Table of Contents
November 21, 2002
Volume 45, Issue 24
Pages 5189-5414
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Articles
Novel Soluble Cationic trans-Diaminedichloroplatinum(II) Complexes that Are Active against Cisplatin Resistant Ovarian Cancer Cell Lines
Yousef Najajreh, Jose Manuel Perez, Carmen Navarro-Ranninger, and Dan Gibson
pp 5189–5195Publication Date (Web): October 30, 2002 (Article)
DOI: 10.1021/jm0201969
Hi-Res PDFNovel Apoptosis-Inducing trans-Platinum Piperidine Derivatives: Synthesis and Biological Characterization
Elena Khazanov, Yechezkel Barenholz, Dan Gibson, and Yousef Najajreh
pp 5196–5204Publication Date (Web): October 30, 2002 (Article)
DOI: 10.1021/jm020817y
Antitumor Agents. 1. Synthesis, Biological Evaluation, and Molecular Modeling of 5H-Pyrido[3,2-a]phenoxazin-5-one, a Compound with Potent Antiproliferative Activity
Adele Bolognese, Gaetano Correale, Michele Manfra, Antonio Lavecchia, Orazio Mazzoni, Ettore Novellino, Vincenzo Barone, Alessandra Pani, Enzo Tramontano, Paolo La Colla, Chiara Murgioni, Ilaria Serra, Giovanna Setzu, and Roberta Loddo
pp 5205–5216Publication Date (Web): October 22, 2002 (Article)
DOI: 10.1021/jm020913z
Antitumor Agents. 2. Synthesis, Structure−Activity Relationships, and Biological Evaluation of Substituted 5H-Pyridophenoxazin-5-ones with Potent Antiproliferative Activity
Adele Bolognese, Gaetano Correale, Michele Manfra, Antonio Lavecchia, Orazio Mazzoni, Ettore Novellino, Vincenzo Barone, Paolo La Colla, and Roberta Loddo
pp 5217–5223Publication Date (Web): October 22, 2002 (Article)
DOI: 10.1021/jm020918w
Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 2. Probing the Indeno Ring Substituent Pattern
David A. Nugiel, Anup Vidwans, Anna-Marie Etzkorn, Karen A. Rossi, Pamela A. Benfield, Catherine R. Burton, Sarah Cox, Deborah Doleniak, and Steven P. Seitz
pp 5224–5232Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm020171+
Full Text HTMLSynthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 3. Structure Activity Relationships at C31,2
Eddy W. Yue, C. Anne Higley, Susan V. DiMeo, David J. Carini, David A. Nugiel, Carrie Benware, Pamela A. Benfield, Catherine R. Burton, Sarah Cox, Robert H. Grafstrom, Diane M. Sharp, Lisa M. Sisk, John F. Boylan, Jodi K. Muckelbauer, Angela M. Smallwood, Haiying Chen, Chong-Hwan Chang, Steven P. Seitz, and George L. Trainor
pp 5233–5248Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm0201722
Molecular Docking and 3D-QSAR Studies on Gag Peptide Analogue Inhibitors Interacting with Human Cyclophilin A
Meng Cui, Xiaoqin Huang, Xiaomin Luo, James M. Briggs, Ruyun Ji, Kaixian Chen, Jianhua Shen, and Hualiang Jiang
pp 5249–5259Publication Date (Web): October 30, 2002 (Article)
DOI: 10.1021/jm020082x
Novel Dual Inhibitors of AChE and MAO Derived from Hydroxy Aminoindan and Phenethylamine as Potential Treatment for Alzheimer's Disease
Jeffrey Sterling, Yaacov Herzig, Tamar Goren, Nina Finkelstein, David Lerner, Willy Goldenberg, Istvan Miskolczi, Sandor Molnar, Ferenc Rantal, Tivadar Tamas, Gyorgy Toth, Adela Zagyva, Andras Zekany, Gila Lavian, Aviva Gross, Rachel Friedman, Michal Razin, Wei Huang, Boris Krais, Michael Chorev, Moussa B. Youdim, and Marta Weinstock
pp 5260–5279Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm020120c
Novel, Potent ORL-1 Receptor Agonist Peptides Containing α-Helix-Promoting Conformational Constraints
Chongwu Zhang, Wendy Miller, Kenneth J. Valenzano, and Donald J. Kyle
pp 5280–5286Publication Date (Web): October 9, 2002 (Article)
DOI: 10.1021/jm0202021
Structure−Activity Studies of the Melanocortin Peptides: Discovery of Potent and Selective Affinity Antagonists for the hMC3 and hMC4 Receptors
Paolo Grieco, Antonio Lavecchia, Minying Cai, Devendra Trivedi, David Weinberg, Tanya MacNeil, L. H. T. Van der Ploeg, and Victor J. Hruby
pp 5287–5294Publication Date (Web): October 22, 2002 (Article)
DOI: 10.1021/jm0202526
Sulfamide-Based Inhibitors for Carboxypeptidase A. Novel Type Transition State Analogue Inhibitors for Zinc Proteases
Jung Dae Park, Dong H. Kim, Seung-Jun Kim, Joo-Rang Woo, and Seong Eon Ryu
pp 5295–5302Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm020258v
Design, Synthesis, and Tripeptidyl Peptidase II Inhibitory Activity of a Novel Series of (S)-2,3-Dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles
Henry J. Breslin, Tamara A. Miskowski, Michael J. Kukla, William H. Leister, Hans L. De Winter, Diane A. Gauthier, Maria V. F. Somers, Daniëlle C. G. Peeters, and Peter W. M. Roevens
