Journal of Medicinal Chemistry
Volume 44, Issue 26 (December 20, 2001)
Copyright © 2001 American Chemical Society

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LETTERS

4497-4500

Synthesis and Biological Evaluation of Myoseverin Derivatives: Microtubule Assembly Inhibitors Young-Tae Chang, Sarah M. Wignall, Gustavo R. Rosania, Nathanael S. Gray, Sarah R. Hanson, Andrew I. Su, John Merlie, Jr., Ho-Sang Moon, Sameep B. Sangankar, Omar Perez, Rebecca Heald, and Peter G. Schultz [Full Article - PDF]

4501-4504

Characterization of the 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione Derivative (S)-CPW399 as a Novel, Potent, and Subtype-Selective AMPA Receptor Full Agonist with Partial Desensitization Properties Giuseppe Campiani, Elena Morelli, Vito Nacci, Caterina Fattorusso, Anna Ramunno, Ettore Novellino, Jeremy Greenwood, Tommy Liljefors, Roger Griffiths, Colin Sinclair, Helen Reavy, Anders S. Kristensen, Darryl S. Pickering, Arne Schousboe, Alfredo Cagnotto, Elena Fumagalli, and Tiziana Mennini [Full Article - PDF]

4505-4508

Design, Synthesis and Biological Evaluation of Novel Arachidonic Acid Derivatives as Highly Potent and Selective Endocannabinoid Transporter Inhibitors María L. López-Rodríguez, Alma Viso, Silvia Ortega-Gutiérrez, Isabel Lastres-Becker, Sara González, Javier Fernández-Ruiz, and José A. Ramos [Full Article - PDF]

ARTICLES

4509-4523

Quadruplex-Interactive Agents as Telomerase Inhibitors: Synthesis of Porphyrins and Structure-Activity Relationship for the Inhibition of Telomerase Dong-Fang Shi, Richard T. Wheelhouse, Daekyu Sun, and Laurence H. Hurley [Full Article - PDF]

4524-4534

Identification of Dipeptidyl Nitriles as Potent and Selective Inhibitors of Cathepsin B through Structure-Based Drug Design Paul D. Greenspan, Kirk L. Clark, Ruben A. Tommasi, Scott D. Cowen, Leslie W. McQuire, David L. Farley, John H. van Duzer, Ronald L. Goldberg, Huanghai Zhou, Zhengming Du, John J. Fitt, David E. Coppa, Zheng Fang, William Macchia, Lijuan Zhu, Michael P. Capparelli, Robert Goldstein, Andrew M. Wigg, John R. Doughty, Regine S. Bohacek, and Ania K. Knap [Full Article - PDF]

4535-4553

Synthetic 2-Aroylindole Derivatives as a New Class of Potent Tubulin-Inhibitory, Antimitotic Agents Siavosh Mahboobi, Herwig Pongratz, Harald Hufsky, Jörg Hockemeyer, Markus Frieser, Alexei Lyssenko, Dietrich H. Paper, Jutta Bürgermeister, Frank-D. Böhmer, Heinz-Herbert Fiebig, Angelika M. Burger, Silke Baasner, and Thomas Beckers [Full Article - PDF]

4554-4562

Synthesis, Biological Evaluation, and Pharmacophore Generation of Uracil, 4(3H)-Pyrimidinone, and Uridine Derivatives as Potent and Selective Inhibitors of Parainfluenza 1 (Sendai) Virus Raffaele Saladino, Claudia Crestini, Anna Teresa Palamara, Maria Chiara Danti, Fabrizio Manetti, Federico Corelli, E. Garaci, and Maurizio Botta [Full Article - PDF]

4563-4576

Design, Synthesis, and Biological Characterization of Bivalent 1-Methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole Derivatives as Selective Muscarinic Agonists W. G. Rajeswaran, Yang Cao, Xi-Ping Huang, Mary Elizabeth Wroblewski, Tracy Colclough, Selina Lee, Fenghua Liu, Peter I. Nagy, James Ellis, Beth A. Levine, Karl H. Nocka, and William S. Messer, Jr. [Full Article - PDF]

