Table of Contents
June 17, 2004
Volume 47, Issue 13
Pages 3329-3461
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
Per-6-substituted-per-6-deoxy β-cyclodextrins Inhibit the Formation of β-Amyloid Peptide Derived Soluble Oligomers
Zhiqiang Wang, Lei Chang, William L. Klein, Gregory R. J. Thatcher, and Duane L. Venton
pp 3329–3333Publication Date (Web): May 15, 2004 (Letter)
DOI: 10.1021/jm034224e
Hi-Res PDFAssessment of Multiple Binding Modes in Ligand−Protein Docking
Per Källblad, Ricardo L. Mancera, and Nikolay P. Todorov
pp 3334–3337Publication Date (Web): May 26, 2004 (Letter)
DOI: 10.1021/jm0498147
Articles
Design and Synthesis of Novel Biologically Active Thrombin Receptor Non-Peptide Mimetics Based on the Pharmacophoric Cluster Phe/Arg/NH2 of the Ser42-Phe-Leu-Leu-Arg46 Motif Sequence: Platelet Aggregation and Relaxant Activities
Kostas Alexopoulos, Panagiotis Fatseas, Euthemia Melissari, Demetrios Vlahakos, Panagiota Roumelioti, Thomas Mavromoustakos, Stefan Mihailescu, Maria Christina Paredes-Carbajal, Dieter Mascher, and John Matsoukas
pp 3338–3352Publication Date (Web): May 19, 2004 (Article)
DOI: 10.1021/jm031080v
Design and Synthesis of Potent Inhibitors of the Malaria Aspartyl Proteases Plasmepsin I and II. Use of Solid-Phase Synthesis to Explore Novel Statine Motifs
Per-Ola Johansson, Yantao Chen, Anna Karin Belfrage, Michael J. Blackman, Ingemar Kvarnström, Katarina Jansson, Lotta Vrang, Elizabeth Hamelink, Anders Hallberg, Åsa Rosenquist, and Bertil Samuelsson
pp 3353–3366Publication Date (Web): May 26, 2004 (Article)
DOI: 10.1021/jm031106i
3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding
Paolo Pevarello, Maria Gabriella Brasca, Raffaella Amici, Paolo Orsini, Gabriella Traquandi, Luca Corti, Claudia Piutti, Pietro Sansonna, Manuela Villa, Betsy S. Pierce, Maurizio Pulici, Patrizia Giordano, Katia Martina, Edward L. Fritzen, Richard A. Nugent, Elena Casale, Alexander Cameron, Marina Ciomei, Fulvia Roletto, Antonella Isacchi, GianPaolo Fogliatto, Enrico Pesenti, Wilma Pastori, Aurelio Marsiglio, Karen L. Leach, Paula M. Clare, Francesco Fiorentini, Mario Varasi, Anna Vulpetti, and Martha A. Warpehoski
pp 3367–3380Publication Date (Web): May 15, 2004 (Article)
DOI: 10.1021/jm031145u
Progesterone Receptor Ligand Binding Pocket Flexibility: Crystal Structures of the Norethindrone and Mometasone Furoate Complexes
Kevin P. Madauss, Su-Jun Deng, Robert J. H. Austin, Millard H. Lambert, Iain McLay, John Pritchard, Steven A. Short, Eugene L. Stewart, Ian J. Uings, and Shawn P. Williams
pp 3381–3387Publication Date (Web): May 13, 2004 (Article)
DOI: 10.1021/jm030640n
Structure−Activity Relationships at Monoamine Transporters for a Series of N-Substituted 3α-(Bis[4-fluorophenyl]methoxy)tropanes: Comparative Molecular Field Analysis, Synthesis, and Pharmacological Evaluation
Santosh S. Kulkarni, Peter Grundt, Theresa Kopajtic, Jonathan L. Katz, and Amy Hauck Newman
pp 3388–3398Publication Date (Web): May 15, 2004 (Article)
DOI: 10.1021/jm030646c
Synthesis, Structure−Activity Relationships, and Drug Resistance of β-d-3‘-Fluoro-2‘,3‘-Unsaturated Nucleosides as Anti-HIV Agents
Wen Zhou, Giuseppe Gumina, Youhoon Chong, Jianing Wang, Raymond F. Schinazi, and Chung K. Chu
pp 3399–3408Publication Date (Web): May 15, 2004 (Article)
DOI: 10.1021/jm040027j
On the Function of the 14 Å Long Internal Cavity of Histone Deacetylase-Like Protein: Implications for the Design of Histone Deacetylase Inhibitors
Di-Fei Wang, Olaf Wiest, Paul Helquist, Hsuan-Yin Lan-Hargest, and Norbert L. Wiech
pp 3409–3417Publication Date (Web): May 25, 2004 (Article)
DOI: 10.1021/jm0498497
Hybrids of [TSAO-T]−[Foscarnet]: The First Conjugate of Foscarnet with a Non-nucleoside Reverse Transcriptase Inhibitor through a Labile Covalent Ester Bond
Sonsoles Velázquez, Esther Lobatón, Erik De Clercq, Dianna L. Koontz, John W. Mellors, Jan Balzarini, and Mara-Jos Camarasa
pp 3418–3426Publication Date (Web): May 21, 2004 (Article)
DOI: 10.1021/jm031045o
Selective Inhibition of Trypanosoma brucei 6-Phosphogluconate Dehydrogenase by High-Energy Intermediate and Transition-State Analogues
Christophe Dardonville, Eliana Rinaldi, Michael P. Barrett, Reto Brun, Ian H. Gilbert, and Stefania Hanau
pp 3427–3437Publication Date (Web): May 22, 2004 (Article)
DOI: 10.1021/jm031066i
Synthesis, X-ray Crystal Structures, Stabilities, and in Vitro Cytotoxic Activities of New Heteroarylacrylonitriles
Franciszek Sa̧czewski, Przemyslaw Reszka, Maria Gdaniec, Renate Grünert, and Patrick J. Bednarski
pp 3438–3449Publication Date (Web): May 15, 2004 (Article)
DOI: 10.1021/jm0311036
Determinants of Corticotropin Releasing Factor. Receptor Selectivity of Corticotropin Releasing Factor Related Peptides
Adam W. Mazur, Feng Wang, Michelle Tscheiner, Elizabeth Donnelly, and Robert J. Isfort
pp 3450–3454Publication Date (Web): May 25, 2004 (Article)
DOI: 10.1021/jm049883l
Novel Pyridazino[4,3-b]indoles with Dual Inhibitory Activity against Mycobacterium tuberculosis and Monoamine Oxidase
Valeriya S. Velezheva, Patrick J. Brennan, Vladimir Yu. Marshakov, Dmitrij V. Gusev, Inessa N. Lisichkina, Alexander S. Peregudov, Larisa N. Tchernousova, Tatiana G. Smirnova, Sofia N. Andreevskaya, and Alexei E. Medvedev
pp 3455–3461Publication Date (Web): May 15, 2004 (Article)
DOI: 10.1021/jm030479g