Table of Contents
February 26, 2004
Volume 47, Issue 5
Pages 1075-1301
About the Cover: Molecular modeling of overlayed trisubstituted acridine derivatives (mauve and green) complexed with G-quadruplex DNA (Harrison, R. J.; et al. J. Med. Chem. 2003, 46, 4463-4476).
Letters
New Class of Corticotropin-Releasing Factor (CRF) Antagonists: Small Peptides Having High Binding Affinity for CRF Receptor
Yasuki Yamada, Kenji Mizutani, Yasuhiro Mizusawa, Yoshiji Hantani, Makoto Tanaka, Yuko Tanaka, Masaki Tomimoto, Makoto Sugawara, Norio Imai, Hideki Yamada, Nobuyuki Okajima, and Jun-ichi Haruta
pp 1075–1078Publication Date (Web): February 03, 2004 (Letter)
DOI: 10.1021/jm034180+
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Hi-Res PDFSabadinine: A Potential Non-Peptide Anti-Severe Acute-Respiratory-Syndrome Agent Identified Using Structure-Aided Design
Jeffrey H. Toney, Sonia Navas-Martín, Susan R. Weiss, and Andreas Koeller
pp 1079–1080Publication Date (Web): January 24, 2004 (Letter)
DOI: 10.1021/jm034137m
Small Molecule Mitochondrial F1F0 ATPase Hydrolase Inhibitors as Cardioprotective Agents. Identification of 4-(N-Arylimidazole)-Substituted Benzopyran Derivatives as Selective Hydrolase Inhibitors
Karnail S. Atwal, Paulina Wang, W. Lynn Rogers, Paul Sleph, Hossain Monshizadegan, Francis N. Ferrara, Sarah Traeger, David W. Green, and Gary J. Grover
pp 1081–1084Publication Date (Web): January 29, 2004 (Letter)
DOI: 10.1021/jm030291x
Articles
Nonpeptide Luteinizing Hormone-Releasing Hormone Antagonists Derived from Erythromycin A: Design, Synthesis, and Biological Activity of Cladinose Replacement Analogues
John T. Randolph, Philip Waid, Charles Nichols, Daryl Sauer, Fortuna Haviv, Gilbert Diaz, Gary Bammert, Leslie M. Besecke, Jason A. Segreti, Kurt M. Mohning, Eugene N. Bush, Craig D. Wegner, and Jonathan Greer
pp 1085–1097Publication Date (Web): February 04, 2004 (Article)
DOI: 10.1021/jm030418i
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a New Class of Synthetic Histone Deacetylase Inhibitors. 2. Effect of Pyrrole-C2 and/or -C4 Substitutions on Biological Activity
Antonello Mai, Silvio Massa, Ilaria Cerbara, Sergio Valente, Rino Ragno, Patrizia Bottoni, Roberto Scatena, Peter Loidl, and Gerald Brosch
pp 1098–1109Publication Date (Web): January 21, 2004 (Article)
DOI: 10.1021/jm030990+
Synthesis and Chemical−Pharmacological Characterization of the Antimetastatic NAMI-A-Type Ru(III) Complexes (Hdmtp)[trans-RuCl4(dmso-S)(dmtp)], (Na)[trans-RuCl4(dmso-S)(dmtp)], and [mer-RuCl3(H2O)(dmso-S)(dmtp)] (dmtp = 5,7-Dimethyl[1,2,4]triazolo[1,5-a]pyrimidine)
Aldrik H. Velders, Alberta Bergamo, Enzo Alessio, Ennio Zangrando, Jaap G. Haasnoot, Claudia Casarsa, Moreno Cocchietto, Sonia Zorzet, and Gianni Sava
pp 1110–1121Publication Date (Web): January 21, 2004 (Article)
DOI: 10.1021/jm030984d
Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Iodine-123 Labeled 2β-Carbomethoxy-3β-[4‘-((Z)-2-haloethenyl)phenyl]tropanes: Candidate Radioligands for in Vivo Imaging of the Serotonin Transporter
Christophe Plisson, Jonathan McConathy, Laurent Martarello, Eugene. J. Malveaux, Vernon M. Camp, Larry Williams, John R. Votaw, and Mark M. Goodman
pp 1122–1135Publication Date (Web): February 03, 2004 (Article)
