Identification of metabolites of the tryptase inhibitor CRA-9249: Observation of a metabolite derived from an unexpected hydroxylation pathway Fulltext Access 6 Pages 2006
Synthesis of pyrazoles and isoxazoles as potent αvβ3 receptor antagonists Fulltext Access 6 Pages 2006
Isoquinoline–pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity Fulltext Access 6 Pages 2006
P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors Fulltext Access 6 Pages 2006
Carboxy derivatized glucosamine is a potent inhibitor of matrix metalloproteinase-9 in HT1080 cells Fulltext Access 6 Pages 2006
Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4 Fulltext Access 6 Pages 2006
The discovery of tetrahydrofluorenones as a new class of estrogen receptor β-subtype selective ligands Fulltext Access 6 Pages 2006
DNA sequence recognition by an imidazole-containing isopropyl-substituted thiazole polyamide (thiazotropsin B) Fulltext Access 6 Pages 2006
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity Fulltext Access 6 Pages 2006
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors Fulltext Access 6 Pages 2006
Discovery and SAR of oxindole–pyridine-based protein kinase B/Akt inhibitors for treating cancers Fulltext Access 6 Pages 2006
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N′-bis[2-oxo-2H-benzopyran]-3-carboxamides Fulltext Access 6 Pages 2006
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: Preparation of FXR and PPAR ligands Fulltext Access 6 Pages 2006
Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors Fulltext Access 6 Pages 2006
P2–P4 Macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease Fulltext Access 6 Pages 2006
N-Acylated sulfonamide sodium salt: A prodrug of choice for the bifunctional 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamide class of COX-2 inhibitors Fulltext Access 6 Pages 2006
Estrogen receptor β-subtype selective tetrahydrofluorenones: Use of a fused pyrazole as a phenol bioisostere Fulltext Access 6 Pages 2006
Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors Fulltext Access 6 Pages 2006
Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes Fulltext Access 6 Pages 2006
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties Fulltext Access 6 Pages 2006
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors Fulltext Access 6 Pages 2006
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements Fulltext Access 6 Pages 2006
Synthesis and structure–activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists Fulltext Access 6 Pages 2006
Structure–activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists Fulltext Access 6 Pages 2006
Nε-Thioacetyl-lysine: A multi-facet functional probe for enzymatic protein lysine Nε-deacetylation Fulltext Access 6 Pages 2006
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors Fulltext Access 6 Pages 2006
Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogs Fulltext Access 6 Pages 2006
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2) Fulltext Access 6 Pages 2006
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series Fulltext Access 6 Pages 2006
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists Fulltext Access 6 Pages 2006
Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors Fulltext Access 6 Pages 2006
Two novel immunosuppressive pregnane glycosides from the roots of Stephanotis mucronata Fulltext Access 6 Pages 2006
Tubeimoside V (1), a new cyclic bisdesmoside from tubers of Bolbostemma paniculatum, functions by inducing apoptosis in human glioblastoma U87MG cells Fulltext Access 6 Pages 2006
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase Fulltext Access 6 Pages 2006
Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors Fulltext Access 6 Pages 2006
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II ‘selective’ inhibitor celecoxib Fulltext Access 6 Pages 2006
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors Fulltext Access 6 Pages 2006
Synthesis and biological activity of the first cyclic biphalin analogues Fulltext Access 6 Pages 2006
Design, synthesis and structure–activity relationships of new phosphinate inhibitors of MurD Fulltext Access 6 Pages 2006
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors Fulltext Access 6 Pages 2006
Specific volume and compressibility of human serum albumin–polyanion complexes Fulltext Access 6 Pages 2006
Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile Fulltext Access 6 Pages 2006
Flexible synthesis and biological evaluation of novel 5-deoxyadenophorine analogues Fulltext Access 6 Pages 2006
Identification of novel PPARα ligands by the structural modification of a PPARγ ligand Fulltext Access 6 Pages 2006
