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Daneshyari Pharmaceutical Science Journas Latest Articles

Pharmaceutical Science Research Articles

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
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Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists
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
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Discovery and SAR of oxindole–pyridine-based protein kinase B/Akt inhibitors for treating cancers
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Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N′-bis[2-oxo-2H-benzopyran]-3-carboxamides
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Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: Preparation of FXR and PPAR ligands
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Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors
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P2–P4 Macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease
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Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors
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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
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Newly discovered orally active pure antiestrogens
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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
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Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3
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Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes
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Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
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Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors
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Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements
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Synthesis and structure–activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists
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Structure–activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists
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Nε-Thioacetyl-lysine: A multi-facet functional probe for enzymatic protein lysine Nε-deacetylation
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Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors
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Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogs
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Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2)
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Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series
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Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists
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Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors
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Two novel immunosuppressive pregnane glycosides from the roots of Stephanotis mucronata
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Tubeimoside V (1), a new cyclic bisdesmoside from tubers of Bolbostemma paniculatum, functions by inducing apoptosis in human glioblastoma U87MG cells
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Modification of the clozapine structure by parallel synthesis
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Discovery of orally active butyrolactam 11β-HSD1 inhibitors
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Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase
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Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors
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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
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Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors
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Synthesis and biological activity of the first cyclic biphalin analogues
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Design, synthesis and structure–activity relationships of new phosphinate inhibitors of MurD
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Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors
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Specific volume and compressibility of human serum albumin–polyanion complexes
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Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile
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Flexible synthesis and biological evaluation of novel 5-deoxyadenophorine analogues
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Identification of novel PPARα ligands by the structural modification of a PPARγ ligand
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Design and synthesis of quinolinones as methionyl-tRNA synthetase inhibitors
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Effect of polycyclic cage amines on the transmembrane potential of neuronal cells
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Guanaconetins, new antitumoral acetogenins, mitochondrial complex I and tumor cell growth inhibitors
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Tyrosinase inhibitory cycloartane type triterpenoids from the methanol extract of the whole plant of Amberboa ramosa Jafri and their structure–activity relationship
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Synthesis, in vitro and in vivo antimycobacterial activities of diclofenac acid hydrazones and amides
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Syntheses of glucose analogues of E5564 as a highly potent anti-sepsis drug candidate
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The reaction of artemisinins with hemoglobin: A unified picture
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Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines
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Synthesis, metal complexation and biological evaluation of a novel semi-rigid bifunctional chelating agent for 99mTc labelling
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Synthesis and in vivo evaluation of [11C]SN003 as a PET ligand for CRF1 receptors
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Expression of N-terminal Cys-protein fragments using an intein refolding strategy
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Synthesis of a library of polycationic lipid core dendrimers and their evaluation in the delivery of an oligonucleotide with hVEGF inhibition
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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
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Synthesis, pulse radiolysis, and in vitro radioprotection studies of melatoninolipoamide, a novel conjugate of melatonin and α-lipoic acid
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Ribokinase from E. coli: Expression, purification, and substrate specificity
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Practical syntheses of dyes for difference gel electrophoresis
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Design of multifunctional peptides expressing both antimicrobial activity and shiga toxin neutralization activity
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A new phenanthrene with a spirolactone from Dendrobium chrysanthum and its anti-inflammatory activities
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A multi-component reaction to 5-cyanouracils: Synthesis and mechanistic study
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Controllable synthesis of polymerizable ester and amide prodrugs of acyclovir by enzyme in organic solvent
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Benzofuro[3,2-f][1]benzopyrans: A new class of antitubercular agents
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The synthesis and anti-proliferative effects of β-elemene derivatives with mTOR inhibition activity
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Development of affinity chromatography using a bioactive peptide as a ligand
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Anticonvulsant and toxicity evaluation of some 7-alkoxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-ones
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Inhibitors of human mitotic kinesin Eg5: Characterization of the 4-phenyl-tetrahydroisoquinoline lead series
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Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors
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Inhibitory effect of carboxylic acid group on hERG binding
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Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
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Synthesis and stability of two indomethacin prodrugs
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Synthesis and activity of small molecule GPR40 agonists
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First dual M3 antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6-diaminopyrimidine derivatives
Fulltext Access 6 Pages 2006
QSAR study of mosquito repellents using Codessa Pro
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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
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Synthesis and anticancer activity of thiosemicarbazones
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
Dipeptide nitrile inhibitors of cathepsin K
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4-Amino derivatives of the Hsp90 inhibitor CCT018159
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Synthesis and structure–activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor
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SAR studies: Designing potent and selective LXR agonists
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Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an α-ketothiazole arginine
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Identification of an indole series of prostaglandin D2 receptor antagonists
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Neuraminidase pharmacophore model derived from diverse classes of inhibitors
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Novel cisplatin-type platinum complexes and their cytotoxic activity
Fulltext Access 6 Pages 2006
Keto-1,3,4-oxadiazoles as cathepsin K 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
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