DOI: 10.1021/jm030384e
Benzo[f]azino[2,1-a]phthalazinium Cations: Novel DNA Intercalating Chromophores with Antiproliferative Activity
Valentín Martínez, Carolina Burgos, Julio Alvarez-Builla, Gerónimo Fernández, Alberto Domingo, Raquel García-Nieto, Federico Gago, Ignacio Manzanares, Carmen Cuevas, and Juan J. Vaquero
pp 1136–1148Publication Date (Web): January 24, 2004 (Article)
DOI: 10.1021/jm0310434
Antineoplastic Agents. 520. Isolation and Structure of Irciniastatins A and B from the Indo-Pacific Marine Sponge Ircinia ramosa1
George R. Pettit, Jun-Ping Xu, Jean-Charles Chapuis, Robin K. Pettit, Larry P. Tackett, Dennis L. Doubek, John N. A. Hooper, and Jean M. Schmidt
pp 1149–1152Publication Date (Web): January 30, 2004 (Article)
DOI: 10.1021/jm030207d
Structure−Activity Studies of Orexin A and Orexin B at the Human Orexin 1 and Orexin 2 Receptors Led to Orexin 2 Receptor Selective and Orexin 1 Receptor Preferring Ligands
Manja Lang, Richard M. Söll, Franz Dürrenberger, Frank M. Dautzenberg, and Annette G. Beck-Sickinger
pp 1153–1160Publication Date (Web): January 24, 2004 (Article)
DOI: 10.1021/jm030982t
Linker Length Modulates DNA Cross-Linking Reactivity and Cytotoxic Potency of C8/C8‘ Ether-Linked C2-exo-Unsaturated Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) Dimers
Stephen J. Gregson, Philip W. Howard, Darren R. Gullick, Anzu Hamaguchi, Kathryn E. Corcoran, Natalie A. Brooks, John A. Hartley, Terence C. Jenkins, Sejal Patel, Matthew J. Guille, and David E. Thurston
pp 1161–1174Publication Date (Web): January 30, 2004 (Article)
DOI: 10.1021/jm030897l
Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1
Joseph H. Chan, George A. Freeman, Jeffrey H. Tidwell, Karen R. Romines, Lee T. Schaller, Jill R. Cowan, Steve S. Gonzales, Gina S. Lowell, C. W. Andrews III, David J. Reynolds, Marty St Clair, Richard J. Hazen, Rob G. Ferris, Katrina L. Creech, Grace B. Roberts, Steven A. Short, Kurt Weaver, George W. Koszalka, and Lawrence R. Boone
pp 1175–1182Publication Date (Web): January 30, 2004 (Article)
DOI: 10.1021/jm030255y
Potent Nonclassical Nucleoside Antiviral Drugs Based on the N,N-Diarylformamidine Concept
Carole Anastasi, Olivier Hantz, Erik De Clercq, Christophe Pannecouque, Pascal Clayette, Nathalie Dereuddre-Bosquet, Dominique Dormont, Françoise Gondois-Rey, Ivan Hirsch, and Jean-Louis Kraus
pp 1183–1192Publication Date (Web): January 24, 2004 (Article)
DOI: 10.1021/jm0309708
Design, Synthesis, and Biological Evaluation of Doxorubicin−Formaldehyde Conjugates Targeted to Breast Cancer Cells
Patrick J. Burke and Tad H. Koch
pp 1193–1206Publication Date (Web): January 24, 2004 (Article)
DOI: 10.1021/jm030352r
Synthesis of 2‘,5‘-Dideoxy-2-fluoroadenosine and 2‘,5‘-Dideoxy-2,5‘-difluoroadenosine: Potent P-Site Inhibitors of Adenylyl Cyclase
Song Ye, Martha M. Rezende, Wei-Ping Deng, Brian Herbert, John W. Daly, Roger A. Johnson, and Kenneth L. Kirk
pp 1207–1213Publication Date (Web): January 29, 2004 (Article)
DOI: 10.1021/jm0303599
Synthesis and Biological Evaluation of New Selective Cytotoxic Cyclolignans Derived from Podophyllotoxin
María Angeles Castro, Jose María Miguel del Corral, Marina Gordaliza, Pablo A. García, María Antonia Gómez-Zurita, María Dolores García-Grávalos, Janis de la Iglesia-Vicente, Consuelo Gajate, Feiyun An, Faustino Mollinedo, and Arturo San Feliciano
