Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand Fulltext Access 4 Pages 2008
Synthesis and evaluation of antitubercular activity of glycosyl thio- and sulfonyl acetamide derivatives Fulltext Access 4 Pages 2008
Simultaneous identification of multiple receptors of natural product using an optimized cDNA phage display cloning Fulltext Access 4 Pages 2008
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts Fulltext Access 4 Pages 2008
Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry Fulltext Access 4 Pages 2008
Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR) Fulltext Access 4 Pages 2008
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent Fulltext Access 4 Pages 2008
Natural products in parallel synthesis: Triazole libraries of nonactic acid Fulltext Access 4 Pages 2008
Carbonic anhydrase inhibitors: Thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? Fulltext Access 4 Pages 2008
Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation Fulltext Access 4 Pages 2008
Detection of structure-switching in G-quadruplexes using end-stacking ability Fulltext Access 4 Pages 2008
Tentacle type peptides as artificial lectins against sulfated Lewis X and A Fulltext Access 4 Pages 2008
Discovery of novel and potent aryl diamines as leukotriene A4 hydrolase inhibitors Fulltext Access 4 Pages 2008
Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A4 hydrolase Fulltext Access 4 Pages 2008
Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives Fulltext Access 4 Pages 2008
Cyclobranol: A substrate for C25-methyl sterol side chains and potent mechanism-based inactivator of plant sterol methyltransferase Fulltext Access 4 Pages 2008
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition Fulltext Access 4 Pages 2008
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists Fulltext Access 4 Pages 2008
Synthesis and structure–activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT2C receptor antagonists Fulltext Access 4 Pages 2008
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: Isoindoline containing inhibitors Fulltext Access 4 Pages 2008
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors Fulltext Access 4 Pages 2008
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I Fulltext Access 4 Pages 2008
N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum Fulltext Access 4 Pages 2008
Enhanced anti-influenza A virus activity of (−)-epigallocatechin-3-O-gallate fatty acid monoester derivatives: Effect of alkyl chain length Fulltext Access 4 Pages 2008
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI) Fulltext Access 4 Pages 2008
Synthesis and screening of small molecule inhibitors of anthrax edema factor Fulltext Access 4 Pages 2008
Synthesis and biological evaluation of 1-(benzenesulfonamido)-2-[5-(N-hydroxypyridin-2(1H)-one)]acetylene regioisomers: A novel class of 5-lipoxygenase inhibitors Fulltext Access 4 Pages 2008
The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity Fulltext Access 4 Pages 2008
Design, synthesis of novel peptidomimetic derivatives of 4-HPR for rhabdoid tumors Fulltext Access 4 Pages 2008
Discovery of a novel, potent and orally active series of γ-lactams as selective NK1 antagonists Fulltext Access 4 Pages 2008
[18F]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of β-amyloid fibrils Fulltext Access 4 Pages 2008
Imidazolidin-4-one peptidomimetic derivatives of primaquine: Synthesis and antimalarial activity Fulltext Access 4 Pages 2008
Molecular recognition of a DNA:RNA hybrid: Sub-nanomolar binding by a neomycin–methidium conjugate Fulltext Access 4 Pages 2008
Correlation between reduction potentials and inhibitions of Epstein–Barr virus activation by anthraquinone derivatives Fulltext Access 4 Pages 2008
Synthesis and in vivo evaluation of 11-substituted estradiol derivatives as anti-implantation agents Fulltext Access 4 Pages 2008
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold Fulltext Access 4 Pages 2008
Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors Fulltext Access 4 Pages 2008
Identifying structural features on 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones critical for Neuropeptide S antagonist activity Fulltext Access 4 Pages 2008
Cyathuscavins A, B, and C, new free radical scavengers with DNA protection activity from the Basidiomycete Cyathus stercoreus Fulltext Access 4 Pages 2008
Designing rapid onset selective serotonin re-uptake inhibitors. 2: Structure–activity relationships of substituted (aryl)benzylamines Fulltext Access 4 Pages 2008
Reprint of “Crystal structure of chemically synthesized HIV-1 protease and a ketomethylene isostere inhibitor based on the p2/NC cleavage site” [Bioorg. Med. Chem. Lett. 18 (2008) 4554-4557] Fulltext Access 4 Pages 2008
