Table of Contents
November 7, 2002
Volume 45, Issue 23
Pages 4947-5188
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
1-Benzyl-3-(5‘-hydroxymethyl-2‘-furyl)indazole (YC-1) Derivatives as Novel Inhibitors Against Sodium Nitroprusside-Induced Apoptosis
Jin-Cherng Lien, Fang-Yu Lee, Li-Jiau Huang, Shiow-Lin Pan, Jih-Hwa Guh, Che-Ming Teng, and Sheng-Chu Kuo
pp 4947–4949Publication Date (Web): October 08, 2002 (Letter)
DOI: 10.1021/jm020070b
Hi-Res PDFDiscovery of the First Nonpeptide Agonist of the GPR14/Urotensin-II Receptor: 3-(4-Chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954)
Glenn E. Croston, Roger Olsson, Erika A. Currier, Ethan S. Burstein, David Weiner, Norman Nash, Daniel Severance, Stig G. Allenmark, Linda Thunberg, Jian-Nong Ma, Nina Mohell, Brian O'Dowd, Mark R. Brann, and Uli Hacksell
pp 4950–4953Publication Date (Web): October 09, 2002 (Letter)
DOI: 10.1021/jm025551+
Full Text HTMLDiscovery of γ-Lactam Hydroxamic Acids as Selective Inhibitors of Tumor Necrosis Factor α Converting Enzyme: Design, Synthesis, and Structure−Activity Relationships
James J.-W. Duan, Lihua Chen, Zelda R. Wasserman, Zhonghui Lu, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, Karl D. Hardman, Ronald L. Magolda, Robert C. Newton, David D. Christ, Ruth R. Wexler, and Carl P. Decicco
pp 4954–4957Publication Date (Web): October 15, 2002 (Letter)
DOI: 10.1021/jm0255670
Aza-Peptide Epoxides: A New Class of Inhibitors Selective for Clan CD Cysteine Proteases
Juliana L. Asgian, Karen Ellis James, Zhao Zhao Li, Wendy Carter, Alan J. Barrett, Jowita Mikolajczyk, Guy S. Salvesen, and James C. Powers
pp 4958–4960Publication Date (Web): October 15, 2002 (Letter)
DOI: 10.1021/jm025581c
Expedited Articles
Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity: Design, Synthesis, and X-ray Cocrystal Structure
Stacie S. Canan Koch, Lars H. Thoresen, Jayashree G. Tikhe, Karen A. Maegley, Robert J. Almassy, Jianke Li, Xiao-Hong Yu, Scott E. Zook, Robert A. Kumpf, Cathy Zhang, Theodore J. Boritzki, Rena N. Mansour, Kanyin E. Zhang, Anne Ekker, Chris R. Calabrese, Nicola J. Curtin, Suzanne Kyle, Huw D. Thomas, Lan-Zhen Wang, A. Hilary Calvert, Bernard T. Golding, Roger J. Griffin, David R. Newell, Stephen E. Webber, and Zdenek Hostomsky
pp 4961–4974Publication Date (Web): October 15, 2002 (Expedited Article)
DOI: 10.1021/jm020259n
Articles
Novel Short Chain Chloroquine Analogues Retain Activity Against Chloroquine Resistant K1 Plasmodium falciparum
Paul A. Stocks, Kaylene J. Raynes, Patrick G. Bray, B. Kevin Park, Paul. M. O'Neill, and Stephen A. Ward
pp 4975–4983Publication Date (Web): October 03, 2002 (Article)
DOI: 10.1021/jm0108707
Synthesis, Solution Structure, and Biological Evaluation of Urokinase Type Plasminogen Activator (uPA)-Derived Receptor Binding Domain Mimetics
Niko Schmiedeberg, Manfred Schmitt, Christian Rölz, Vincent Truffault, Martin Sukopp, Markus Bürgle, Olaf G. Wilhelm, Wolfgang Schmalix, Viktor Magdolen, and Horst Kessler
pp 4984–4994Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm020254q
Thrombin Inhibition by Novel Benzamidine Derivatives: A Free-Energy Perturbation Study
Cristiano Ruch Werneck Guimarães and Ricardo Bicca de Alencastro
pp 4995–5004Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm020123p
Identification of Potent and Selective Small-Molecule Inhibitors of Caspase-3 through the Use of Extended Tethering and Structure-Based Drug Design
Ingrid C. Choong, Willard Lew, Dennis Lee, Phuongly Pham, Matthew T. Burdett, Joni W. Lam, Christian Wiesmann, Tinh N. Luong, Bruce Fahr, Warren L. DeLano, Robert S. McDowell, Darin A. Allen, Daniel A. Erlanson, Eric M. Gordon, and Tom O'Brien
pp 5005–5022Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm020230j
Efficient Synthesis and Cell-Transfection Properties of a New Multivalent Cationic Lipid for Nonviral Gene Delivery
