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Daneshyari Pharmaceutical Science Journas Latest Articles

Pharmaceutical Science Research Articles

Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S
Fulltext Access 5 Pages 2007
Design and synthesis of novel prodrugs of 2′-deoxy-2′-methylidenecytidine activated by membrane dipeptidase overexpressed in tumor tissues
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Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3
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SAR studies on a novel series of human cytomegalovirus primase inhibitors
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Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1)
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Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: Synthesis and biological evaluation
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Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at μ and δ opioid receptors
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3D-QSAR studies with the aid of molecular docking for a series of non-steroidal FXR agonists
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Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors
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Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors
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Bridged androstenediol analogs as ER-β selective SERMs
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Geldanamycin derivatives and neuroprotective effect on cultured P19-derived neurons
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Cell differentiation enhancement by hydrophilic derivatives of 4,8-Dihydrobenzo[1,2-b:5,4-b′]dithiophene-4,8-diones in HL-60 leukemia cells
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Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: Development of an expedient and divergent synthetic route and preliminary SAR
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Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: Evaluation of novel conjugates as cytotoxic agents
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Design and evaluation of ‘Linkerless’ hydroxamic acids as selective HDAC8 inhibitors
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PDE-10A inhibitors as insulin secretagogues
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Pyrazolo[1,5-a]pyridine antiherpetics: Effects of the C3 substituent on antiviral activity
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Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel
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Hybrid molecules containing benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and α-bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukaemia cells
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Preparation of novel anthranilic acids as antibacterial agents. Extensive evaluation of alternative amide bioisosteres connecting the A- and the B-rings
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Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization
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Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity
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Evaluation of N-(phenylmethyl)-4-[5-(phenylmethyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-4-yl]benzamide inhibitors of Mycobacterium tuberculosis growth
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Imidazo[1,2-a]pyridines with potent activity against herpesviruses
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Different protein-binding selectivities for N-acyl heparin derivatives having N-phenylacetyl and heterocycle analogs of N-phenylacetyl substituted in place of N-sulfo groups
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Novel thiazolones as HCV NS5B polymerase allosteric inhibitors: Further designs, SAR, and X-ray complex structure
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Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists
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Analogues of 2-crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxycyclohex-2-enone (COTC) with anti-tumor properties
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Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER
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New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases
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Phenylalanyl-aminocyclophosphamides as model prodrugs for proteolytic activation: Synthesis, stability, and stereochemical requirements for enzymatic cleavage
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Structure–activity relationships of novel non-competitive mGluR1 antagonists: A potential treatment for chronic pain
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Synthesis and biological evaluation of novel T-type calcium channel blockers
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Construction of saccharide-modified DNAs by DNA polymerase
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Continuing efforts on the improvement of Beckmann rearrangement of indanone oxime
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Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators
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Thioimidoyl furanosides as first inhibitors of the α-l-arabinofuranosidase AbfD3
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Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: Synthesis and preliminary SAR analysis
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Development of a novel therapeutic suppressor of brain proinflammatory cytokine up-regulation that attenuates synaptic dysfunction and behavioral deficits
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The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain
Fulltext Access 5 Pages 2007
Novel β-lactam derivatives: Potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome
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N/C-4 substituted azetidin-2-ones: Synthesis and preliminary evaluation as new class of antimicrobial agents
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Synthesis of carbon-11 labeled sulfonanilide analogues as new potential PET agents for imaging of aromatase in breast cancer
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α-Methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands
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Synthesis and biological activity of 5-aza-ellipticine derivatives
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Synthesis and antitumor properties of 2,5-bis(3′-indolyl)thiophenes: Analogues of marine alkaloid nortopsentin
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Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics
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Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R)
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Discovery of tertiary aminoacids as dual PPARα/γ agonists-I
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Design and synthesis of bioactive adamantane spiro heterocycles
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Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists
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Biaryl cannabinoid mimetics—Synthesis and structure–activity relationship
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Himbacine derived thrombin receptor antagonists: Discovery of a new tricyclic core
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Paclitaxel C-10 carbamates: Potential candidates for the treatment of neurodegenerative tauopathies
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Novel potent antimitotic heterocyclic ketones: Synthesis, antiproliferative activity, and structure–activity relationships
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Bradykinin B1 antagonists: Biphenyl SAR studies in the cyclopropanecarboxamide series
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Evaluation of 4′-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5α-reductase
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Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 2: Structure–activity relationship studies on the benzopyran scaffold
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Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling
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Antifungal activity in triterpene glycosides from the sea cucumber Actinopyga lecanora
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Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma
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Indanylacetic acids as PPAR-δ activator insulin sensitizers
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N-(3-Triethoxysilylpropyl)-4-(N′-maleimidylmethyl)cyclohexanamide (TPMC): A heterobifunctional reagent for immobilization of oligonucleotides on glass surface
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Structure–activity studies of phenanthroindolizidine alkaloids as potential antitumor agents
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Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors
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Primary amides as selective inhibitors of cathepsin K
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Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists
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Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists
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Preparation of 1,3,5-thiadiazine-2-thione derivatives of chitosan and their potential antioxidant activity in vitro
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Novel ebselen–porphyrin conjugates: Synthesis and nucleic acid interaction study
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Design and synthesis of 1,2-dithiolane derivatives and evaluation of their neuroprotective activity
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Dual bioactivity of resveratrol fatty alcohols: Differentiation of neural stem cells and modulation of neuroinflammation
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Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating d-cysteine derivatives as P2/P3 moieties
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Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors
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Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor
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Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains
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Covalent bonding of vancomycin to Ti6Al4V alloy pins provides long-term inhibition of Staphylococcus aureus colonization
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Syntheses and antibacterial activity of phendioxy substituted cyclic enediynes
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6-Hydroxy to 6‴-amino tethered ring-to-ring macrocyclic aminoglycosides as probes for APH(3′)-IIIa kinase
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Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates
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Structural effects on the phosphorylation of 3-substituted 1-β-d-ribofuranosyl-1,2,4-triazoles by human adenosine kinase
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Design of potent PPARα agonists
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Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker—Synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase
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Safrole oxide is a useful tool for investigating the effect of apoptosis in vascular endothelial cells on neural stem cell survival and differentiation in vitro
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Aptazyme-based riboswitches as label-free and detector-free sensors for cofactors
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Small molecule antagonists of the CC chemokine receptor 4 (CCR4)
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Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors
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Paraliane and pepluane diterpenes as anti-inflammatory agents: First insights in structure–activity relationships
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Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile
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Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II
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Synthesis and structure–activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1
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Novel aminoethylbiphenyls as 5-HT7 receptor ligands
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Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity
Fulltext Access 5 Pages 2007
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists
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1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
Fulltext Access 5 Pages 2007
Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I
Fulltext Access 5 Pages 2007
Synthesis, bioactivity, theoretical and molecular docking study of 1-cyano-N-substituted-cyclopropanecarboxamide as ketol-acid reductoisomerase inhibitor
Fulltext Access 5 Pages 2007
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors
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Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands
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