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties Fulltext Access 4 Pages 2008
(3R)-3-Amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Fulltext Access 4 Pages 2008
In vitro biological evaluation of novel 7-O-dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines Fulltext Access 4 Pages 2008
A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity Fulltext Access 4 Pages 2008
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists Fulltext Access 4 Pages 2008
Design, synthesis and RNase A inhibition activity of catechin and epicatechin and nucleobase chimeric molecules Fulltext Access 4 Pages 2008
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A2A antagonists with improved solubility and metabolic stability Fulltext Access 4 Pages 2008
Semisynthesis and antitumoral activity of 2-acetylfuranonaphthoquinone and other naphthoquinone derivatives from lapachol Fulltext Access 4 Pages 2008
Inhibition of Candida albicans isocitrate lyase activity by sesterterpene sulfates from the tropical sponge Dysidea sp. Fulltext Access 4 Pages 2008
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors Fulltext Access 4 Pages 2008
NODAPA-OH and NODAPA-(NCS)n: Synthesis, 68Ga-radiolabelling and in vitro characterisation of novel versatile bifunctional chelators for molecular imaging Fulltext Access 4 Pages 2008
Studies on the synthesis of neamine-dinucleosides and neamine-PNA conjugates and their interaction with RNA Fulltext Access 4 Pages 2008
Antibiotic evaluation and in vivo analysis of alkynyl Coenzyme A antimetabolites in Escherichia coli Fulltext Access 4 Pages 2008
Synthesis of β-hydroxy-α-amino acids with a reengineered alanine racemase Fulltext Access 4 Pages 2008
Evaluation of a focused library of N-aryl l-homoserine lactones reveals a new set of potent quorum sensing modulators Fulltext Access 4 Pages 2008
Paclitaxel succinate analogs: Anionic and amide introduction as a strategy to impart blood–brain barrier permeability Fulltext Access 4 Pages 2008
Descriptor-free molecular discovery in large libraries by adaptive substituent reordering Fulltext Access 4 Pages 2008
Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis Fulltext Access 4 Pages 2008
Kinetic isotope effects in the oxidation of arachidonic acid by soybean lipoxygenase-1 Fulltext Access 4 Pages 2008
Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta Fulltext Access 4 Pages 2008
Evaluation of new migrastatin and dorrigocin congeners unveils cell migration inhibitors with dramatically improved potency Fulltext Access 4 Pages 2008
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine KCa channel blockers Fulltext Access 4 Pages 2008
Novel design principle validated: Glucopyranosylidene-spiro-oxathiazole as new nanomolar inhibitor of glycogen phosphorylase, potential antidiabetic agent Fulltext Access 4 Pages 2008
Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor γ Fulltext Access 4 Pages 2008
Identification of novel protein kinase CK1 delta (CK1δ) inhibitors through structure-based virtual screening Fulltext Access 4 Pages 2008
Cu-free cycloaddition for identifying catalytic active adenylation domains of nonribosomal peptide synthetases by phage display Fulltext Access 4 Pages 2008
DNA-templated click chemistry for creation of novel DNA binding molecules Fulltext Access 4 Pages 2008
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors Fulltext Access 4 Pages 2008
Synthesis and immunostimulatory properties of the phosphorothioate analogues of cdiGMP Fulltext Access 4 Pages 2008
bis-Pyridinium cyclophanes: Novel ligands with high affinity for the blood–brain barrier choline transporter Fulltext Access 4 Pages 2008
Synthesis and biological evaluation of alkoxycoumarins as novel nematicidal constituents Fulltext Access 4 Pages 2008
Phage display of functional, full-length human and viral membrane proteins Fulltext Access 4 Pages 2008
Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators Fulltext Access 4 Pages 2008
Synthesis and evaluation of novel 4-amino-4,6-androstadiene-3,17-dione: An analog of formestane Fulltext Access 4 Pages 2008
Design and synthesis of reboxetine analogs morpholine derivatives as selective norepinephrine reuptake inhibitors Fulltext Access 4 Pages 2008
5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk) Fulltext Access 4 Pages 2008
Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead Fulltext Access 4 Pages 2008
Design, synthesis and structure–activity relationship of simple bis-amides as potent inhibitors of GlyT1 Fulltext Access 4 Pages 2008
Using proton nuclear magnetic resonance to study the mode of ribonuclease A inhibition by competitive and noncompetitive inhibitors Fulltext Access 4 Pages 2008
3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators Fulltext Access 4 Pages 2008