Journal of Medicinal Chemistry————————个性化文献订阅—

Synthesis and Biological Evaluation of Bivalent Ligands for the Cannabinoid 1 Receptor
[作者：ZHANG YANAN; GILLIAM ANNE; MAITRA RANGAN; DAMAJ M IMAD; TAJUBA JULIANNE M; SELTZMAN HERBERT H; THOMAS BRIAN F,期刊：Journal of Medicinal Chemistry, 页码：7048-7060 , 文章类型： Article，,卷期：2010年53-19]
Dimerization or oligomerization Or many G-protein-coupled receptors (GPCRs), including the cannabinoid I (CBI) receptor, is now widely accepted and may have significant implications for medications development targeting ...

Crystal Structures of HLA-A*0201 Complexed with Melan-A/MART-1(26(27L)-35) Peptidomimetics Reveal Conformational Heterogeneity and Highlight Degeneracy of T Cell Recognition
[作者：DOUATCASASSUS CELINE; BORBULEVYCH OLEG; TARBE MARION; GERVOIS NADINE; JOTERCAU FRANCINE; BAKER BRIAN M; QUIDEAU STEPHANE,期刊：Journal of Medicinal Chemistry, 页码：7061-7066 , 文章类型： Article，,卷期：2010年53-19]
There is growing interest in using tumor associated antigens presented by class1 major histocompatibility complex (MHC-I) proteins as cancer vaccines. As native peptides are poorly stable in biological fluids, researcher...

1-Aryl-3-(1-acylpiperidin-4-yl)urea Inhibitors of Human and Murine Soluble Epoxide Hydrolase: Structure-Activity Relationships, Pharmacokinetics, and Reduction of Inflammatory Pain
[作者：ROSE TRISTAN E; MORISSEAU CHRISTOPHE; LIU JUNYAN; INCEOGLU BORA; JONES PAUL D; SANBORN JAMES R; HAMMOCK BRUCE D,期刊：Journal of Medicinal Chemistry, 页码：7067-7075 , 文章类型： Article，,卷期：2010年53-19]
1,3-Disubstituted ureas possessing a piperidyl moiety have been synthesized to investigate their structure activity relationships as inhibitors of the human and murine soluble epoxide hydrolase (sEH). Oral administration...

Endochin Optimization: Structure-Activity and Structure-Property Relationship Studies of 3-Substituted 2-Methyl-4(1H)-quinolones with Antimalarial Activity
[作者：CROSS R MATTHEW; MONASTYRSKYI ANDRII; MUKTA TINA S; BURROWS JEREMY N; KYLE DENNIS E; MANETSCH ROMAN,期刊：Journal of Medicinal Chemistry, 页码：7076-7094 , 文章类型： Article，,卷期：2010年53-19]
Since the 1940s endochin and analogues thereof were known to be causal prophylactic and potent erythrocytic stage agents in avian models. Preliminary screening in a current in vitro assay identified several 4(1H)-quinolo...

Development of Molecular Probes for the Human 5-HT6 Receptor
[作者：VAZQUEZVILLA HENAR; GONZALEZVERA JUAN A; BENHAMU BELLINDA; VISO ALMA; FERNANDEZ DE LA PRADILLA ROBERTO; JUNQUERA ELENA; AICART EMILIO; LOPEZRODRIGUEZ MARIA L; ORTEGAGUTIERREZ SILVIA,期刊：Journal of Medicinal Chemistry, 页码：7095-7106 , 文章类型： Article，,卷期：2010年53-19]
In this work we report the synthesis of a set of labeled ligands targeting the human 5-HT6, receptor (h5-HT6R). Among the synthesized compounds, fluorescent probe 10 (K-i = 175 nM and Phi(f) = 0.21 land biotinylated deri...

Design, Synthesis, and Structure-Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5
[作者：BURDI DOUGLAS F; HUNT RACHEL; FAN LEI; HU TAO; WANG JUN; GUO ZIHONG; HUANG ZHIQIANG; WU CHENGDE; HARDY LARRY; DETHEUX MICHEL; ORSINI MICHAEL A; QUINTON MARIA S; LEW ROBERT; SPEAR KERRY,期刊：Journal of Medicinal Chemistry, 页码：7107-7118 , 文章类型： Article，,卷期：2010年53-19]
A novel series of diaryl bicyclic azole-amines that are potent selective negative modulators of meta botropic glutamate receptor 5 (mGluR5) were identified through rational design. An initial hit compound 5a of modest po...

Click-Chemistry-Derived Triazole Ligands of Arginine-Glycine-Aspartate (RGD) Integrins with a Broad Capacity To Inhibit Adhesion of Melanoma Cells and Both in Vitro and in Vivo Angiogenesis
[作者：TRABOCCHI ANDREA; MENCHI GLORIA; CINI NICOLETTA; BIANCHINI FRANCESCA; RASPANTI SILVIA; BOTTONCETTI ANNA; PUPI ALBERTO; CALORINI LIDO; GUARNA ANTONIO,期刊：Journal of Medicinal Chemistry, 页码：7119-7128 , 文章类型： Article，,卷期：2010年53-19]
A click chemistry approach was applied for the discovery of triazole-based arginine-glycine-aspartate (RGD) mimetics by Cu(1)-catalyzed 1,3-dipolar alkyne azide coupling reaction, which showed binding all properties towa...

Exploration of the Amine Terminus in a Novel Series of 1,2,4-Triazolo-3-yl-azabicyclo[3.1.0]hexanes as Selective Dopamine D-3 Receptor Antagonists
[作者：MICHELI FABRIZIO; ARISTA LUCA; BERTANI BARBARA; BRAGGIO SIMONE; CAPELLI ANNA MARIA; CREMONESI SUSANNA; DIFABIO ROMANO; GELARDI GIACOMO; GENTILE GABRIELLA; MARCHIORO CARLA; PASQUARELLO ALESSANDRA; PROVERA STEFANO; TEDESCO GIOVANNA; TARSI LUCA; TERRENI SILVIA; WORBY ANGELA; HEIDBREDER CHRISTIAN,期刊：Journal of Medicinal Chemistry, 页码：7129-7139 , 文章类型： Article，,卷期：2010年53-19]
A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes with high affinity and selectivity for the DA D-3 receptor and excellent pharmacokinetic profiles was recently reported. We also recently discussed the role o...

Synthesis and Antitumor Effect in Vitro and in Vivo of Substituted 1,3-Dihydroindole-2-ones
[作者：CHRISTENSEN METTE K; ERICHSEN KAMILLE D; TROJELHANSEN CHRISTINA; TJORNELUND JETTE; NIELSEN SOREN J; FRYDENVANG KARLA; JOHANSEN TOMMY N; NIELSEN BIRGITTE; SCHESTED MAXWELL; JENSEN PETER B; IKAUNIEKS MARTINS; ZAICHENKO ANDREI; LOZA EINARS; KALVINSH IVARS; BJORKLING FREDRIK,期刊：Journal of Medicinal Chemistry, 页码：7140-7145 , 文章类型： Article，,卷期：2010年53-19]
Optimization of the anticancer activity for a class of compounds built on a 1,3-dihydroindole-2-one scaffold was performed. In comparison with recently published derivatives of oxyphenisatin the new analogues exhibited a...

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