Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3 Fulltext Access 5 Pages 2005
Effects of linking 15-zinc finger domains on DNA binding specificity and multiple DNA binding modes Fulltext Access 5 Pages 2005
Structure–activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption Fulltext Access 5 Pages 2005
Induction of apoptosis by a novel indirubin-5-nitro-3′-monoxime, a CDK inhibitor, in human lung cancer cells Fulltext Access 5 Pages 2005
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series Fulltext Access 5 Pages 2005
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain Fulltext Access 5 Pages 2005
Ketoheterocycle-based inhibitors of cathepsin K: A novel entry into the synthesis of peptidic ketoheterocycles Fulltext Access 5 Pages 2005
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors Fulltext Access 5 Pages 2005
Radiosynthesis of carbon-11-labeled camptothecin derivatives as potential positron emission tomography tracers for imaging of topoisomerase I in cancers Fulltext Access 5 Pages 2005
Synthesis of an N-acyl sulfamate analog of luciferyl-AMP: A stable and potent inhibitor of firefly luciferase Fulltext Access 5 Pages 2005
SAR and biological evaluation of novel trans-3,4-dimethyl-4-arylpiperidine derivatives as opioid antagonists Fulltext Access 5 Pages 2005
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series Fulltext Access 5 Pages 2005
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors Fulltext Access 5 Pages 2005
Synthesis of doxorubicin–peptide conjugate with multidrug resistant tumor cell killing activity Fulltext Access 5 Pages 2005
Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2″-hydroxy naphthalen-1″-yl)-1,5-diphenyl-2-pyrazolines Fulltext Access 5 Pages 2005
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor Fulltext Access 5 Pages 2005
High affinity iron(III) scavenging by a novel hexadentate 3-hydroxypyridin-4-one-based dendrimer: Synthesis and characterization Fulltext Access 5 Pages 2005
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists Fulltext Access 5 Pages 2005
Pentacyclic triterpenes. Part 1: The first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases Fulltext Access 5 Pages 2005
Bis(indole) alkaloids as sortase A inhibitors from the sponge Spongosorites sp. Fulltext Access 5 Pages 2005
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides Fulltext Access 5 Pages 2005
Synthesis and anthelmintic activity of 7-substituted 3,4a-dimethyl-4a,5a,8a,8b-tetrahydro-6H-pyrrolo[3â²,4â²:4,5]furo[3,2-b]pyridine-6,8(7H)-diones Fulltext Access 5 Pages 2005
Chemical modification of the naphthoyl 3-position of JWH-015: In search of a fluorescent probe to the cannabinoid CB2 receptor Fulltext Access 5 Pages 2005
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands Fulltext Access 5 Pages 2005
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. Part 3: Chemical derivatization Fulltext Access 5 Pages 2005
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives Fulltext Access 5 Pages 2005
Functionalized head-to-head hairpin polyamides: Synthesis, double-stranded DNA-binding activity and affinity Fulltext Access 5 Pages 2005
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis Fulltext Access 5 Pages 2005
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1 Fulltext Access 5 Pages 2005
4-Fluorosulfonylpiperidines: Selective 5-HT2A ligands for the treatment of insomnia Fulltext Access 5 Pages 2005
Synthesis and bioactivities of two multiple antigen peptides as potential vaccine against schistosoma Fulltext Access 5 Pages 2005
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production Fulltext Access 5 Pages 2005
3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2) Fulltext Access 5 Pages 2005
Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes Fulltext Access 5 Pages 2005
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED Fulltext Access 5 Pages 2005
Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives Fulltext Access 5 Pages 2005
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase Fulltext Access 5 Pages 2005
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor Fulltext Access 5 Pages 2005
The development of monocyclic pyrazolone based cytokine synthesis inhibitors Fulltext Access 5 Pages 2005
Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure–activity relationships Fulltext Access 5 Pages 2005
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives Fulltext Access 5 Pages 2005
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor Fulltext Access 5 Pages 2005
Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain Fulltext Access 5 Pages 2005
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action Fulltext Access 5 Pages 2005
A structural screening approach to ketoamide-based inhibitors of cathepsin K Fulltext Access 5 Pages 2005
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains Fulltext Access 5 Pages 2005
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors Fulltext Access 5 Pages 2005
