Journal of Medicinal Chemistry: Volume 48, Issue 18 (ACS Publications)

September 8, 2005

Volume 48, Issue 18

Pages 5613-5874

About the Cover: Illustration of the binding mode of a biheteroaryl inhibitor to vascular endothelial growth factor receptor-2 (Kuo, G.-H.; et al. J. Med. Chem. 2005, 48, 1886-1900).

2005 American Chemical Society
A. C. Cope Award Address

Joys of Molecules. 2. Endeavors in Chemical Biology and Medicinal Chemistry

K. C. Nicolaou

pp 5613–5638

Publication Date (Web): September 1, 2005 (Special Topics)

DOI: 10.1021/jm050524f

Abstract

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Letters

Discovery of a 1H-Benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) Inhibitor of Insulin-like Growth Factor I Receptor Kinase with in Vivo Antitumor Activity

Mark Wittman, Joan Carboni, Ricardo Attar, Balu Balasubramanian, Praveen Balimane, Patrick Brassil, Francis Beaulieu, Chiehying Chang, Wendy Clarke, Janet Dell, Jeffrey Eummer, David Frennesson, Marco Gottardis, Ann Greer, Steven Hansel, Warren Hurlburt, Bruce Jacobson, Subramaniam Krishnananthan, Francis Y. Lee, Aixin Li, Tai-An Lin, Peiying Liu, Carl Ouellet, Xiaopeng Sang, Mark G. Saulnier, Karen Stoffan, Yax Sun, Upender Velaparthi, Henry Wong, Zheng Yang, Kurt Zimmermann, Mary Zoeckler, and Dolatrai Vyas

pp 5639–5643

Publication Date (Web): August 6, 2005 (Letter)

DOI: 10.1021/jm050392q

Table of Contents

2005 American Chemical SocietyA. C. Cope Award Address

Joys of Molecules. 2. Endeavors in Chemical Biology and Medicinal Chemistry

Letters

Discovery of a 1H-Benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) Inhibitor of Insulin-like Growth Factor I Receptor Kinase with in Vivo Antitumor Activity

4-Aryl-1,2,3-triazole: A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo

A Systematic Analysis of the Effect of Small-Molecule Binding on Protein Flexibility of the Ligand-Binding Sites

Enhancement of Aqueous Solubility and Stability Employing a Trans Acetate Axis in Trans Planar Amine Platinum Compounds while Maintaining the Biological Profile

The First de Novo-Designed Antagonists of the Human NK2 Receptor

Articles

Factorizing Selectivity Determinants of Inhibitor Binding toward Aldose and Aldehyde Reductases: Structural and Thermodynamic Properties of the Aldose Reductase Mutant Leu300Pro−Fidarestat Complex

Impact of Induced Fit on Ligand Binding to the Androgen Receptor: A Multidimensional QSAR Study To Predict Endocrine-Disrupting Effects of Environmental Chemicals

6,19-Sulfur-Bridged Progesterone Analogues with Antiimmunosuppressive Activity1

6-Acylamino-2-aminoquinolines as Potent Melanin-Concentrating Hormone 1 Receptor Antagonists. Identification, Structure−Activity Relationship, and Investigation of Binding Mode

Autocorrelation of Molecular Electrostatic Potential Surface Properties Combined with Partial Least Squares Analysis as New Strategy for the Prediction of the Activity of Human A3 Adenosine Receptor Antagonists

Synthesis and Biological Activity of Flurbiprofen Analogues as Selective Inhibitors of β-Amyloid1-42 Secretion

Carbonic Anhydrase Inhibitors: Stacking with Phe131 Determines Active Site Binding Region of Inhibitors As Exemplified by the X-ray Crystal Structure of a Membrane-Impermeant Antitumor Sulfonamide Complexed with Isozyme II

Theoretical and Experimental Design of Atypical Kinase Inhibitors: Application to p38 MAP Kinase

Conformationally Constrained Analogues of Diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 Carbonyl Functionality Reveals the Essential Role of the sn-1 Carbonyl at the Lipid Interface in the Binding of DAG-Lactones to Protein Kinase C

E-Ring Modified Steroids as Novel Potent Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1

Pharmacophore-Guided Drug Discovery Investigations Leading to Bioactive 5-Aminotetrahydropyrazolopyridines. Implications for the Binding Mode of Heterocyclic Dopamine D3 Receptor Agonists

Design and Synthesis of Tricyclic Corticotropin-Releasing Factor-1 Antagonists

4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as Non-Nucleoside Inhibitors of Human Cytomegalovirus and Related Herpesvirus Polymerases

Modifications to the Tetracaine Scaffold Produce Cyclic Nucleotide-Gated Channel Blockers with Widely Varying Efficacies

Synthesis and Structure−Activity Relationship of a Novel Series of Aminoalkylindoles with Potential for Imaging the Neuronal Cannabinoid Receptor by Positron Emission Tomography

Novel Potent Antagonists of Transient Receptor Potential Channel, Vanilloid Subfamily Member 1: Structure−Activity Relationship of 1,3-Diarylalkyl Thioureas Possessing New Vanilloid Equivalents

Discovery of Potent, Nonsystemic Apical Sodium-Codependent Bile Acid Transporter Inhibitors (Part 1)

Discovery of Potent, Nonsystemic Apical Sodium-Codependent Bile Acid Transporter Inhibitors (Part 2)

Brief Articles

Cytostatic 6-Arylpurine Nucleosides. 6. SAR in Anti-HCV and Cytostatic Activity of Extended Series of 6-Hetarylpurine Ribonucleosides

Additions and Corrections

Synthesis and Biological Evaluation of Dimeric RGD Peptide−Paclitaxel Conjugate as a Model for Integrin-Targeted Drug Delivery.

2005 American Chemical Society
A. C. Cope Award Address

The First de Novo-Designed Antagonists of the Human NK₂ Receptor

6,19-Sulfur-Bridged Progesterone Analogues with Antiimmunosuppressive Activity¹

Autocorrelation of Molecular Electrostatic Potential Surface Properties Combined with Partial Least Squares Analysis as New Strategy for the Prediction of the Activity of Human A₃ Adenosine Receptor Antagonists

Synthesis and Biological Activity of Flurbiprofen Analogues as Selective Inhibitors of β-Amyloid₁_-₄₂ Secretion