Design and synthesis of quinolinones as methionyl-tRNA synthetase inhibitors Fulltext Access 6 Pages 2006
Effect of polycyclic cage amines on the transmembrane potential of neuronal cells Fulltext Access 6 Pages 2006
Guanaconetins, new antitumoral acetogenins, mitochondrial complex I and tumor cell growth inhibitors Fulltext Access 6 Pages 2006
Tyrosinase inhibitory cycloartane type triterpenoids from the methanol extract of the whole plant of Amberboa ramosa Jafri and their structure–activity relationship Fulltext Access 6 Pages 2006
Synthesis, in vitro and in vivo antimycobacterial activities of diclofenac acid hydrazones and amides Fulltext Access 6 Pages 2006
Syntheses of glucose analogues of E5564 as a highly potent anti-sepsis drug candidate Fulltext Access 6 Pages 2006
Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines Fulltext Access 6 Pages 2006
Synthesis, metal complexation and biological evaluation of a novel semi-rigid bifunctional chelating agent for 99mTc labelling Fulltext Access 6 Pages 2006
Synthesis and in vivo evaluation of [11C]SN003 as a PET ligand for CRF1 receptors Fulltext Access 6 Pages 2006
Expression of N-terminal Cys-protein fragments using an intein refolding strategy Fulltext Access 6 Pages 2006
Synthesis of a library of polycationic lipid core dendrimers and their evaluation in the delivery of an oligonucleotide with hVEGF inhibition Fulltext Access 6 Pages 2006
Closing in on the AMPA receptor: Synthesis and evaluation of 2-acetyl-1-(4′-chlorophenyl)-6-methoxy-7-[11C]methoxy-1,2,3,4-tetrahydroisoquinoline as a potential PET tracer Fulltext Access 6 Pages 2006
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors Fulltext Access 6 Pages 2006
Synthesis, pulse radiolysis, and in vitro radioprotection studies of melatoninolipoamide, a novel conjugate of melatonin and α-lipoic acid Fulltext Access 6 Pages 2006
Ribokinase from E. coli: Expression, purification, and substrate specificity Fulltext Access 6 Pages 2006
Design of multifunctional peptides expressing both antimicrobial activity and shiga toxin neutralization activity Fulltext Access 6 Pages 2006
A new phenanthrene with a spirolactone from Dendrobium chrysanthum and its anti-inflammatory activities Fulltext Access 6 Pages 2006
A multi-component reaction to 5-cyanouracils: Synthesis and mechanistic study Fulltext Access 6 Pages 2006
Controllable synthesis of polymerizable ester and amide prodrugs of acyclovir by enzyme in organic solvent Fulltext Access 6 Pages 2006
The synthesis and anti-proliferative effects of β-elemene derivatives with mTOR inhibition activity Fulltext Access 6 Pages 2006
Development of affinity chromatography using a bioactive peptide as a ligand Fulltext Access 6 Pages 2006
Anticonvulsant and toxicity evaluation of some 7-alkoxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-ones Fulltext Access 6 Pages 2006
Inhibitors of human mitotic kinesin Eg5: Characterization of the 4-phenyl-tetrahydroisoquinoline lead series Fulltext Access 6 Pages 2006
Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors Fulltext Access 6 Pages 2006
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists Fulltext Access 6 Pages 2006
First dual M3 antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6-diaminopyrimidine derivatives Fulltext Access 6 Pages 2006
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors Fulltext Access 6 Pages 2006
Potent blockers of the monocarboxylate transporter MCT1: Novel immunomodulatory compounds Fulltext Access 6 Pages 2006
Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (−)-dysiherbaine Fulltext Access 6 Pages 2006
Matrix compare analysis discriminates subtle structural differences in a family of novel antiproliferative agents, diaryl-3-hydroxy-2,3,3a,10a-tetrahydrobenzo[b]cycylopenta[e]azepine-4,10(1H,5H)-diones Fulltext Access 6 Pages 2006
Synthesis and antimalarial activities of novel 3,3,6,6-tetraalkyl-1,2,4,5-tetraoxanes Fulltext Access 6 Pages 2006
Synthesis and structure–activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor Fulltext Access 6 Pages 2006
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an α-ketothiazole arginine Fulltext Access 6 Pages 2006
Identification of an indole series of prostaglandin D2 receptor antagonists Fulltext Access 6 Pages 2006
Neuraminidase pharmacophore model derived from diverse classes of inhibitors Fulltext Access 6 Pages 2006
Design, synthesis, and preliminary biological evaluation of 2,3-dihydro-3-hydroxymethyl-1,4-benzoxazine derivatives Fulltext Access 6 Pages 2006
New thioderivatives of gossypol and gossypolone, as prodrugs of cytotoxic agents Fulltext Access 6 Pages 2006