Journal of Medicinal Chemistry
Volume 43, Issue 12 (June 15, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

2293-2296

Structure-Based Design and Synthesis of a Potent Matrix Metalloproteinase-13 Inhibitor Based on a Pyrrolidinone Scaffold Ralph P. Robinson, Ellen R. Laird, James F. Blake, Jon Bordner, Kathleen M. Donahue, Lori L. Lopresti-Morrow, Peter G. Mitchell, Matthew R. Reese, Lisa M. Reeves, Ethan J. Stam, and Sue A. Yocum [Full Article - PDF]

2297-2299

Fenchylamine Sulfonamide Inhibitors of Amyloid Peptide Production by the -Secretase Proteolytic Pathway: Potential Small-Molecule Therapeutic Agents for the Treatment of Alzheimer's Disease Gilbert M. Rishton, Daniel M. Retz, Paul A. Tempest, James Novotny, Steve Kahn, James J. S. Treanor, Jack D. Lile, and Martin Citron [Full Article - PDF]

ARTICLES

2300-2309

A 3D-QSAR Study on the Structural Requirements for Binding to CB1 and CB2 Cannabinoid Receptors Maria Fichera, Gabriele Cruciani, Alfredo Bianchi, and Giuseppe Musumarra [Full Article - PDF]

2310-2323

New Anilinophthalazines as Potent and Orally Well Absorbed Inhibitors of the VEGF Receptor Tyrosine Kinases Useful as Antagonists of Tumor-Driven Angiogenesis Guido Bold, Karl-Heinz Altmann, Jörg Frei, Marc Lang, Paul W. Manley, Peter Traxler, Bernhard Wietfeld, Josef Brüggen, Elisabeth Buchdunger, Robert Cozens, Stefano Ferrari, Pascal Furet, Francesco Hofmann, Georg Martiny-Baron, Jürgen Mestan, Johannes Rösel, Matthew Sills, David Stover, Figan Acemoglu, Eugen Boss, René Emmenegger, Laurent Lässer, Elvira Masso, Rosemarie Roth, Christian Schlachter, Werner Vetterli, Dominique Wyss, and Jeanette M. Wood [Full Article - PDF]

2324-2331

Hydroxamic Acid Derivatives as Potent Peptide Deformylase Inhibitors and Antibacterial Agents Christian Apfel, David W. Banner, Daniel Bur, Michel Dietz, Takahiro Hirata, Christian Hubschwerlen, Hans Locher, Malcolm G. P. Page, Wolfgang Pirson, Gérard Rossé, and Jean-Luc Specklin [Full Article - PDF]

2332-2349

17-O-Aminoalkyloximes of 5-Androstane-3,14-diol with Digitalis-like Activity: Synthesis, Cardiotonic Activity, Structure-Activity Relationships, and Molecular Modeling of the Na+,K+-ATPase Receptor Alberto Cerri, Nicoletta Almirante, Paolo Barassi, Alessandra Benicchio, Giorgio Fedrizzi, Patrizia Ferrari, Rosella Micheletti, Luisa Quadri, Enzio Ragg, Roberto Rossi, Marco Santagostino, Antonio Schiavone, Fulvio Serra, Maria Pia Zappavigna, and Piero Melloni [Full Article - PDF]

2350-2355

CCK Peptides with Combined Features of Hexa- and Tetrapeptide CCK-A Agonists M. Edward Pierson, Jeanne M. Comstock, Roy D. Simmons, Ronald Julien, Frederick Kaiser, and James D. Rosamond [Full Article - PDF]

2356-2361

Synthesis and Biological Evaluation of Bombesin Constrained Analogues Michèle Cristau, Chantal Devin, Catherine Oiry, Olivier Chaloin, Muriel Amblard, Nicole Bernad, Annie Heitz, Jean-Alain Fehrentz, and Jean Martinez [Full Article - PDF]

2362-2370

Design, Synthesis, and Structure-Activity Relationships of Novel Non-Imidazole Histamine H3 Receptor Antagonists Ian D. Linney, Ildiko M. Buck, Elaine A. Harper, S. Barret Kalindjian, Michael J. Pether, Nigel P. Shankley, Gillian F. Watt, and Paul T. Wright [Full Article - PDF]

2371-2381

Indeno[1,2-b]pyrazin-2,3-diones: A New Class of Antagonists at the Glycine Site of the NMDA Receptor with Potent in Vivo Activity Patrick Jimonet, Yves Ribeill, Georg Andrees Bohme, Alain Boireau, Michel Chevé, Dominique Damour, Adam Doble, Arielle Genevois-Borella, Frédéric Herman, Assunta Imperato, Sylvain Le Guern, Franco Manfré, Jeremy Pratt, John C. R. Randle, Jean-Marie Stutzmann, and Serge Mignani [Full Article - PDF]

