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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives
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Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic
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The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists
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Interaction of dopamine and acetylcholine with an amphiphilic resorcinarene receptor in aqueous micelle system
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Ab initio studies of the properties of intracellular thiols ergothioneine and ovothiol
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Biaryls and heterobiaryls as α-glucosidase and protein tyrosine phosphatase inhibitors
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Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors
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The discovery and synthesis of novel adenosine receptor (A2A) antagonists
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Synthesis and biological activity of new 5-O-sugar modified ketolide and 2-fluoro-ketolide antibiotics
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Synthesis and radiopharmacological evaluation of 2′-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11β,17α-dihydroxy-pregn-4-eno[3,2-c]pyrazole as potential glucocorticoid receptor ligand for positron emission tomography (PET)
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Functionalized dendrimers as endotoxin sponges
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Amino acid conjugates as κ opioid receptor agonists
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Instructions to Authors
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Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors
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Novel 1β-methylcarbapenems with isoxazoloethenyl moieties containing carboxylic acid sodium salt
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A new class of androgen receptor antagonists bearing carborane in place of a steroidal skeleton
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2,3-Diphenylpropionic acids as potent VLA-4 antagonists
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Himeic acid A: a new ubiquitin-activating enzyme inhibitor isolated from a marine-derived fungus, Aspergillus sp.
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Design, synthesis, and biological evaluation of achiral analogs of duocarmycin SA
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Efficient cleavage of RNA, enhanced cellular uptake, and controlled intracellular localization of conjugate DNAzymes
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Cytotoxic neolignans: an SAR study
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Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase
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Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5α-reductases 1 and 2
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New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties
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Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core
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In vivo incorporation of an alkyne into proteins in Escherichia coli
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Design and synthesis of a peptide-PEG transporter tool for carrying adenovirus vector into cells
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Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives
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The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma
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Studies on the structure-activity relationship of 2′,6′-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH3
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Generation of a new class of hNK2 receptor ligands using the 'fragment approach'
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Synthesis of modified proanthocyanidins: easy and general introduction of a hydroxy group at C-6 of catechin; efficient synthesis of elephantorrhizol
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Synthesis of modified proanthocyanidins: introduction of acyl substituents at C-8 of catechin. Selective synthesis of a C-4 → O → C-3 ether-linked procyanidin-like dimer
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Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists
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Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B
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Enantiomerical excess determination, purification and biological evaluation of (3S) and (3R) α,β-butenolide analogues of isobenzofuranone
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2-Mercaptoimidazoles, a new class of potent CCR2 antagonists
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Instructions to contributors
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Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase
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Glucokinase-activating ureas
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Structure-activity relationships of dimeric PPAR agonists
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Synthesis and evaluation of diverse analogs of amygdalin as potential peptidomimetics of peptide T
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Aglycon specificity profiling of α-glucosidases using synthetic probes
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2-Substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist
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Crystal structures of human HSP90α-complexed with dihydroxyphenylpyrazoles
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Electronic structure calculations on the thiazole-containing antibiotic thiostrepton: molecular mechanics, semi-empirical and ab initio analyses
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Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity
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Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor α/β agonist scaffold
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Protein microarray using α-amino acids as metal tags on chips
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4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands
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Novel fluoroquinolones: design, synthesis, and in vivo activity in mice against Mycobacterium tuberculosis H37Rv
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3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis
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Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture
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Instructions to contributors
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Antitubercular agents. Part 1: Synthesis of phthalimido- and naphthalimido-linked phenazines as new prototype antitubercular agents
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Molecular-modeling based design, synthesis, and activity of substituted piperidines as γ-secretase inhibitors
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Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents
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Synthesis of 15R-PGD2: a potential DP2 receptor agonist
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Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2
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Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists
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Asymmetric synthesis of novel tetrahydroquinoline derivatives with a sugar building block and their bioactivities
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Enhancement in antimicrobial activity of 2-(phenyl)-3-(2-butyl-4-chloro-1H-imidazolyl)-5-butylate isoxazolidine
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Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14
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Novel cyclized Pifithrin-α p53 inactivators: synthesis and biological studies
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Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues
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Structure-activity relationships of the oxindole growth hormone secretagogues
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Quinolinium salt as a potent inhibitor of lymphocyte apoptosis
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Novel 2-aminothiazonaphthalimides as visible light activatable photonucleases: effects of intercalation, heterocyclic-fused area and side chains
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Instructions to contributors
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N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
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Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists
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Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors
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1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1
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7α,11β-Dimethyl-19-nortestosterone: a potent and selective androgen response modulator with prostate-sparing properties
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Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists
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Synthesis and characterization of a carboranyl-tetrabenzoporphyrin
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Amide derivatives of 9,11-seco-estra-1,3,5(10)-trien-11-oic acid as modified orally active estrogen agonists with moderate antagonistic activity
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Characterization of l-glutamine:2-deoxy-scyllo-inosose aminotransferase (tbmB) from Streptomyces tenebrarius
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Optimization of pyrrolidinone based HIV protease inhibitors
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Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials
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2,3-Ethylene- and 2,3-trimethylene-bridged analogues of the group III metabotropic glutamate receptor ligand 2-amino-4-phosphonobutanoic acid
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Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors
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Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas
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A new strategy to combat Alzheimer's disease. Combining radical-scavenging potential with metal-protein-attenuating ability in one molecule
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Instructions to contributors
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From a total synthesis of cepabactin and its 3:1 ferric complex to the isolation of a 1:1:1 mixed complex between iron (III), cepabactin and pyochelin
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Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification
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Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates
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Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
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Nonpeptide αvβ3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics
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3-(2,5-Dihydro-1H-pyrrol-2-ylmethoxy)pyridines: synthesis and analgesic activity
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3-Arylidene-1-(4-nitrophenylmethylene)-3,4-dihydro-1H-naphthalen-2-ones and related compounds displaying selective toxicity and reversal of multidrug resistance in neoplastic cells
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Synthesis and activity of oleanolic acid derivatives, a novel class of inhibitors of osteoclast formation
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The stability of lipidic analogues of GnRH in plasma and kidney preparations: the stereoselective release of the parent peptide
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Inositol tripyrophosphate: a new membrane permeant allosteric effector of haemoglobin
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Cyclization-activated prodrugs. Synthesis, reactivity and toxicity of dipeptide esters of paracetamol
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Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents: parallel synthesis for lead optimization of amide region
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Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)
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Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide
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Synthesis of isonicotinic acid N′-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents
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