pp 1214–1222Publication Date (Web): January 30, 2004 (Article)
DOI: 10.1021/jm030978h
Structure−Activity Relationships of Small Phosphopeptides, Inhibitors of Grb2 SH2 Domain, and Their Prodrugs
Wang-Qing Liu, Michel Vidal, Catherine Olszowy, Emmanuelle Million, Christine Lenoir, Hélène Dhôtel, and Christiane Garbay
pp 1223–1233Publication Date (Web): February 03, 2004 (Article)
DOI: 10.1021/jm031005k
Chemical and Functional Identification and Characterization of Novel Sulfated α-Conotoxins from the Cone Snail Conus anemone
Marion L. Loughnan, Annette Nicke, Alun Jones, David J. Adams, Paul F. Alewood, and Richard J. Lewis
pp 1234–1241Publication Date (Web): January 29, 2004 (Article)
DOI: 10.1021/jm031010o
Prediction of Human Volume of Distribution Values for Neutral and Basic Drugs. 2. Extended Data Set and Leave-Class-Out Statistics
Franco Lombardo, R. Scott Obach, Marina Y. Shalaeva, and Feng Gao
pp 1242–1250Publication Date (Web): February 03, 2004 (Article)
DOI: 10.1021/jm030408h
Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin
Benjamin P. Ross, Shaun E. DeCruz, Thomas B. Lynch, Karen Davis-Goff, and Istvan Toth
pp 1251–1258Publication Date (Web): January 15, 2004 (Article)
DOI: 10.1021/jm030474j
Synthesis and Structure−Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists
Zhiqiang Guo, Yun-Fei Zhu, Timothy D. Gross, Fabio C. Tucci, Yinghong Gao, Manisha Moorjani, Patrick J. Connors, Jr., Martin W. Rowbottom, Yongsheng Chen, R. Scott Struthers, Qiu Xie, John Saunders, Greg Reinhart, Ta Kung Chen, Anne L. Killam Bonneville, and Chen Chen
pp 1259–1271Publication Date (Web): February 04, 2004 (Article)
DOI: 10.1021/jm030472z
Carbonic Anhydrase Inhibitors. Inhibition of Mitochondrial Isozyme V with Aromatic and Heterocyclic Sulfonamides
Daniela Vullo, Marco Franchi, Enzo Gallori, Jochen Antel, Andrea Scozzafava, and Claudiu T. Supuran
pp 1272–1279Publication Date (Web): January 29, 2004 (Article)
DOI: 10.1021/jm031057+
Synthesis, Characterization, and Preliminary in Vivo Tests of New Poly(ethylene glycol) Conjugates of the Antitumor Agent 10-Amino-7-ethylcamptothecin
Andrea Guiotto, Mirta Canevari, Piero Orsolini, Olivier Lavanchy, Christine Deuschel, Norimasa Kaneda, Akinobu Kurita, Takeshi Matsuzaki, Takeshi Yaegashi, Seigo Sawada, and Francesco M. Veronese
pp 1280–1289Publication Date (Web): January 17, 2004 (Article)
DOI: 10.1021/jm031072e
Antimalarial and Antitumor Evaluation of Novel C-10 Non-Acetal Dimers of 10β-(2-Hydroxyethyl)deoxoartemisinin
J. Prince Jeyadevan, Patrick G. Bray, James Chadwick, Amy E. Mercer, Aoife Byrne, Stephen A. Ward, B. Kevin Park, Dominic P. Williams, Rick Cosstick, Jill Davies, Adrian P. Higson, Ed Irving, Gary H. Posner, and Paul M. O'Neill
pp 1290–1298Publication Date (Web): January 31, 2004 (Article)
DOI: 10.1021/jm030974c
Brief Articles
Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents
Gary H. Posner, Andrew J. McRiner, Ik-Hyeon Paik, Surojit Sur, Kristina Borstnik, Suji Xie, Theresa A. Shapiro, Adebusola Alagbala, and Barbara Foster
pp 1299–1301Publication Date (Web): January 31, 2004 (Brief Article)
DOI: 10.1021/jm0303711