Kai Ewert, Ayesha Ahmad, Heather M. Evans, Hans-Werner Schmidt, and Cyrus R. Safinya
pp 5023–5029Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm020233w
Design, Synthesis and Biological Evaluation of Novel N-Alkyl- and N-Acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as Novel A1 Adenosine Receptor Antagonists
Ettore Novellino, Enrico Abignente, Barbara Cosimelli, Giovanni Greco, Manuela Iadanza, Sonia Laneri, Antonio Lavecchia, and Maria Grazia RimoliFederico Da Settimo and Giampaolo PrimofioreDaniela Tuscano, Letizia Trincavelli, and Claudia Martini
pp 5030–5036Publication Date (Web): October 16, 2002 (Article)
DOI: 10.1021/jm020911e
Antitumor Agents. 217. Curcumin Analogues as Novel Androgen Receptor Antagonists with Potential as Anti-Prostate Cancer Agents
Hironori Ohtsu, Zhiyan Xiao, Junko Ishida, Masahiro Nagai, Hui-Kang Wang, Hideji Itokawa, Ching-Yuan Su, Charles Shih, Tzuying Chiang, Eugene Chang, YiFen Lee,YiFen Lee, Meng-Yin Tsai, Chawnshang Chang, and Kuo-Hsiung Lee
pp 5037–5042Publication Date (Web): October 12, 2002 (Article)
DOI: 10.1021/jm020200g
Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABAA Receptor
Pamela A. Albaugh, Lu Marshall, James Gregory, Geoff White, Alan Hutchison, Phil C. Ross, Dorothy W. Gallagher, John F. Tallman, Matt Crago, and James V. Cassella
pp 5043–5051Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm0202019
Synthesis and Biological Activity of Strongly Fluorescent Tricyclic Analogues of Acyclovir and Ganciclovir
Tomasz Goslinski, Bozenna Golankiewicz, Erik De Clercq, and Jan Balzarini
pp 5052–5057Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm020827z
Syntheses and Antitumor Targeting G1 Phase of the Cell Cycle of Benzoyldihydroisoquinolines and Related 1-Substituted Isoquinolines
Almudena Bermejo, Inmaculada Andreu, Fernando Suvire, Stephane Léonce, Daniel H. Caignard, Pierre Renard, Alain Pierré, Ricardo D. Enriz, Diego Cortes, and Nuria Cabedo
pp 5058–5068Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm020831a
Multiobjective Optimization in Quantitative Structure−Activity Relationships: Deriving Accurate and Interpretable QSARs
Orazio Nicolotti, Valerie J. Gillet, Peter J. Fleming, and Darren V. S. Green
pp 5069–5080Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm020919o
Synthesis and Structure−Activity Relationships of an Orally Available and Long-Acting Analgesic Peptide, Nα-Amidino-Tyr-d-Arg-Phe-MeβAla-OH (ADAMB)
Tadashi Ogawa, Tetsuhisa Miyamae, Kimie Murayama, Kaori Okuyama, Toru Okayama, Masaki Hagiwara, Shinobu Sakurada, and Tadanori Morikawa
pp 5081–5089Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm010357t
Novel p53 Inactivators with Neuroprotective Action: Syntheses and Pharmacological Evaluation of 2-Imino-2,3,4,5,6,7-hexahydrobenzothiazole and 2-Imino-2,3,4,5,6,7-hexahydrobenzoxazole Derivatives
Xiaoxiang Zhu, Qian-sheng Yu, Roy G. Cutler, Carsten W. Culmsee, Harold W. Holloway, Debomoy K. Lahiri, Mark P. Mattson, and Nigel H. Greig
pp 5090–5097Publication Date (Web): October 03, 2002 (Article)
DOI: 10.1021/jm020044d
Effect of Spermine Conjugation on the Cytotoxicity and Cellular Transport of Acridine
Jean-Guy Delcros, Sophie Tomasi, Simon Carrington, Bénédicte Martin, Jacques Renault, Ian S. Blagbrough, and Philippe Uriac
pp 5098–5111Publication Date (Web): October 02, 2002 (Article)
DOI: 10.1021/jm020843w
Synthesis and Evaluation of Analogues of 5‘-([(Z)-4-Amino-2-butenyl]methylamino)-5‘-deoxyadenosine as Inhibitors of Tumor Cell Growth, Trypanosomal Growth, and HIV-1 Infectivity
Canio J. Marasco, Jr., Debora L. Kramer, John Miller, Carl W. Porter, Cyrus J. Bacchi, Donna Rattendi, Louis Kucera, Nathan Iyer, Ralph Bernacki, Paula Pera, and Janice R. Sufrin
pp 5112–5122Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm0201621