4577-4583

Synthesis and Antitumor Activity of Novel C-7 Paclitaxel Ethers: Discovery of BMS-184476 Thomas J. Altstadt, Craig R. Fairchild, Jerzy Golik, Kathy A. Johnston, John F. Kadow, Francis Y. Lee, Byron H. Long, William C. Rose, Dolatrai M. Vyas, Henry Wong, Mu-Jen Wu, and Mark D. Wittman [Full Article - PDF]

4584-4594

Structure of Protein Tyrosine Phosphatase 1B in Complex with Inhibitors Bearing Two Phosphotyrosine Mimetics Zongchao Jia, Qilu Ye, A. Nicole Dinaut, Qingping Wang, Deena Waddleton, Paul Payette, Chidambaram Ramachandran, Brian Kennedy, Gabriel Hum, and Scott D. Taylor [Full Article - PDF]

4595-4614

Dimerization of G-Protein-Coupled Receptors Mark K. Dean, Christopher Higgs, Richard E. Smith, Robert P. Bywater, Christopher R. Snell, Paul D. Scott, Graham J. G. Upton, Trevor J. Howe, and Christopher A. Reynolds [Full Article - PDF]

4615-4627

Structure-Based Generation of a New Class of Potent Cdk4 Inhibitors: New de Novo Design Strategy and Library Design Teruki Honma, Kyoko Hayashi, Tetsuya Aoyama, Noriaki Hashimoto, Takumitsu Machida, Kazuhiro Fukasawa, Toshiharu Iwama, Chinatsu Ikeura, Mari Ikuta, Ikuko Suzuki-Takahashi, Yoshikazu Iwasawa, Takashi Hayama, Susumu Nishimura, and Hajime Morishima [Full Article - PDF]

4628-4640

A Novel Approach for the Development of Selective Cdk4 Inhibitors: Library Design Based on Locations of Cdk4 Specific Amino Acid Residues Teruki Honma, Takashi Yoshizumi, Noriaki Hashimoto, Kyoko Hayashi, Nobuhiko Kawanishi, Kazuhiro Fukasawa, Tohru Takaki, Chinatsu Ikeura, Mari Ikuta, Ikuko Suzuki-Takahashi, Takashi Hayama, Susumu Nishimura, and Hajime Morishima [Full Article - PDF]

4641-4649

Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues Teruhisa Tokunaga, W. Ewan Hume, Takashi Umezome, Kazuhiko Okazaki, Yasuyuki Ueki, Kazuo Kumagai, Shinji Hourai, Jun Nagamine, Hitoshi Seki, Mutsuo Taiji, Hiroshi Noguchi, and Ryu Nagata [Full Article - PDF]

4650-4660

Structural Basis for the Binding Affinity of Xanthines with the DNA Intercalator Acridine Orange Mark B. Lyles, Ivan L. Cameron, and H. Ralph Rawls [Full Article - PDF]

4661-4667

Mononuclear Platinum(II) Complex with 2-Phenylpyridine Ligands Showing High Cytotoxicity against Mouse Sarcoma 180 Cells Acquiring High Cisplatin Resistance Tomoko Okada, Ibrahim M. El-Mehasseb, Masato Kodaka, Takenori Tomohiro, Ken-ichi Okamoto, and Hiroaki Okuno [Full Article - PDF]

4668-4676

Chemosensitization of a Multidrug-Resistant Leishmania tropica Line by New Sesquiterpenes from Maytenus magellanica and Maytenus chubutensis María L. Kennedy, Fernando Cortés-Selva, José M. Pérez-Victoria, Ignacio A. Jiménez, Antonio G. González, Orlando M. Muñoz, Francisco Gamarro, Santiago Castanys, and Angel G. Ravelo [Full Article - PDF]