2382-2386

Synthesis and Biological Evaluation of Bradykinin B1/B2 and Selective B1 Receptor Antagonists Muriel Amblard, Philippe Bedos, Christophe Olivier, Isabelle Daffix, Jean-Michel Luccarini, Pierre Dodey, Didier Pruneau, Jean-Luc Paquet, and Jean Martinez [Full Article - PDF]

2387-2394

A Rational Approach to the Design and Synthesis of a New Bradykinin B1 Receptor Antagonist Philippe Bedos, Muriel Amblard, Gilles Subra, Pierre Dodey, Jean-Michel Luccarini, Jean-Luc Paquet, Didier Pruneau, André Aumelas, and Jean Martinez [Full Article - PDF]

2395-2402

Synthesis and Cytotoxic and Antitumor Activity of Benzo[b]pyrano[3,2-h]acridin-7-one Analogues of Acronycine Nadine Costes, Hervé Le Deit, Sylvie Michel, François Tillequin, Michel Koch, Bruno Pfeiffer, Pierre Renard, Stéphane Léonce, Nicolas Guilbaud, Laurence Kraus-Berthier, Alain Pierré, and Ghanem Atassi [Full Article - PDF]

2403-2410

Water-Soluble, Core-Modified Porphyrins as Novel, Longer-Wavelength-Absorbing Sensitizers for Photodynamic Therapy Corey E. Stilts, Marina I. Nelen, David G. Hilmey, Sherry R. Davies, Sandra O. Gollnick, Allan R. Oseroff, Scott L. Gibson, Russell Hilf, and Michael R. Detty [Full Article - PDF]

2411-2418

X-ray Structure of Cytotoxic trans-[PtCl2(dimethylamine)(isopropylamine)]: Interstrand Cross-Link Efficiency, DNA Sequence Specificity, and Inhibition of the B-Z Transition José M. Pérez, Eva I. Montero, Ana M. González, Xavier Solans, Mercé Font-Bardia, Miguel A. Fuertes, Carlos Alonso, and Carmen Navarro-Ranninger [Full Article - PDF]

2419-2429

Synthesis of B-Ring Homologated Estradiol Analogues that Modulate Tubulin Polymerization and Microtubule Stability Zhiqiang Wang, Donglai Yang, Arasambattu K. Mohanakrishnan, Phillip E. Fanwick, Priya Nampoothiri, Ernest Hamel, and Mark Cushman [Full Article - PDF]

2430-2437

Design, Synthesis, and Biological Evaluation of Tricyclic Nucleosides (Dimensional Probes) as Analogues of Certain Antiviral Polyhalogenated Benzimidazole Ribonucleosides Zhijian Zhu, Blaise Lippa, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

2438-2448

Deoxy Sugar Analogues of Triciribine: Correlation of Antiviral and Antiproliferative Activity with Intracellular Phosphorylation Anthony R. Porcari, Roger G. Ptak, Katherine Z. Borysko, Julie M. Breitenbach, Sauro Vittori, Linda L. Wotring, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

2449-2456

Synthesis and Antiviral Evaluation of Trisubstituted Indole N-Nucleosides as Analogues of 2,5,6-Trichloro-1-(-D-ribofuranosyl)benzimidazole (TCRB) Jiong J. Chen, Yuan Wei, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

2457-2463

6-N-Acyltriciribine Analogues: Structure-Activity Relationship between Acyl Carbon Chain Length and Activity against HIV-1 Anthony R. Porcari, Roger G. Ptak, Katherine Z. Borysko, Julie M. Breitenbach, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

2464-2472

Synthesis and Antiviral Evaluation of Halogenated -D- and -L-Erythrofuranosylbenzimidazoles Kristjan S. Gudmundsson, Jeffrey Tidwell, Nicole Lippa, George W. Koszalka, Nanine van Draanen, Roger G. Ptak, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

BRIEF ARTICLES

2473-2478

Synthesis of Fluorosugar Analogues of 2,5,6-Trichloro-1-(-D-ribofuranosyl)benzimidazole as Antivirals with Potentially Increased Glycosidic Bond Stability Kristjan S. Gudmundsson, George A. Freeman, John C. Drach, and Leroy B. Townsend [Full Article - PDF]

2479-2483

A Potent Aldose Reductase Inhibitor, (2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): Its Absolute Configuration and Interactions with the Aldose Reductase by X-ray Crystallography Mitsuru Oka, Yukiharu Matsumoto, Shigeru Sugiyama, Nobuaki Tsuruta, and Masaaki Matsushima [Full Article - PDF]

2484-2487

Polyether Mimics of Naturally Occurring Cytotoxic Annonaceous Acetogenins Zhu-Jun Yao, Hai-Ping Wu, and Yu-Lin Wu [Full Article - PDF]

BOOK REVIEWS

2488-2488

Comprehensive Organic Transformations. A Guide to Functional Group Preparations By Richard A. Larock. Wiley-VCH Publishers, New York. 1999. xliii + 2583 pp. 18.5 × 26 cm. ISBN 0-471-19031-4. $150.00. Jan W. F. Wasley [Full Article - PDF]