3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: A class of potent DPP-4 inhibitors Fulltext Access 5 Pages 2008
IRAK-4 inhibitors. Part II: A structure-based assessment of imidazo[1,2-a]pyridine binding Fulltext Access 5 Pages 2008
Copper-mediated DNA photocleavage by a tetrapyridoacridine (tpac) ligand Fulltext Access 5 Pages 2008
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents Fulltext Access 5 Pages 2008
Stereospecific deuteration of α-furanosyl azomycin nucleosides: A model reaction for tritium radiolabeling Fulltext Access 5 Pages 2008
Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase Fulltext Access 5 Pages 2008
Structure–activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors Fulltext Access 5 Pages 2008
Verification of the C-terminal intramolecular β-sheet in Aβ42 aggregates using solid-state NMR: Implications for potent neurotoxicity through the formation of radicals Fulltext Access 5 Pages 2008
Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma Fulltext Access 5 Pages 2008
Allosteric inhibitors of Akt1 and Akt2: A naphthyridinone with efficacy in an A2780 tumor xenograft model Fulltext Access 5 Pages 2008
Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase Fulltext Access 5 Pages 2008
Pyridine amides as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 Fulltext Access 5 Pages 2008
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: Application to the discovery of potent niacin receptor agonists Fulltext Access 5 Pages 2008
Indirect oxidation of the antitumor agent procarbazine by tyrosinase—Possible application in designing anti-melanoma prodrugs Fulltext Access 5 Pages 2008
Design, synthesis and in vitro antiprotozoal activity of benzimidazole-pentamidine hybrids Fulltext Access 5 Pages 2008
Identification of acridinyl hydrazides as potent aspartic protease inhibitors Fulltext Access 5 Pages 2008
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor Fulltext Access 5 Pages 2008
A novel pyrene-guanidiniocarbonyl-pyrrole cation efficiently differentiates between ds-DNA and ds-RNA by two independent, sensitive spectroscopic methods Fulltext Access 5 Pages 2008
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity Fulltext Access 5 Pages 2008
New targeting system for antimycotic drugs: β-Glucosidase sensitive Amphotericin B–star poly(ethylene glycol) conjugate Fulltext Access 5 Pages 2008
Conformation–activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity Fulltext Access 5 Pages 2008
Novel 2-imidazoles as potent and selective α1A adrenoceptor partial agonists Fulltext Access 5 Pages 2008
Design and synthesis of tacrine–ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates Fulltext Access 5 Pages 2008
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives Fulltext Access 5 Pages 2008
Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents Fulltext Access 5 Pages 2008
Protective effects of amide constituents from the fruit of Piper chaba on d-galactosamine/TNF-α-induced cell death in mouse hepatocytes Fulltext Access 5 Pages 2008
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein Fulltext Access 5 Pages 2008
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor Fulltext Access 5 Pages 2008
New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity Fulltext Access 5 Pages 2008
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series Fulltext Access 5 Pages 2008
Synthesis and structure–activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists Fulltext Access 5 Pages 2008
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1inhibitors (SHI-1) Fulltext Access 5 Pages 2008
Design and structure–activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): Tetramic, tetronic acids and dihydropyridin-2-ones Fulltext Access 5 Pages 2008
Combinatorial selection of a single stranded DNA thioaptamer targeting TGF-β1 protein Fulltext Access 5 Pages 2008
4-Aminopyrimidine tetrahydronaphthols: A series of novel vanilloid receptor-1 antagonists with improved solubility properties Fulltext Access 5 Pages 2008
Design and synthesis of tetrazole-based growth hormone secretagogue: The SAR studies of the O-benzyl serine side chain Fulltext Access 5 Pages 2008
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series Fulltext Access 5 Pages 2008
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase Fulltext Access 5 Pages 2008
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones Fulltext Access 5 Pages 2008
Phenylcyclobutyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I Fulltext Access 5 Pages 2008
Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs Fulltext Access 5 Pages 2008
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors Fulltext Access 5 Pages 2008
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives Fulltext Access 5 Pages 2008
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity Fulltext Access 5 Pages 2008
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands Fulltext Access 5 Pages 2008
Synthesis, biological evaluation and radiochemical labeling of a dansylhydrazone derivative as a potential imaging agent for apoptosis Fulltext Access 5 Pages 2008
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase Fulltext Access 5 Pages 2008
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone Fulltext Access 5 Pages 2008
Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli Fulltext Access 5 Pages 2008
Discovery of benzamide tetrahydro-4H-carbazol-4-ones as novel small molecule inhibitors of Hsp90 Fulltext Access 5 Pages 2008
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines Fulltext Access 5 Pages 2008
Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases Fulltext Access 5 Pages 2008
Design, synthesis, and antibacterial activities of novel 3,6-bicyclolide oximes: Length optimization and zero carbon linker oximes Fulltext Access 5 Pages 2008
Carbonic anhydrase inhibitors: Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions Fulltext Access 5 Pages 2008
Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives Fulltext Access 5 Pages 2008
Synthesis and biological evaluation of 2-amino-3-(3′,4′,5′-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization Fulltext Access 5 Pages 2008
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor: In vitro and in vivo activity Fulltext Access 5 Pages 2008
1-Benzylbenzimidazoles: The discovery of a novel series of bradykinin B1 receptor antagonists Fulltext Access 5 Pages 2008
Design, syntheses, and structure–activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives Fulltext Access 5 Pages 2008
Syntheses and structure–activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists Fulltext Access 5 Pages 2008
Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening Fulltext Access 5 Pages 2008
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists Fulltext Access 5 Pages 2008
Synthesis and antiviral properties of some polyphenols related to Salvia genus Fulltext Access 5 Pages 2008
Allosteric FBPase inhibitors gain 105 times in potency when simultaneously binding two neighboring AMP sites Fulltext Access 5 Pages 2008
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines Fulltext Access 5 Pages 2008
Structure–activity relationship studies of the chromosome segregation inhibitor, Incentrom A Fulltext Access 5 Pages 2008
Structure–activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors Fulltext Access 5 Pages 2008
Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin Fulltext Access 5 Pages 2008
Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties Fulltext Access 5 Pages 2008
Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase Fulltext Access 5 Pages 2008
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases Fulltext Access 5 Pages 2008
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines Fulltext Access 5 Pages 2008
In silico multi-filter screening approaches for developing novel β-secretase inhibitors Fulltext Access 5 Pages 2008
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode Fulltext Access 5 Pages 2008
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes Fulltext Access 5 Pages 2008
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity Fulltext Access 5 Pages 2008
Effects of the aryl linker and the aromatic substituent on the anti-HCV activities of aryl diketoacid (ADK) analogues Fulltext Access 5 Pages 2008
Design and synthesis of regioisomerically pure unsymmetrical xanthene derivatives for staining live cells and their photochemical properties Fulltext Access 5 Pages 2008
Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria Fulltext Access 5 Pages 2008
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity Fulltext Access 5 Pages 2008
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064 Fulltext Access 5 Pages 2008
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase Fulltext Access 5 Pages 2008
Carbonic anhydrase activators: Activation of the human cytosolic isozyme III and membrane-associated isoform IV with amino acids and amines Fulltext Access 5 Pages 2008
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors Fulltext Access 5 Pages 2008
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies Fulltext Access 5 Pages 2008
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the κ opioid receptor Fulltext Access 5 Pages 2008
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment Fulltext Access 5 Pages 2008