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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共31条记录   4-Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands: Structural Insights into the Design of a Novel Inverse Agonist Series [作者：EL BAKALI JAMAL; MUCCIOLI GIULIO G; RENAULT NICOLAS; PRADAL DELPHINE; BODYMALAPEL MATHILDE; DJOUINA MADJID; HAMTIAUX LAURIE; ANDRZEJAK VIRGINIE; DESREUMAUX PIERRE; CHAVATTE PHILIPPE; LAMBERT DIDIER M; MILLET REGIS,期刊：Journal of Medicinal Chemistry, 页码：7918-7931 , 文章类型： Article，,卷期：2010年53-22] Growing evidence shows that CB2 receptor is an attractive therapeutic target. Starting from a series of 4-oxo-1,4-dihydroquinoline-3-carboxamide as selective CB2 agonists, we describe here the medicinal chemistry approac... Synthetic Human Serum Albumin Sudlow I Binding Site Mimics [作者：KARLSSON BJORN C G; ROSENGREN ANNIKA M; NASLUND INGA; ANDERSSON PER OLA; NICHOLLS IAN A,期刊：Journal of Medicinal Chemistry, 页码：7932-7937 , 文章类型： Article，,卷期：2010年53-22] Here, we report the design, synthesis, and characterization of molecularly imprinted polymer (MIP) derived mimics of the human serum albumin (HSA) Sudlow I site-the binding site for the anticoagulant warfarin. MIP design... 4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6 [作者：CHO YOUNG SHIN; BORLAND MARIA; BRAIN CHRISTOPHER; CHEN CHRISTINE H T; CHENG HONG; CHOPRA RAJIV; CHUNG KRISTY; GROARKE JAMES; HE GUO; HOU YING; KIM SUNKYU; KOVATS STEVEN; LU YIPIN; OREILLY MARC; SHEN JUNQING; SMITH TROY; TRAKSHEL GARY; VOEGTLE MARKUS; XU MEI; XU MING; SUNG MOO JE,期刊：Journal of Medicinal Chemistry, 页码：7938-7957 , 文章类型： Article，,卷期：2010年53-22] Identification and structure-guided optimization of a series of 4-(pyrazol-4-yl)-pyrimidines as selective CDK 4/6 inhibitors is reported herein. Several potency and selectivity determinants were established based on the ... Synthesis of a 6-Methyl-7-deaza Analogue of Adenosine That Potently Inhibits Replication of Polio and Dengue Viruses [作者：WU RUNZHI; SMIDANSKY ERIC D; OH HYUNG SUK; TAKHAMPUNYA RATREE; PADMANABHAN RADHAKRISHNAN; CAMERON CRAIG E; PETERSON BLAKE R,期刊：Journal of Medicinal Chemistry, 页码：7958-7966 , 文章类型： Article，,卷期：2010年53-22] Bioisosteric deaza analogues of 6-methyl-9-beta-D-ribofuranosylpurine, a hydrophobic analogue of adenosine, were synthesized and evaluated for antiviral activity. Whereas the 1-deaza and 3-deaza analogues were essentiall... Synthesis and Biological Evaluation of Polyenylpyrrole Derivatives as Anticancer Agents Acting through Caspases-Dependent Apoptosis [作者：FANG ZHANXIONG; LIAO PEICHUN; YANG YULIANG; YANG FENGLING; CHEN YILIN; LAM YULIN; HUA KUOFENG; WU SHIHHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：7967-7978 , 文章类型： Article，,卷期：2010年53-22] A class of polyenylpyrroles and their analogues were designed from a hit compound identified in a fungus. The compounds synthesized were evaluated for their cell cytotoxicity against human non-small-cell lung carcinoma c... Electron Density Guided Fragment-Based Lead Discovery of Ketohexokinase Inhibitors [作者：GIBBS ALAN