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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

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Fulltext Access 10 Pages 2006
Short pseudopeptides containing turn scaffolds with high AT2 receptor affinity
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Synthesis and biological evaluation of carboacyclic nucleosides with (Z) and (E)-9-[4,4-bis(hydroxymethyl)]-2-butenyl side chain
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Synthesis of 1-O-monoacyl or 12-O-monoacyl, 1-,12-O-diacyl-, and 11,12-dehydrated excisanin A 7,14-acetonides and their cytotoxic activity
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Carbonic anhydrase inhibitors: Transepithelial transport of thioureido sulfonamide inhibitors of the cancer-associated isozyme IX is dependent on efflux transporters
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Synthesis of new bioactive venlafaxine analogs: Novel thiazolidin-4-ones as antimicrobials
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Effect of cholesterol on DMPC phospholipid membranes and QSAR model construction in membrane-interaction QSAR study through molecular dynamics simulation
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Synthesis and biological evaluation of new dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted with various saturated and unsaturated side chains via palladium catalyzed cross-coupling reactions
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N-Thiolated β-lactam antibacterials: Effects of the N-organothio substituent on anti-MRSA activity
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Hydroxyl-terminated peptidomimetic inhibitors of neuronal nitric oxide synthase
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[(S)-γ-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors
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Comparative structure–activity relationships of benztropine analogues at the dopamine transporter and histamine H1 receptors
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Synthesis, characterization, and DNA-binding properties of the Ln(III) complexes with 6-hydroxy chromone-3-carbaldehyde-(2′-hydroxy) benzoyl hydrazone
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Novel 2-substituted nitronyl nitroxides as free radical scavengers: Synthesis, biological evaluation and structure–activity relationship
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Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists
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Antitumor agents 251: Synthesis, cytotoxic evaluation, and structure–activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents
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Structure–activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416
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Phosphatidylinositol mannosides: Synthesis and adjuvant properties of phosphatidylinositol di- and tetramannosides
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Synthesis and receptor binding studies of halogenated N,N-dialkylel-(2-phenyl-1H-indol-3-yl)glyoxylamides to visualize peripheral benzodiazepine receptors with SPECT or PET
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Synthesis, characterization, and anti-bacterial efficacy of some novel cyclophane amide
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Synthesis and biological evaluation of deoxy salacinols, the role of polar substituents in the side chain on the α-glucosidase inhibitory activity
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DNA binding potential and cytotoxicity of newly designed pyrrolobenzodiazepine dimers linked through a piperazine side-armed-alkane spacer
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Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum
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Enaminones 9. Further studies on the anticonvulsant activity and potential type IV phosphodiesterase inhibitory activity of substituted vinylic benzamides
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Parallel synthesis of modular chiral Schiff base ligands and evaluation in the titatium(IV) catalyzed asymmetric trimethylsilylcyanation of aldehydes
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Synthesis of linear and cyclic homo-β-peptides based on a binaphthylic β-amino acid with only axial chirality
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Preparation and biological activity of 6-benzylaminopurine derivatives in plants and human cancer cells
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3D-QSAR study of ring-substituted quinoline class of anti-tuberculosis agents
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Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry
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Design, synthesis, and antifungal activity of inhibitors of brassilexin detoxification in the plant pathogenic fungus Leptosphaeria maculans
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Putative drug binding conformations of monoamine transporters
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Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cells
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Molecular modeling and 3D-QSAR studies of indolomorphinan derivatives as kappa opioid antagonists
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Induction of apoptosis in HeLa cells by 3β-hydroxy-12-oleanen-27-oic acid from the rhizomes of Astilbe chinensis
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Combination of porphyrins and DNA-alkylation agents: Synthesis and tumor cell apoptosis induction
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Synthesis and properties of 2′-O,4′-C-methyleneoxymethylene bridged nucleic acid
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2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands
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Versatile synthesis and biological evaluation of 1,3-diamino-substituted 1α,25-dihydroxyvitamin D3 analogues
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Synthesis, molecular modelling and enzymatic evaluation of (±)3,5-diphenyl-2-thioxoimidazolidin-4-ones as new potential cyclooxygenase inhibitors
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Dicationic pyridium porphyrins appending different peripheral substituents: Synthesis and studies for their interactions with DNA
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Structure basis for the inhibitory mechanism of a novel DNase γ-specific inhibitor, DR396
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Tetrahydropyrrolo[3,2-c]azepin-4-ones as a new class of cytotoxic compounds
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The application of a 3D-QSAR (autoMEP/PLS) approach as an efficient pharmacodynamic-driven filtering method for small-sized virtual library: Application to a lead optimization of a human A3 adenosine receptor antagonist
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Structure–activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists
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Synthesis, reactions and structure–activity relationships of 1-hydroxyspiro[2.5]cyclooct-4-en-3-ones: Illudin analogs with in vitro cytotoxic activity
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Luminescent pyrimidine hydrazide oligomers with peptide affinity
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QSAR analysis of antimicrobial and haemolytic effects of cyclic cationic antimicrobial peptides derived from protegrin-1
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The binding of 3′-N-piperidine-4-carboxyl-3′-deoxy-ara-uridine to ribonuclease A in the crystal
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Biotinylated biphenyl ketone-containing 2,4-dioxobutanoic acids designed as HIV-1 integrase photoaffinity ligands
