Journal of Medicinal Chemistry
Volume 41, Issue 24 (November 19, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

4677-4680

Novel CDC25A Phosphatase Inhibitors from Pyrolysis of 3--Azido-B-homo-6-oxa-4-cholesten-7-one on Silica Gel Hairuo Peng and Leon H. Zalkow , Robert T. Abraham , Garth Powis [Full Article - PDF]

EXPEDITED ARTICLES

4681-4685

Syntheses of New Isodethiaazacephems as Potent Antibacterial Agents Jih Ru Hwu, Shwu-Chen Tsay, and Shahram Hakimelahi [Full Article - PDF]

ARTICLES

4686-4692

Synthesis and Evaluation of 11-Substituted 21-Chloro/Iodo-(17,20E/Z)-19-norpregna-1,3,5(10),20-tetraene-3,17-diols: High-Affinity Ligands for the Estrogen Receptor Robert N. Hanson, Elio Napolitano, and Rita Fiaschi [Full Article - PDF]

4693-4705

Nonpeptide Somatostatin Agonists with sst4 Selectivity: Synthesis and Structure-Activity Relationships of Thioureas Shenquan Liu, Cheng Tang, Bin Ho, Michael Ankersen, Carsten E. Stidsen, and A. Michael Crider [Full Article - PDF]

4706-4715

Synthesis, Activity, and Molecular Modeling of New 2,4-Dioxo-5-(naphthylmethylene)-3-thiazolidineacetic Acids and 2-Thioxo Analogues as Potent Aldose Reductase Inhibitors Patrick Fresneau, Max Cussac, Jean-Marc Morand, Barbara Szymonski, Duc Tranqui, and Gérard Leclerc [Full Article - PDF]

4716-4722

Synthesis and Cytotoxicity of 2-Methyl-4,9-dihydro-1-substituted-1H-imidazo[4,5-g]quinoxaline-4,9-diones and 2,3-Disubstituted-5,10-pyrazino[2,3-g]quinoxalinediones Hee-Won Yoo, Myung-Eun Suh, and Sang Woo Park [Full Article - PDF]

4723-4732

Conformationally Restricted Analogues of 1N,12N-Bisethylspermine: Synthesis and Growth Inhibitory Effects on Human Tumor Cell Lines Venodhar K. Reddy, Aldonia Valasinas, Aparajita Sarkar, Hirak S. Basu, Laurence J. Marton, and Benjamin Frydman [Full Article - PDF]

4733-4743

Synthesis of 7-Benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and Novel Derivatives Free of Positional Isomers. Potent Inhibitors of cAMP-Specific Phosphodiesterase and of Malignant Tumor Cell Growth Karl-Heinz Merz, Doris Marko, Thomas Regiert, Guido Reiss, Walter Frank, and Gerhard Eisenbrand [Full Article - PDF]

4744-4754

DNA-Directed Alkylating Agents. 7. Synthesis, DNA Interaction, and Antitumor Activity of Bis(hydroxymethyl)- and Bis(carbamate)-Substituted Pyrrolizines and Imidazoles Graham J. Atwell, Jun-Yao Fan, Karin Tan, and William A. Denny [Full Article - PDF]

4755-4766

Indolequinone Antitumor Agents: Correlation between Quinone Structure, Rate of Metabolism by Recombinant Human NAD(P)H:Quinone Oxidoreductase, and in Vitro Cytotoxicity Howard D. Beall, Shannon Winski, Elizabeth Swann, Anna R. Hudnott, Ann S. Cotterill, Noeleen O'Sullivan, Stephen J. Green, Richard Bien, David Siegel, David Ross, and Christopher J. Moody [Full Article - PDF]

4767-4776

De Novo Design, Synthesis, and Biological Activities of High-Affinity and Selective Non-Peptide Agonists of the -Opioid Receptor Subo Liao, Josue Alfaro-Lopez, Mark D. Shenderovich, Keiko Hosohata, Jun Lin, Xiaoping Li, Dagmar Stropova, Peg Davis, Kevin A. Jernigan, Frank Porreca, Henry I. Yamamura, and Victor J. Hruby [Full Article - PDF]

4777-4789

Conformational Analysis and Automated Receptor Docking of Selective Arylacetamide-Based -Opioid Agonists Govindan Subramanian, M. Germana Paterlini, Dennis L. Larson, Philip S. Portoghese, and David M. Ferguson [Full Article - PDF]