4677-4687

Diaminoindanes as Microsomal Triglyceride Transfer Protein Inhibitors Gary M. Ksander, Reynalda deJesus, Andrew Yuan, Cynthia Fink, Michael Moskal, Eric Carlson, Paivi Kukkola, Natalie Bilci, Eli Wallace, Alan Neubert, David Feldman, Therese Mogelesky, Kevin Poirier, Michael Jeune, Ronald Steele, Jong Wasvery, Zouhair Stephan, Edna Cahill, Randy Webb, Aida Navarrete, Warren Lee, Joyce Gibson, Natalya Alexander, Haamid Sharif, and Ashok Hospattankar [Full Article - PDF]

4688-4695

C-16 Artemisinin Derivatives and Their Antimalarial and Cytotoxic Activities: Syntheses of Artemisinin Monomers, Dimers, Trimers, and Tetramers by Nucleophilic Additions to Artemisitene Sanchai Ekthawatchai, Sumalee Kamchonwongpaisan, Palangpon Kongsaeree, Bongkoch Tarnchompoo, Yodhathai Thebtaranonth, and Yongyuth Yuthavong [Full Article - PDF]

4696-4703

Design, Synthesis, and Pharmacological Evaluation of Thapsigargin Analogues for Targeting Apoptosis to Prostatic Cancer Cells Carsten M. Jakobsen, Samuel R. Denmeade, John T. Isaacs, Alyssa Gady, Carl E. Olsen, and Sren Brgger Christensen [Full Article - PDF]

4704-4715

2-(2-Piperidyl)- and 2-(2-Pyrrolidyl)chromans as Nicotine Agonists: Synthesis and Preliminary Pharmacological Characterization Simon M. N. Efange, Zhude Tu, Krystyna von Hohenberg, Lynn Francesconi, Robertha C. Howell, Marilyn V. Rampersad, Louis J. Todaro, Roger L. Papke, and Mei-Ping Kung [Full Article - PDF]

4716-4732

Dopamine D3 Receptor Antagonists. 1. Synthesis and Structure-Activity Relationships of 5,6-Dimethoxy-N-alkyl- and N-Alkylaryl-Substituted 2-Aminoindans Susanne R. Haadsma-Svensson, Kerry A. Cleek, Dac M. Dinh, J. Neil Duncan, Christopher L. Haber, Rita M. Huff, Mary E. Lajiness, Nanette F. Nichols, Martin W. Smith, Kjell A. Svensson, Matt J. Zaya, Arvid Carlsson, and Chiu-Hong Lin [Full Article - PDF]

BRIEF ARTICLES

4733-4736

Synthesis, in Vitro Pharmacology, and Molecular Modeling of syn-Huprines as Acetylcholinesterase Inhibitors Pelayo Camps, Elena Gómez, Diego Muñoz-Torrero, Albert Badia, Nuria María Vivas, Xavier Barril, Modesto Orozco, and Francisco Javier Luque [Full Article - PDF]

4737-4740

Design and Synthesis of Non-peptidic Inhibitors for the Syk C-Terminal SH2 Domain Based on Structure-Based In-Silico Screening Tatsuya Niimi, Masaya Orita, Miwa Okazawa-Igarashi, Hitoshi Sakashita, Kazumi Kikuchi, Evelyn Ball, Atsushi Ichikawa, Yoko Yamagiwa, Shuichi Sakamoto, Akihiro Tanaka, Shinichi Tsukamoto, and Shigeo Fujita , Kuniaki Tatsuta, Yasuhide Maeda, and Ken Chikauchi [Full Article - PDF]

BOOK REVIEWS

4741-4741

Principles and Applications of Asymmetric Synthesis By Guo-Qiang Lin, Yue-Ming Li, and Albert S. C. Chan. Wiley Interscience, New York. 2001. xvii + 515 pp. 16 × 24 cm. ISBN 0-471-40027-0. $89.95. Jeffrey Aubé [Full Article - PDF]

4741-4742

Synthesis and Applications of Isotopically Labelled Compounds. Volume 7. Proceedings of the Seventh International Symposium, Dresden, Germany, June 18-22, 2000 Edited by U. Pleiss and R. Voges. Wiley, New York. 2001. xxv + 702 pp. 17 × 25 cm. ISBN 0-471-49501-8. $220.00. Crist N. Filer [Full Article - PDF]