Docking studies and development of novel 5-heteroarylamino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as potential antimalarials Fulltext Access 5 Pages 2006
Zn2+ dependent DNA binders based on terminally modified peptide nucleic acids Fulltext Access 5 Pages 2006
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents Fulltext Access 5 Pages 2006
Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant Fulltext Access 5 Pages 2006
3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent Fulltext Access 5 Pages 2006
Novel substituted naphthalen-1-yl-methanone derivatives as anti-hyperglycemic agents Fulltext Access 5 Pages 2006
N-Alkyl-N-arylmethylpiperidin-4-amines: Novel dual inhibitors of serotonin and norepinephrine reuptake Fulltext Access 5 Pages 2006
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy Fulltext Access 5 Pages 2006
A fast and robust 19F NMR-based method for finding new HIV-1 protease inhibitors Fulltext Access 5 Pages 2006
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: Synthesis and structure–activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors Fulltext Access 5 Pages 2006
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors Fulltext Access 5 Pages 2006
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors Fulltext Access 5 Pages 2006
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors Fulltext Access 5 Pages 2006
New 4-(4-methyl-phenyl)phthalazin-1(2H)-one derivatives and their effects on α1-receptors Fulltext Access 5 Pages 2006
Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas’ disease Fulltext Access 5 Pages 2006
p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones Fulltext Access 5 Pages 2006
Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay Fulltext Access 5 Pages 2006
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors Fulltext Access 5 Pages 2006
Analysis of complexes of inhibitors with Cryptosporidium hominis DHFR leads to a new trimethoprim derivative Fulltext Access 5 Pages 2006
Structure–activity relationships of N-substituted piperazine amine reuptake inhibitors Fulltext Access 5 Pages 2006
Synthesis and evaluation of novel 8-oxo-8H-cyclopenta[a]acenaphthylene-7-carbonitriles as long-wavelength fluorescent markers for hypoxic cells in solid tumor Fulltext Access 5 Pages 2006
Synthesis and insecticidal activity of fluorinated 2-(2,6-dichloro-4-trifluoromethylphenyl)-2,4,5,6-tetrahydrocyclopentapyrazoles Fulltext Access 5 Pages 2006
Aryl O- and S-galactosides and lactosides as specific inhibitors of human galectins-1 and -3: Role of electrostatic potential at O-3 Fulltext Access 5 Pages 2006
Biological studies of photoinducible phenol quaternary ammonium derivatives Fulltext Access 5 Pages 2006
New photoantimicrobial films composed of porphyrinated lipophilic cellulose esters Fulltext Access 5 Pages 2006
Discovery and optimization of a novel series of liver X receptor-α agonists Fulltext Access 5 Pages 2006
Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket Fulltext Access 5 Pages 2006
Novel inhibitors of hepatitis C NS3–NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid Fulltext Access 5 Pages 2006
Structural modifications of the cannabinoid side chain towards C3-aryl and 1′,1′-cycloalkyl-1′-cyano cannabinoids Fulltext Access 5 Pages 2006
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates Fulltext Access 5 Pages 2006
1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors Fulltext Access 5 Pages 2006
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases Fulltext Access 5 Pages 2006
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials Fulltext Access 5 Pages 2006
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists Fulltext Access 5 Pages 2006
Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17β-hydroxysteroid dehydrogenase type 3 Fulltext Access 5 Pages 2006
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors Fulltext Access 5 Pages 2006
8-Fluoroimidazo[1,2-a]pyridine: Synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABAA receptor Fulltext Access 5 Pages 2006
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl Fulltext Access 5 Pages 2006
6H,13H-Pyrazino[1,2-a;4,5-a′]diindole analogs: Probing the pharmacophore for allosteric ligands of muscarinic M2 receptors Fulltext Access 5 Pages 2006
Synthesis, characterization and antiamoebic activity of 1-(thiazolo[4,5-b]quinoxaline-2-yl)-3-phenyl-2-pyrazoline derivatives Fulltext Access 5 Pages 2006
Synthesis and in vitro anti-tumor activity of N-{1-[(3-thioxo-5,6-dihydroimidazo[2,1-c][1,2,4]thiadiazol-7-ylthio)thiocarbonyl]-2-imidazolidene}arylsulfonamides Fulltext Access 5 Pages 2006
Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase Fulltext Access 5 Pages 2006