A practical molecular clip for immobilization of receptors and biomolecules on devices’ surface: Synthesis, grafting protocol and analytical assay Fulltext Access 5 Pages 2005
Sialyl Lewisx analogs based on a quinic acid scaffold as the fucose mimic Fulltext Access 5 Pages 2005
Design, synthesis, and evaluation of dioxane-based antiviral agents targeted against the Sindbis virus capsid protein Fulltext Access 5 Pages 2005
Estrogen receptor β selective ligands: Discovery and SAR of novel heterocyclic ligands Fulltext Access 5 Pages 2005
A novel one-pot three-component reaction: Synthesis of triheterocyclic 4H-pyrimido[2,1-b]benzazoles ring systems Fulltext Access 5 Pages 2005
Antioxidant and cytotoxic activities of xanthones from Cudrania tricuspidata Fulltext Access 5 Pages 2005
Cyclohexyl-linked tricyclic isoxazoles are potent and selective modulators of the multidrug resistance protein (MRP1) Fulltext Access 5 Pages 2005
Molecular docking and 3D-QSAR on 2-(oxalylamino) benzoic acid and its analogues as protein tyrosine phosphatase 1B inhibitors Fulltext Access 5 Pages 2005
Preparation of human Melanocortin-4 receptor agonist libraries: Linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2 Fulltext Access 5 Pages 2005
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: Orally active prostacyclin mimetics. Part 2 Fulltext Access 5 Pages 2005
Toll-like receptor 2 antagonists. Part 1: Preliminary SAR investigation of novel synthetic phospholipids Fulltext Access 5 Pages 2005
Synthesis and antimicrobial activity of 5-hydroxymethyl- 8-methyl-2-(N-arylimino)-pyrano[2,3-c]pyridine-3-(N-aryl)-carboxamides Fulltext Access 5 Pages 2005
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists Fulltext Access 5 Pages 2005
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1β converting enzyme inhibitors Fulltext Access 5 Pages 2005
Synthesis and structure–activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II Fulltext Access 5 Pages 2005
Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones Fulltext Access 5 Pages 2005
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands Fulltext Access 5 Pages 2005
Selection of 5′-untranslated sequences that enhance initiation of translation in a cell-free protein synthesis system from wheat embryos Fulltext Access 5 Pages 2005
Synthesis and in vitro anti-hepatitis B and C virus activities of ring-expanded ('fat') nucleobase analogues containing the imidazo[4,5-e][1,3]diazepine-4,8-dione ring system Fulltext Access 5 Pages 2005
Photoisomerization as a trigger for Bergman cyclization: Synthesis and reactivity of azoenediynes Fulltext Access 5 Pages 2005
Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates Fulltext Access 5 Pages 2005
Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): Efficacy in an animal model for schizophrenia Fulltext Access 5 Pages 2005
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles Fulltext Access 5 Pages 2005
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry Fulltext Access 5 Pages 2005
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain Fulltext Access 5 Pages 2005
Discovery of selective aldo-keto reductase ligands—an on-bead assay strategy Fulltext Access 5 Pages 2005
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity Fulltext Access 5 Pages 2005
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors Fulltext Access 5 Pages 2005
Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes Fulltext Access 5 Pages 2005
Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5) Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of sulfonamidooxazoles and β-keto sulfones: selective inhibitors of 11β-hydroxysteroid dehydrogenase type I Fulltext Access 5 Pages 2005
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization Fulltext Access 5 Pages 2005
Factors affecting the protease activity of venom from jellyfish Rhopilema esculentum Kishinouye Fulltext Access 5 Pages 2005
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters Fulltext Access 5 Pages 2005
Design, synthesis, and evaluation of proline based melanocortin receptor ligands Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors Fulltext Access 5 Pages 2005
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives Fulltext Access 5 Pages 2005
Decrease in the particle size of low-density lipoprotein (LDL) by oxidation Fulltext Access 5 Pages 2005
New cytotoxic bisindole alkaloids with protein tyrosine kinase inhibitory activity from a myxomycete Lycogala epidendrum Fulltext Access 5 Pages 2005
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold Fulltext Access 5 Pages 2005
Synthesis of all-trans arachidonic acid and its effect on rabbit platelet aggregation Fulltext Access 5 Pages 2005
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2) Fulltext Access 5 Pages 2005
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: Toward agents for boron neutron capture therapy of hypoxic tumo Fulltext Access 5 Pages 2005