In Vitro Photodynamic Properties of Chalcogenopyrylium Analogues of the Thiopyrylium Antitumor Agent AA1
Nancy K. Brennan, Jonathan P. Hall, Sherry R. Davies, Sandra O. Gollnick, Allan R. Oseroff, Scott L. Gibson, Russell Hilf, and Michael R. Detty
pp 5123–5135Publication Date (Web): October 09, 2002 (Article)
DOI: 10.1021/jm020260m
New Pyridobenzodiazepine Derivatives: Modifications of the Basic Side Chain Differentially Modulate Binding to Dopamine (D4.2, D2L) and Serotonin (5-HT2A) Receptors
Jean-François Liégeois, Laurence Eyrolles, Bart A. Ellenbroek, Christel Lejeune, Pascal Carato, Jacques Bruhwyler, Joseph Géczy, Jacques Damas, and Jacques Delarge
pp 5136–5149Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm0104825
Synthesis and Evaluation of No-Carrier-Added 8-Cyclopentyl-3-(3-[18F]fluoropropyl)-1-propylxanthine ([18F]CPFPX): A Potent and Selective A1-Adenosine Receptor Antagonist for in Vivo Imaging
Marcus H. Holschbach, Ray A. Olsson, Dirk Bier, Walter Wutz, Wiebke Sihver, Manfred Schüller, Bettina Palm, and Heinz H. Coenen
pp 5150–5156Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm020905i
CycloSal-BVDUMP Pronucleotides: How to Convert an Antiviral-Inactive Nucleoside Analogue into a Bioactive Compound against EBV
Chris Meier, Andreas Lomp, Astrid Meerbach, and Peter Wutzler
pp 5157–5172Publication Date (Web): October 08, 2002 (Article)
DOI: 10.1021/jm0209275
Synthesis of Classical and Nonclassical, Partially Restricted, Linear, Tricyclic 5-Deaza Antifolates1
Aleem Gangjee, Yibin Zeng, John J. McGuire, and Roy L. Kisliuk
pp 5173–5181Publication Date (Web): October 01, 2002 (Article)
DOI: 10.1021/jm0202369
Brief Articles
Spectral and Crystallographic Study of Pyridinic Analogues of Nimesulide: Determination of the Active Form of Methanesulfonamides as COX-2 Selective Inhibitors
Fabien Julémont, Xavier de Leval, Catherine Michaux, Jacques Damas, Caroline Charlier, François Durant, Bernard Pirotte, and Jean-Michel Dogné
pp 5182–5185Publication Date (Web): October 03, 2002 (Brief Article)
DOI: 10.1021/jm020920n
Book Reviews
Pharmaceutical and Medical Applications of Near-Infrared Spectroscopy. Practical Spectroscopy Series. Volume 31 By E. W. Ciurczak and J. K. Drennen III. Marcel Dekker, New York. 2002. ix + 192 pp. 16 × 23.5 cm. ISBN 0-8247-9453-2. $135.00.
p 5186Publication Date (Web): October 08, 2002 (Book Review)
DOI: 10.1021/jm020369u
Stereochemistry By David G. Morris. Wiley-Interscience/Royal Society of Chemistry, New York. 2002. vii + 170 pp. 19 × 24.5 cm. ISBN 0-471-22477. $34.95.
Kennerly S. Patrick
pp 5186–5187Publication Date (Web): October 08, 2002 (Book Review)
DOI: 10.1021/jm020370t
Houben−Weyl Methods of Organic Chemistry. Volume E22A. Synthesis of Peptides and Peptidomimetics Edited by Murray Goodman, Arthur Felix, Luis Moroder, and Claudio Toniolo. Georg Thieme Verlag, Stuttgart, Germany. 2001. xxvii + 901 pp. 18 × 26 cm. ISBN 3 132 19604 5. 1840 euro.
Victor J. Hruby
p 5187Publication Date (Web): October 08, 2002 (Book Review)
DOI: 10.1021/jm020371l
Additions and Corrections
Discovery of N-[2-[2-[[3-Methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4-morpholineacetamide as a Novel and Potent Inhibitor of Inosine Monophosphate Dehydrogenase (IMPDH) with Excellent in Vivo Activity.
T. G. Murali Dhar, Zhongqi Shen, Junqing Guo, Chunjian Liu, Scott H. Watterson, Henry H. Gu, William J. Pitts, Catherine A. Fleener, Katherine A. Rouleau, N. Z. Sherbina, Kim W. McIntyre, David J. Shuster, Mark R. Witmer, Jeffrey A. Tredup, Bang-Chi Chen, Rulin Zhao, Mark S. Bednarz, Daniel L. Cheney, John F. MacMaster, Laura M. Miller, Karen K. Berry, Timothy W. Harper, Joel C. Barrish, Diane L. Hollenbaugh, and Edwin J. Iwanowicz:
p 5188Publication Date (Web): October 12, 2002 (Addition/Correction)
DOI: 10.1021/jm020366h