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Synthesis and SAR studies of a novel series of T-type calcium channel blockers
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Fluorescent intercalator displacement analyses of DNA binding by the peptide-derived natural products netropsin, actinomycin, and bleomycin
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Essential structural profile of a dual functional inhibitor against cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX): Molecular docking and 3D-QSAR analyses on DHDMBF analogues
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Carbonyl- and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases
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Fragment-based drug discovery of carbonic anhydrase II inhibitors by dynamic combinatorial chemistry utilizing alkene cross metathesis
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High-mannose-type glycan modifications of dihydrofolate reductase using glycan–methotrexate conjugates
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Total syntheses of three copper (II) tetracarboranylphenylporphyrins containing 40 or 80 boron atoms and their biological properties in EMT-6 tumor-bearing mice
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Graphical contents list
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Biochemical and functional characterization of an l-amino acid oxidase isolated from Bothrops pirajai snake venom
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Synthesis of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl carbamate analogs as σ2 receptor ligands
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Structure-activity relationships in nitrothiophenes
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Synthesis of dopamine transporter selective 3-diarylmethoxymethyl-8-arylalkyl-8-azabicyclo[3.2.1]octane derivatives
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Inhibition of monoamine oxidase B by analogues of the adenosine A2A receptor antagonist (E)-8-(3-chlorostyryl)caffeine (CSC)
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Synthesis of 2,4,6-trisubstituted pyrimidine and triazine heterocycles as antileishmanial agents
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Synthesis and transdermal permeation-enhancing activity of carbonate and carbamate analogs of Transkarbam 12
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Synthesis and effects of 3-methylthiopropanoyl thiolesters of lipoic acid, methional metabolite mimics
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Reaction of acrolein with 2′-deoxyadenosine and 9-ethyladenine-Formation of cyclic adducts
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Synthesis, structure, and hydrolytic reaction of trans-dichlorobis(diethanolamine-N)palladium(II) with N-acetylated L-histidylglycine dipeptide
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Synthesis and differential antiproliferative activity of Biginelli compounds against cancer cell lines: Monastrol, oxo-monastrol and oxygenated analogues
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A convenient route to enantiomerically pure, conjugated dienes from sugar allyltin derivatives
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The preparation of new enantiopure imidazolinium salts and their evaluation as catalysts and shift reagents
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Screening, substrate specificity and stereoselectivity of yeast strains, which reduce sterically hindered isopropyl ketones
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Reversing Dane’s strategy: a new, concise, enantioselective synthesis of the steroid nucleus
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Biocatalytic preparation of optically active 4-(N,N-dimethylamino)pyridines for application in chemical asymmetric catalysis
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A modelling study of a non-concerted hydrolytic cycloaddition reaction by the catalytic antibody H11
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Synthesis of 26,27-bisnorcastasterone analogs and analysis of conformation–activity relationship for brassinolide-like activity
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The development of 3D-QSAR study and recursive partitioning of heterocyclic quinone derivatives with antifungal activity
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Inactivation of bovine plasma amine oxidase by haloallylamines
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Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands
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Graphical contents list
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Synthesis of multisubstituted quinolines from Baylis–Hillman adducts obtained from substituted 2-chloronicotinaldehydes and their antimicrobial activity
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Antioxidant activity of β-blockers: An effect mediated by scavenging reactive oxygen and nitrogen species?
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Graphical contents list
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Novel cyano- and amidino-substituted derivatives of thieno[2,3-b]- and thieno[3,2-b]thiophene-2-carboxanilides and thieno[3′,2′:4,5]thieno- and thieno[2′,3′:4,5]thieno [2,3-c]quinolones: Synthesis, photochemical synthesis, DNA binding, and antitumor evalu
Fulltext Access 10 Pages 2006
Synthesis and in vitro evaluation of pseudosaccharinamine derivatives as potential elastase inhibitors
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QSAR models for Daphnia toxicity of pesticides based on combinations of topological parameters of molecular structures
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Synthesis of verbenachalcone congeners and their biological assessment against activation of the NGF-mediated neurite outgrowth of PC12D cells’ activity
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Preparation of N-phenyl-(S)-prolinol-derived P,N-ligands and their application in Pd-catalyzed asymmetric allylic alkylation
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Fluorescein-based amino acids for solid phase synthesis of fluorogenic protease substrates
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Synthesis and appetite suppressant activity of 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes as conformationally rigid analogues of fluoxetine
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New cytotoxic furoquinones obtained from terpenyl-1,4-naphthoquinones and 1,4-anthracenediones
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Synthesis of novel 5-substituted indirubins as protein kinases inhibitors
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Boc-lysinated-betulonic acid: A potent, anti-prostate cancer agent
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N-Terminal amino acid side-chain cleavage of chemically modified peptides in the gas phase: A mass spectrometry technique for N-terminus identification
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Polycationic lipophilic-core dendrons as penetration enhancers for the oral administration of low molecular weight heparin
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Synthesis, antiplatelet and antithrombotic activities of new 2-substituted benzopyrano[4,3-d]pyrimidin-4-cycloamines and 4-amino/cycloamino-benzopyrano[4,3-d]pyrimidin-5-ones
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Optimizing phenylethylphosphonamidates for the inhibition of prostate-specific membrane antigen
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Structural and functional characterization of human microsomal prostaglandin E synthase-1 by computational modeling and site-directed mutagenesis
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Aponeocarzinostatin-A superior drug carrier exhibiting unusually high endurance against denaturants
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