Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 α-amino acid by a α-hydroxy acid Fulltext Access 5 Pages 2005
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS Fulltext Access 5 Pages 2005
Synthesis of alkyne derivatives of a novel triazolopyrazine as A2A adenosine receptor antagonists Fulltext Access 5 Pages 2005
Hybridization dependent cleavage of internally modified disulfide-peptide nucleic acids Fulltext Access 5 Pages 2005
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies Fulltext Access 5 Pages 2005
Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors Fulltext Access 5 Pages 2005
New derivatives of 1α,25-dihydroxy-19-norvitamin D3 with two substituents at C-2: synthesis and biological activity Fulltext Access 5 Pages 2005
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors Fulltext Access 5 Pages 2005
Synthesis and in vitro antitrypanosomal activity of novel Nifurtimox analogues Fulltext Access 5 Pages 2005
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists Fulltext Access 5 Pages 2005
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor Fulltext Access 5 Pages 2005
Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives Fulltext Access 5 Pages 2005
Chiral polyamines from reduction of polypeptides: asymmetric pyridoxamine-mediated transaminations Fulltext Access 5 Pages 2005
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents Fulltext Access 5 Pages 2005
cis-6-Oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition Fulltext Access 5 Pages 2005
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells Fulltext Access 5 Pages 2005
Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability Fulltext Access 5 Pages 2005
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors Fulltext Access 5 Pages 2005
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist Fulltext Access 5 Pages 2005
Enzymatic syntheses and selective hydrolysis of O-β-d-galactopyranosides using a marine mollusc β-galactosidase Fulltext Access 5 Pages 2005
A comparative binding study of BIV Tat peptide against its TAR RNA duplex, RNA-DNA heteroduplex and DNA duplex Fulltext Access 5 Pages 2005
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides Fulltext Access 5 Pages 2005
Potent Kv1.3 inhibitors from correolide-modification of the C18 position Fulltext Access 5 Pages 2005
Novel estimation of lipophilicity using 13C NMR chemical shifts as molecular descriptor Fulltext Access 5 Pages 2005
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus Fulltext Access 5 Pages 2005
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists Fulltext Access 5 Pages 2005
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design Fulltext Access 5 Pages 2005
Trypanocidal activity of (â)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi Fulltext Access 5 Pages 2005
Detection of aptamer-protein interactions using QCM and electrochemical indicator methods Fulltext Access 5 Pages 2005
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors Fulltext Access 5 Pages 2005
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines Fulltext Access 5 Pages 2005
Specific recognition of napthyridine-based ligands toward guanine-containing bulges in RNA duplexes and RNA-DNA heteroduplexes Fulltext Access 5 Pages 2005
Possible role of hydroxyl radicals in the oxidative degradation of folic acid Fulltext Access 5 Pages 2005
Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics Fulltext Access 5 Pages 2005
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists Fulltext Access 5 Pages 2005
Increased catalytic activity of protein disulfide isomerase using aromatic thiol based redox buffers Fulltext Access 5 Pages 2005
3,4-Dihydro-2H-benzoxazinones are 5-HT1A receptor antagonists with potent 5-HT reuptake inhibitory activity Fulltext Access 5 Pages 2005
Synthesis of 9-(2-β-C-methyl-β-d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication Fulltext Access 5 Pages 2005
Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake inhibitors Fulltext Access 5 Pages 2005
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8 Fulltext Access 5 Pages 2005
Synthesis and incorporation into DNA fragments of the artificial nucleobase, 2-amino-8-oxopurine Fulltext Access 5 Pages 2005
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors Fulltext Access 5 Pages 2005
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships Fulltext Access 5 Pages 2005
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents Fulltext Access 5 Pages 2005
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands Fulltext Access 5 Pages 2005
Kinetic model studies on the chemical ligation of oligonucleotides via hydrazone formation Fulltext Access 5 Pages 2005
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines Fulltext Access 5 Pages 2005
2,3-Dimethoxy-5-methyl-1,4-benzoquinones and 2-methyl-1,4-naphthoquinones: glycation inhibitors with lipid peroxidation activity Fulltext Access 5 Pages 2005
Synthesis and evaluation of novel peripherally restricted κ-opioid receptor agonists Fulltext Access 5 Pages 2005
Fluorescent metal ion indicators based on benzoannelated crown systems: a green fluorescent indicator for intracellular sodium ions Fulltext Access 5 Pages 2005
Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent Fulltext Access 5 Pages 2005
Spiro-annulation of barbituric acid derivatives and its analogs by ring-closing metathesis reaction Fulltext Access 5 Pages 2005
Synthesis and biological activity evaluation of lignan lactones derived from (â)-cubebin Fulltext Access 5 Pages 2005
Synthesis of mono-glucose-branched cyclodextrins with a high inclusion ability for doxorubicin and their efficient glycosylation using Mucor hiemalis endo-β-N-acetylglucosaminidase Fulltext Access 5 Pages 2005
Identification of nonpeptidic small-molecule inhibitors of interleukin-2 Fulltext Access 5 Pages 2005
QSAR of estrogen receptor modulators: exploring selectivity requirements for ERα versus ERβ binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters Fulltext Access 5 Pages 2005
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates Fulltext Access 5 Pages 2005
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP Fulltext Access 5 Pages 2005
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors Fulltext Access 5 Pages 2005
The development of potent and selective bisarylmaleimide GSK3 inhibitors Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes Fulltext Access 5 Pages 2005
Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity Fulltext Access 5 Pages 2005
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents Fulltext Access 5 Pages 2005
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist Fulltext Access 5 Pages 2005
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor Fulltext Access 5 Pages 2005
A two-state homology model of the hERG K+ channel: application to ligand binding Fulltext Access 5 Pages 2005
A chromism-based assay (CHROBA) technique for in situ detection of protein kinase activity Fulltext Access 5 Pages 2005
Synthesis and fluorescence studies of thiazole orange tethered onto oligonucleotide: development of a self-contained DNA biosensor on a fiber optic surface Fulltext Access 5 Pages 2005
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands Fulltext Access 5 Pages 2005
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands Fulltext Access 5 Pages 2005
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors Fulltext Access 5 Pages 2005
Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs) Fulltext Access 5 Pages 2005
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor Fulltext Access 5 Pages 2005
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides Fulltext Access 5 Pages 2005
Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design Fulltext Access 5 Pages 2005
Design, synthesis, and biological activity of novel PPARγ ligands based on rosiglitazone and 15d-PGJ2 Fulltext Access 5 Pages 2005
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases Fulltext Access 5 Pages 2005
Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1 Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides Fulltext Access 5 Pages 2005
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors Fulltext Access 5 Pages 2005
Structure-activity relationship study of novel tissue transglutaminase inhibitors Fulltext Access 5 Pages 2005
Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome Fulltext Access 5 Pages 2005
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists Fulltext Access 5 Pages 2005