Journal of Medicinal Chemistry
Volume 43, Issue 7 (April 6, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

1251-1252

Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the -Opioid Receptor Does Not Affect Dynorphin A(1-13) Affinity and Function David M. Ferguson, Stacy Kramer, Thomas G. Metzger, Ping Y. Law, and Philip S. Portoghese [Full Article - PDF]

1253-1256

A Novel Macromolecular Prodrug Concept Exploiting Endogenous Serum Albumin as a Drug Carrier for Cancer Chemotherapy Felix Kratz, Ralph Müller-Driver, Inga Hofmann, Joachim Drevs, and Clemens Unger [Full Article - PDF]

EXPEDITED ARTICLES

1257-1263

N-3-Substituted Imidazoquinazolinones: Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile Dysfunction David P. Rotella, Zhong Sun, Yeheng Zhu, John Krupinski, Ronald Pongrac, Laurie Seliger, Diane Normandin, and John E. Macor [Full Article - PDF]

ARTICLES

1264-1270

Synthesis, Conformational Analysis, and Biological Activity of C-Thioribonucleosides Related to Tiazofurin Palmarisa Franchetti, Stefano Marchetti, Loredana Cappellacci, Hiremagalur N. Jayaram, Joel Aaron Yalowitz, Barry M. Goldstein, Jean-Louis Barascut, David Dukhan, Jean-Louis Imbach, and Mario Grifantini [Full Article - PDF]

1271-1281

Conformational Selection of Inhibitors and Substrates by Proteolytic Enzymes: Implications for Drug Design and Polypeptide Processing David P. Fairlie, Joel D. A. Tyndall, Robert C. Reid, Allan K. Wong, Giovanni Abbenante, Martin J. Scanlon, Darren R. March, Douglas A. Bergman, Christina L. L. Chai, and Brendan A. Burkett [Full Article - PDF]

1282-1292

Cyclin-Dependent Kinase Inhibition by New C-2 Alkynylated Purine Derivatives and Molecular Structure of a CDK2-Inhibitor Complex Michel Legraverend, Paul Tunnah, Martin Noble, Pierre Ducrot, Odile Ludwig, David S. Grierson, Maryse Leost, Laurent Meijer, and Jane Endicott [Full Article - PDF]

1293-1310

Novel Benzofuran and Benzothiophene Biphenyls as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic Properties Michael S. Malamas, Janet Sredy, Christopher Moxham, Alan Katz, Weixin Xu, Robert McDevitt, Folake O. Adebayo, Diane R. Sawicki, Laura Seestaller, Donald Sullivan, and Joseph R. Taylor [Full Article - PDF]

1311-1319

Synthesis and Anticonvulsant and Neurotoxic Properties of Substituted N-Phenyl Derivatives of the Phthalimide Pharmacophore Joseph Vamecq, Pierre Bac, Christine Herrenknecht, Pierre Maurois, Philippe Delcourt, and James P. Stables [Full Article - PDF]

1320-1328

Statistical Molecular Design of Building Blocks for Combinatorial Chemistry Anna Linusson, Johan Gottfries, Fredrik Lindgren, and Svante Wold [Full Article - PDF]

1329-1338

High-Affinity, Non-Peptide Agonists for the ORL1 (Orphanin FQ/Nociceptin) Receptor Stephan Röver, Geo Adam, Andrea M. Cesura, Guido Galley, François Jenck, Frederick J. Monsma, Jr., Jürgen Wichmann, and Frank M. Dautzenberg [Full Article - PDF]

1339-1349

Derivatives of (R)-1,11-Methyleneaporphine: Synthesis, Structure, and Interactions with G-Protein Coupled Receptors Tero Linnanen, Magnus Brisander, Lena Unelius, Göran Sundholm, Uli Hacksell, and Anette M. Johansson [Full Article - PDF]

1350-1358

Bis(phenazine-1-carboxamides): Structure-Activity Relationships for a New Class of Dual Topoisomerase I/II-Directed Anticancer Drugs Julie A. Spicer, Swarna A. Gamage, Gordon W. Rewcastle, Graeme J. Finlay, David J. A. Bridewell, Bruce C. Baguley, and William A. Denny [Full Article - PDF]

1359-1366

Deltorphin II Analogues with 6-Hydroxy-2-aminotetralin-2-carboxylic Acid in Position 1 Zsuzsanna Darula, Katalin E. Kövér, Krisztina Monory, Anna Borsodi, Éva Makó, András Rónai, Dirk Tourwé, Antal Péter, and Géza Tóth [Full Article - PDF]

1367-1379

Lipopolycationic Telomers for Gene Transfer: Synthesis and Evaluation of Their in Vitro Transfection Efficiency Géraldine Verderone, Nathalie Van Craynest, Otmane Boussif, Catherine Santaella, Rainer Bischoff, Hanno V. J. Kolbe, and Pierre Vierling [Full Article - PDF]

1380-1397

Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions Jeff B. Smaill, Gordon W. Rewcastle, Joseph A. Loo, Kenneth D. Greis, O. Helen Chan, Eric L. Reyner, Elke Lipka, H. D. Hollis Showalter, Patrick W. Vincent, William L. Elliott, and William A. Denny [Full Article - PDF]

1398-1408

Phosphinic Derivatives as New Dual Enkephalin-Degrading Enzyme Inhibitors: Synthesis, Biological Properties, and Antinociceptive Activities Huixiong Chen, Florence Noble, Aurélie Mothé, Hervé Meudal, Pascale Coric, Sophie Danascimento, Bernard P. Roques, Pascal George, and Marie-Claude Fournié-Zaluski [Full Article - PDF]

BRIEF ARTICLES

1409-1412

Synthesis and Oral Antitumor Activity of Tetrakis(carboxylato)platinum(IV) Complexes Young-A Lee, Sung Sil Lee, Kwan Mook Kim, Chong Ock Lee, and Youn Soo Sohn [Full Article - PDF]

1413-1417

Inhibition of Protein Kinase C by Dequalinium Analogues: Dependence on Linker Length and Geometry Donghui Qin, Regina Sullivan, William F. Berkowitz, Robert Bittman, and Susan A. Rotenberg [Full Article - PDF]

1418-1421

Protection against Oxidative Damage by Iron Chelators: Effect of Lipophilic Analogues and Prodrugs of N,N'-Bis(3,4,5-trimethoxybenzyl)ethylenediamine- N,N'-diacetic Acid (OR10141) Jean-Baptiste Galey, Odile Destrée, Jacqueline Dumats, Sylvie Génard, and Pierre Tachon [Full Article - PDF]

BOOK REVIEWS

1422-1422

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1422-1422

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ADDITIONS AND CORRECTIONS

1423-1426

2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the 2D Adrenergic Receptor Tina M. Ross, Michele C. Jetter, Mark E. McDonnell, Robert E. Boyd, Charlene D. Connelly, Rebecca P. Martinez, Martin A. Lewis, Ellen E. Codd, Robert B. Raffa, and Allen B. Reitz [Full Article - PDF]