Macrocyclic peptidomimetic inhibitors of β-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complex Fulltext Access 5 Pages 2006
Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5] Fulltext Access 5 Pages 2006
C8c–C15 monoseco-analogues of the phenanthroquinolizidine alkaloids julandine and cryptopleurine exhibiting potent anti-angiogenic properties Fulltext Access 5 Pages 2006
Synthesis and biological evaluation of novel heterocyclic quinones as inhibitors of the dual specificity protein phosphatase CDC25C Fulltext Access 5 Pages 2006
A novel class of potent influenza virus inhibitors: Polysubstituted acylthiourea and its fused heterocycle derivatives Fulltext Access 5 Pages 2006
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases Fulltext Access 5 Pages 2006
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection Fulltext Access 5 Pages 2006
Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents Fulltext Access 5 Pages 2006
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists Fulltext Access 5 Pages 2006
The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase Fulltext Access 5 Pages 2006
Pyrazole CCK1 receptor antagonists. Part 1: Solution-phase library synthesis and determination of Free–Wilson additivity Fulltext Access 5 Pages 2006
p38 MAP kinase inhibitors: Metabolically stabilized piperidine-substituted quinolinones and naphthyridinones Fulltext Access 5 Pages 2006
3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitors Fulltext Access 5 Pages 2006
Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: Potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubility Fulltext Access 5 Pages 2006
Design, synthesis and in vitro antimalarial activity of an acylhydrazone library Fulltext Access 5 Pages 2006
N-Hydroxyurea as zinc binding group in matrix metalloproteinase inhibition: Mode of binding in a complex with MMP-8 Fulltext Access 5 Pages 2006
Targeting the DNA minor groove with fused ring dicationic compounds: Comparison of in silico screening and a high-resolution crystal structure Fulltext Access 5 Pages 2006
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor Fulltext Access 5 Pages 2006
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists Fulltext Access 5 Pages 2006
Synthesis of 2-C-hydroxymethylribofuranosylpurines as potent anti-hepatitis C virus (HCV) agents Fulltext Access 5 Pages 2006
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters Fulltext Access 5 Pages 2006
N-Hydroxyurea—A versatile zinc binding function in the design of metalloenzyme inhibitors Fulltext Access 5 Pages 2006
Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability Fulltext Access 5 Pages 2006
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners Fulltext Access 5 Pages 2006
The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck) Fulltext Access 5 Pages 2006
Gram-scale synthesis of pinusolide and evaluation of its antileukemic potential Fulltext Access 5 Pages 2006
Antiproliferation and apoptosis induced by C-glycosides in human leukemia cancer cells Fulltext Access 5 Pages 2006
Synthesis and hypoxic–cytotoxic activity of some 3-amino-1,2,4-benzotriazine-1,4-dioxide derivatives Fulltext Access 5 Pages 2006
Synthesis and antitumor activity of two natural N-acetylglucosamine-bearing triterpenoid saponins: Lotoidoside D and E Fulltext Access 5 Pages 2006
Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc Fulltext Access 5 Pages 2006
Design, microwave-assisted synthesis, and spasmolytic activity of 2-(alkyloxyaryl)-1H-benzimidazole derivatives as constrained stilbene bioisosteres Fulltext Access 5 Pages 2006
Synthesis and antibacterial evaluation of ureides of Baylis–Hillman derivatives Fulltext Access 5 Pages 2006
Association studies of aggregated aqueous lutein diphosphate with human serum albumin and α1-acid glycoprotein in vitro: Evidence from circular dichroism and electronic absorption spectroscopy Fulltext Access 5 Pages 2006
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors Fulltext Access 5 Pages 2006
Putative therapeutic agents for the learning and memory deficits of people with Down syndrome Fulltext Access 5 Pages 2006
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase Fulltext Access 5 Pages 2006
Discovery of 3,5-bis(trifluoromethyl)benzyl l-arylglycinamide based potent CCR2 antagonists Fulltext Access 5 Pages 2006
Shaken not stirred: A facile synthesis of 1,4-bis(furo[2,3-d]-pyrimidine-2,4(1H,3H)-dione-5-yl)benzenes by one-pot reaction of isocyanides, N,N′-dimethylbarbituric acid, and terephthaldialdehyde Fulltext Access 5 Pages 2006
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4 Fulltext Access 5 Pages 2006
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes Fulltext Access 5 Pages 2006