4790-4799

Selective Tight Binding Inhibitors of Trypanosomal Glyceraldehyde-3-phosphate Dehydrogenase via Structure-Based Drug Design Alex M. Aronov, Christophe L. M. J. Verlinde, Wim G. J. Hol, and Michael H. Gelb [Full Article - PDF]

4800-4818

Covalent Modification of Cyclooxygenase-2 (COX-2) by 2-Acetoxyphenyl Alkyl Sulfides, a New Class of Selective COX-2 Inactivators Amit S. Kalgutkar, Kevin R. Kozak, Brenda C. Crews, G. Phillip Hochgesang, Jr., and Lawrence J. Marnett [Full Article - PDF]

4819-4832

Antileishmanial Chalcones: Statistical Design, Synthesis, and Three-Dimensional Quantitative Structure-Activity Relationship Analysis Simon Feldbæk Nielsen, Sren Brgger Christensen, Gabriele Cruciani, Arsalan Kharazmi, and Tommy Liljefors [Full Article - PDF]

4833-4843

Design and Synthesis of Hydrazinopeptides and Their Evaluation as Human Leukocyte Elastase Inhibitors Laure Guy, Joëlle Vidal, and André Collet , Augustin Amour and Michèle Reboud-Ravaux [Full Article - PDF]

4844-4853

Design, Synthesis, and Biological Activity of Prazosin-Related Antagonists. Role of the Piperazine and Furan Units of Prazosin on the Selectivity for 1-Adrenoreceptor Subtypes Maria L. Bolognesi, Roberta Budriesi, Alberto Chiarini, Elena Poggesi, Amedeo Leonardi, and Carlo Melchiorre [Full Article - PDF]

4854-4860

1,2-Benzisothiazol-3-one 1,1-Dioxide Inhibitors of Human Mast Cell Tryptase Keith D. Combrink, H. Belgin Gülgeze, Nicholas A. Meanwell, Bradley C. Pearce, Pi Zulan, Gregory S. Bisacchi, Daniel G. M. Roberts, Paul Stanley, and Steven M. Seiler [Full Article - PDF]

4861-4872

Exploration of Biologically Relevant Conformations of Anandamide, 2-Arachidonylglycerol, and Their Analogues Using Conformational Memories Judy Barnett-Norris, Frank Guarnieri, Dow P. Hurst, and Patricia H. Reggio [Full Article - PDF]

4873-4884

Human Telomerase Inhibition by Regioisomeric Disubstituted Amidoanthracene-9,10-diones Philip J. Perry, Anthony P. Reszka, Alexis A. Wood, Martin A. Read, Sharon M. Gowan, Harvinder S. Dosanjh, John O. Trent, Terence C. Jenkins, Lloyd R. Kelland, and Stephen Neidle [Full Article - PDF]

4885-4889

Synthesis and Biological Evaluation of 4-Chloro-3,5-dinitrobenzotrifluoride Analogues as Antileishmanial Agents Kevin K. Pitzer, Karl A. Werbovetz, James J. Brendle, and John P. Scovill [Full Article - PDF]

4890-4902

(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): A Very Potent Farnesyl Protein Transferase Inhibitor as a Novel Antitumor Agent F. George Njoroge, Arthur G. Taveras, Joseph Kelly, Stacy Remiszewski, Alan K. Mallams, Ronald Wolin, Adriano Afonso, Alan B. Cooper, Dinananth F. Rane, Yi-Tsung Liu, Jesse Wong, Bancha Vibulbhan, Patrick Pinto, Jeffrey Deskus, Carmen S. Alvarez, Joycelyn del Rosario, Michael Connolly, James Wang, Jagdish Desai, Randall R. Rossman, W. Robert Bishop, Robert Patton, Lynn Wang, Paul Kirschmeier, Mathew S. Bryant, Amin A. Nomeir, C.-C. Lin, Ming Liu, Andrew T. McPhail, Ronald J. Doll, Viyyoor M. Girijavallabhan, and Ashit K. Ganguly [Full Article - PDF]

NOTES

4903-4909

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: A Potent and Selective Dopamine D4 Ligand Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Marcello Leopoldo, and Vincenzo Tortorella [Full Article - PDF]

ADDITIONS AND CORRECTIONS

4910-4910

Cecil Chan, Hong Yin, Jacqui Garforth, James H. McKie, Rabih Jaouhari, Peter Speers, Kenneth T. Douglas, Peter J. Rock, Vanessa Yardley, Simon L. Croft, and Alan H. Fairlamb Phenothiazine Inhibitors of Trypanothione Reductase as Potential Antitrypanosomal and Antileishmanial Drugs [Full Article - PDF]