiz, Johan E. van Lier, and Clifford C. Leznoff [Full Article - PDF]

1803-1814

Three-Dimensional Models of Estrogen Receptor Ligand Binding Domain Complexes, Based on Related Crystal Structures and Mutational and Structure-Activity Relationship Data Jean-Marie Wurtz, Ursula Egner, Nikolaus Heinrich, Dino Moras, and Anke Mueller-Fahrnow [Full Article - PDF]

1815-1826

Molecular Modeling of Phenothiazines and Related Drugs As Multidrug Resistance Modifiers: A Comparative Molecular Field Analysis Study Ilza Pajeva and Michael Wiese [Full Article - PDF]

1827-1837

Synthesis, Rotamer Orientation, and Calcium Channel Modulation Activities of Alkyl and 2-Phenethyl 1,4-Dihydro-2,6-dimethyl-3-nitro-4-(3- or 6-substituted-2-pyridyl)-5-pyridinecarboxylates Nadeem Iqbal, Murthy R. Akula, Dean Vo, Wandikayi C. Matowe, Carol-Anne McEwen, Michael W. Wolowyk, and Edward E. Knaus [Full Article - PDF]

1838-1845

Identification of Novel Ligands for the Gabapentin Binding Site on the 2 Subunit of a Calcium Channel and Their Evaluation as Anticonvulsant Agents Justin S. Bryans, Natasha Davies, Nicolas S. Gee, Visaka U. K. Dissanayake, Giles S. Ratcliffe, David C. Horwell, Clare O. Kneen, Andrew I. Morrell, Ryszard J. Oles, John C. O'Toole, Gemma M. Perkins, Lakhbir Singh, Nirmala Suman-Chauhan, and Jacqueline A. O'Neill [Full Article - PDF]

1846-1854

Propofol Analogues. Synthesis, Relationships between Structure and Affinity at GABAA Receptor in Rat Brain, and Differential Electrophysiological Profile at Recombinant Human GABAA Receptors Giuseppe Trapani, Andrea Latrofa, Massimo Franco, Cosimo Altomare, Enrico Sanna, Marcello Usala, Giovanni Biggio, and Gaetano Liso [Full Article - PDF]

1855-1868

New Azole Antifungals. 2. Synthesis and Antifungal Activity of Heterocyclecarboxamide Derivatives of 3-Amino-2-aryl-1-azolyl-2-butanol Javier Bartroli, Enric Turmo, Mònica Algueró, Eulàlia Boncompte, Maria L. Vericat, Lourdes Conte, Joaquim Ramis, Manuel Merlos, Julián García-Rafanell, and Javier Forn [Full Article - PDF]

1869-1882

New Azole Antifungals. 3. Synthesis and Antifungal Activity of 3-Substituted-4(3H)-quinazolinones Javier Bartroli, Enric Turmo, Mònica Algueró, Eulàlia Boncompte, Maria L. Vericat, Lourdes Conte, Joaquim Ramis, Manuel Merlos, Julián García-Rafanell, and Javier Forn [Full Article - PDF]

1883-1893

Synthesis and Structure-Activity Relationships of Bafilomycin A1 Derivatives as Inhibitors of Vacuolar H+-ATPase Stefania Gagliardi, P. Andrea Gatti, Pietro Belfiore, Andrea Zocchetti, Geoffrey D. Clarke, and Carlo Farina [Full Article - PDF]

1894-1908

Potent Dipeptide Inhibitors of the pp60c-src SH2 Domain Gregory J. Pacofsky, Karen Lackey, Krystal J. Alligood, Judd Berman, Paul S. Charifson,,1 Renae M. Crosby, George F. Dorsey, Jr., Paul L. Feldman, Tona M. Gilmer, Conrad W. Hummel,,1 Steven R. Jordan,,1 Christopher Mohr, Lisa M. Shewchuk, Daniel D. Sternbach, and Marc Rodriguez,1 [Full Article - PDF]

1909-1926

Synthesis and Activity of Dipeptides, Linked to Targeting Ligands, as Specific NK Cell Enhancers Shaun D. Abbott, Lyne Gagnon, Mouna Lagraoui, Salam Kadhim, Giorgio Attardo, Boulos Zacharie, and Christopher L. Penney [Full Article - PDF]

1927-1933

Isoxazolidine-3,5-dione and Noncyclic 1,3-Dicarbonyl Compounds as Hypoglycemic Agents Hisashi Shinkai, Syoji Onogi, Masahiro Tanaka, Tsutomu Shibata, Megumi Iwao, Korekiyo Wakitani, and Itsuo Uchida [Full Article - PDF]