pp 5303–5310Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm0202831
A New Approach to Finding Natural Chemical Structure Classes
Jun Xu
pp 5311–5320Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm010520k
Design of Noncovalent Inhibitors of Human Cathepsin L. From the 96-Residue Proregion to Optimized Tripeptides
Shafinaz F. Chowdhury, J. Sivaraman, Jing Wang, Gopal Devanathan, Paule Lachance, Hongtao Qi, Robert Ménard, Jean Lefebvre, Yasuo Konishi, Miroslaw Cygler, Traian Sulea, and Enrico O. Purisima
pp 5321–5329Publication Date (Web): October 17, 2002 (Article)
DOI: 10.1021/jm020238t
Effects of Isoprenoid Analogues of SDB-Ethylenediamine on Multidrug Resistant Tumor Cells Alone and in Combination with Chemotherapeutic Drugs
Tatyana A. Sidorova, Albert G. Nigmatov, Eugenia S. Kakpakova, Alla A. Stavrovskaya, Galina K. Gerassimova, Alexander A. Shtil, and Edward P. Serebryakov
pp 5330–5339Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm011010t
Syntheses and Calcium-Mobilizing Evaluations of N1-Glycosyl-Substituted Stable Mimics of Cyclic ADP-Ribose
Li-Jun Huang, Yong-Yuan Zhao, Lan Yuan, Ji-Mei Min, and Li-He Zhang
pp 5340–5352Publication Date (Web): October 18, 2002 (Article)
DOI: 10.1021/jm010530l
Probing Opioid Receptor Interactions with Azacycloalkane Amino Acids. Synthesis of a Potent and Selective ORL1 Antagonist
Liliane Halab, Jérôme A. J. Becker, Zsuzsanna Darula, Dirk Tourwé, Brigitte L. Kieffer, Frédéric Simonin, and William D. Lubell
pp 5353–5357Publication Date (Web): October 15, 2002 (Article)
DOI: 10.1021/jm020078l
Investigations on Estrogen Receptor Binding. The Estrogenic, Antiestrogenic, and Cytotoxic Properties of C2-Alkyl-Substituted 1,1-Bis(4-hydroxyphenyl)-2-phenylethenes
Veronika Lubczyk, Helmut Bachmann, and Ronald Gust
pp 5358–5364Publication Date (Web): October 23, 2002 (Article)
DOI: 10.1021/jm0209230
Structure−Activity Relationships of 1-Alkyl-5-(3,4-dichlorophenyl)- 5-{2-[(3-substituted)-1-azetidinyl]ethyl}-2-piperidones. 1. Selective Antagonists of the Neurokinin-2 Receptor
A. Roderick MacKenzie, Allan P. Marchington, Donald S. Middleton, Sandra D. Newman, and Barry C. Jones
pp 5365–5377Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm0209331
Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 17. Highly δ Opioid Receptor Selective 14-Alkoxy-Substituted Indolo- and Benzofuromorphinans
Johannes Schütz, Christina M. Dersch, Robert Horel, Mariana Spetea, Martin Koch, Ruth Meditz, Elisabeth Greiner, Richard B. Rothman, and Helmut Schmidhammer
pp 5378–5383Publication Date (Web): October 29, 2002 (Article)
DOI: 10.1021/jm020940p
Adenosine 5‘-O-(1-Boranotriphosphate) Derivatives as Novel P2Y1 Receptor Agonists
Victoria Nahum, Gregor Zündorf, Sébastien A. Lévesque, Adrien R. Beaudoin, Georg Reiser, and Bilha Fischer
pp 5384–5396Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm020251d
Synthesis of Halogen-Substituted Pyridyl and Pyrimidyl Derivatives of [3,2-c]Pyrazolo Corticosteroids: Strategies for the Development of Glucocorticoid Receptor Mediated Imaging Agents
Robert M. Hoyte, Jing-xin Zhang, Ronald Lerum, Aladejebi Oluyemi, Prita Persaud, Craig O'Connor, David C. Labaree, and Richard B. Hochberg
pp 5397–5405Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm0202775
Brief Articles
Nitric Oxide Releasing Morpholine Derivatives as Hypolipidemic and Antioxidant Agents
Michael C. Chrysselis, Eleni A. Rekka, Ioanna C. Siskou, and Panos N. Kourounakis
pp 5406–5409Publication Date (Web): October 26, 2002 (Brief Article)
DOI: 10.1021/jm011062i
Design, Synthesis, Structure−Activity Relationships, and Molecular Modeling Studies of 2,3-Diaryl-1,3-thiazolidin-4-ones as Potent Anti-HIV Agents
Maria L. Barreca, Jan Balzarini, Alba Chimirri, Erik De Clercq, Laura De Luca, Hans Dieter Höltje, Monika Höltje, Anna Maria Monforte, Pietro Monforte, Christophe Pannecouque, Angela Rao, and Maria Zappalà
pp 5410–5413Publication Date (Web): October 25, 2002 (Brief Article)
DOI: 10.1021/jm020977+
Additions and Corrections
Synthesis and Biological Activities of Cyclic Lanthionine Enkephalin Analogues: δ-Opioid Receptor Selective Ligands.
Yosup Rew, Shelle Malkmus, Camilla Svensson, Tony L. Yaksh, Nga N. Chung, Peter W. Schiller, Joel A. Cassel, Robert N. DeHaven, Joseph P. Taulane, and Murray Goodman:
p 5414Publication Date (Web): October 26, 2002 (Addition/Correction)
DOI: 10.1021/jm0203682