1934-1942

(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl]morpholine Methanesulfonate: A New Selective Rat 5-Hydroxytryptamine1B Receptor Antagonist Stefan Berg, Lars-Gunnar Larsson, Lucy Rényi, Svante B. Ross, Seth-Olof Thorberg, and Gun Thorell-Svantesson [Full Article - PDF]

1943-1955

Synthesis and Structure-Activity Relationships of Potent and Orally Active 5-HT4 Receptor Antagonists: Indazole and Benzimidazolone Derivatives John M. Schaus, Dennis C. Thompson, William E. Bloomquist, Alice D. Susemichel, David O. Calligaro, and Marlene L. Cohen [Full Article - PDF]

1956-1961

Antitumor Agents. 185. Synthesis and Biological Evaluation of Tridemethylthiocolchicine Analogues as Novel Topoisomerase II Inhibitors Jian Guan, Xiao-Kang Zhu, Yoko Tachibana, Kenneth F. Bastow, Arnold Brossi, Ernest Hamel, and Kuo-Hsiung Lee [Full Article - PDF]

1962-1969

Chemistry and Pharmacology of the Piperidine-Based Analogues of Cocaine. Identification of Potent DAT Inhibitors Lacking the Tropane Skeleton Alan P. Kozikowski, Gian Luca Araldi, John Boja, William M. Meil, Kenneth M. Johnson, Judith L. Flippen-Anderson, Clifford George, and Eddine Saiah [Full Article - PDF]

1970-1979

(±)-trans-2-[3-Methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a Potent Dual 5-Lipoxygenase Inhibitor and Platelet-Activating Factor Receptor Antagonist Xiong Cai, Ralph T. Scannell, David Yaeger, Md. Sajjat Hussoin, David B. Killian, Changgeng Qian, Joseph Eckman, San-Bao Hwang, Lynn Libertine-Garahan, C. Grace Yeh, Stephen H. Ip, and T. Y. Shen [Full Article - PDF]

1980-1990

Investigation of the N-Substituent Conformation Governing Potency and Receptor Subtype-Selectivity in (+)-(3R,4R)-Dimethyl-4-(3-hydroxyphenyl)- piperidine Opioid Antagonists James B. Thomas, S. Wayne Mascarella, Richard B. Rothman, John S. Partilla, Heng Xu, Karen B. McCullough, Christina M. Dersch, Buddy E. Cantrell, Dennis M. Zimmerman, and F. Ivy Carroll [Full Article - PDF]

BOOK REVIEWS

1991-1991

Structure-Based Drug Design Edited by Pandi Veerapandian. Marcel Dekker, Inc., New York. 1997. xiii + 647 pp. 16 × 23.5 cm. ISBN 0-8247-9869-4. $175.00. James F. Kerwin, Jr. [Full Article - PDF]

1991-1992

Asymmetric Synthesis By Gary Proctor. Oxford University Press, Oxford, UK. 1997. 237 pp. 16 × 24 cm. ISBN 0-19-855726-3. $85.00. Thomas J. Caggiano [Full Article - PDF]

1992-1992

Monosaccharide Sugars By Zoltán Györgydeák and István F. Pelyvás. Academic Press, San Diego, CA. 1998. xviii-508 pp. 15.5 × 23.5 cm. ISBN 0-12-550360-1. $89.95. Hélène G. Bazin and Robert J. Linhardt [Full Article - PDF]

1992-1994

Reviews in Computational Chemistry, Volume 11 Edited by Kenney B. Lipkowitz and Donald B. Boyd. Wiley-VCH, Inc., New York, NY. 1997. xxiv + 431 pp. 16 x 24 cm. ISBN 0-471-19248-1. $120.00. Emile M. Bellott [Full Article - PDF]

1994-1995

From Chemical Topology to Three Dimensional Geometry Edited by Alexandru T. Balaban. Plenum Press, New York, NY. 1997. xviii + 420 pp. 16 × 23 cm. ISBN 0-30645462. $125.00. Emile M. Bellott [Full Article - PDF]

1995-1995

Books of Interest [Full Article - PDF]

ADDITIONS AND CORRECTIONS

1996-1996

Synthesis of Gonadotropin-Releasing Hormone III Analogs. Structure-Antitumor Activity Relationships Imre Mezö, Sándor Lovas, István Pályi, Borbála Vincze, Adrien Kálnay, Gizella Turi, Zsolt Vadász, János Seprödi, Miklós Idei,Géza Tóth, Eva Gulyás, Ferenc Ötvös, Mariann Mák, Judit E. Horváth, István Teplán, and Richard F. Murphy [Full Article - PDF]