C; ABAD MARTA C; ZHANG XUQING; TOUNGE BRETT A; LEWANDOWSKI FRANCIS A; STRUBLE GEOFFREY T; SUN WEIMEI; SUI ZHIHUA; KUO LAWRENCE C,期刊：Journal of Medicinal Chemistry, 页码：7979-7991 , 文章类型： Article，,卷期：2010年53-22] A fragment-based drug design paradigm has been successfully applied in the discovery of lead series of ketohexokinase inhibitors. The paradigm consists of three iterations of design, synthesis, and X-ray crystallographic... Phenolic Bis-styrylbenzenes as beta-Amyloid Binding Ligands and Free Radical Scavengers [作者：FLAHERTY DANIEL P; KIYOTA TOMOMI; DONG YUXIANG; IKEZU TSUNEYA; VENNERSTROM JONATHAN L,期刊：Journal of Medicinal Chemistry, 页码：7992-7999 , 文章类型： Article，,卷期：2010年53-22] Starting from bisphenolic bis-styrylbenzene DF-9 (4), P-amyloid (A beta) binding affinity and specificity for phenolic bis-styrylbenzenes, monostyrylbenzenes, and alkyne controls were determined by fluorescence titration... Synthesis and Biological Evaluation of Apogossypolone Derivatives as Pan-active Inhibitors of Antiapoptotic B-Cell Lymphoma/Leukemia-2 (Bcl-2) Family Proteins [作者：WEI JUN; KITADA SHINICHI; STEBBINS JOHN L; PLACZEK WILLIAM; ZHAI DAYONG; WU BAINAN; REGA MICHELE F; HANG ZIMING; CELLITTI JASON; YANG LI; DAHL RUSSELL; REED JOHN C; PELLECCHIA MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：8000-8011 , 文章类型： Article，,卷期：2010年53-22] Overexpression of antiapoptotic Bcl-2 family proteins is commonly related with tumor maintenance, progression, and chemoresistance. Inhibition of these antiapoptotic proteins is an attractive approach for cancer therapy.... Preparation and Evaluation of Carborane Analogues of Tamoxifen [作者：BEER MICHAEL L; LEMON JENNIFER; VALLIANT JOHN F,期刊：Journal of Medicinal Chemistry, 页码：8012-8020 , 文章类型： Article，,卷期：2010年53-22] A stereoselective synthesis or closo carborane analogues or tamoxifen was developed where the products represent a new approach to developing metabolically robust SERMs. The A-ring round in the backbone of tamoxifen was ... Essential Structural Features of TNF-alpha Lectin-like Domain Derived Peptides for Activation of Amiloride-Sensitive Sodium Current in A549 Cells [作者：HAZEMI PARASTOO; TZOTZOS SUSAN J; FISCHER BERNHARD; ANDAVAN GOWRI SHANKAR BAGAVANANTHEM; FISCHER HENDRIK; PIETSCHMANN HELMUT; LUCAS RUDOLF; LEMMENSGRUBER ROSA,期刊：Journal of Medicinal Chemistry, 页码：8021-8029 , 文章类型： Article，,卷期：2010年53-22] The amiloride-sensitive epithelial sodium channel (ENaC) plays a prominent role in sodium uptake from alveolar fluid and is the major component in alveolar fluid clearance in normal and diseased lungs. The lectin-like do... Effects on Molecular Conformation and Anticoagulant Activities of 1,6-Anhydrosugars at the Reducing Terminal of Antithrombin-Binding Octasaccharides Isolated from Low-Molecular-Weight Heparin Enoxaparin [作者：GUERRINI MARCO; ELLI STEFANO; GAUDESI DAVIDE; TORRI GIANGIACOMO; CASU BENITO; MOURIER PIERRE; HERMAN FREDERIC; BOUDIER CHRISTIAN; LORENZ MARTIN; VISKOV CHRISTIAN,期刊：Journal of Medicinal Chemistry, 页码：8030-8040 , 文章类型： Article，,卷期：2010年53-22] Terminal 1,6-anhydro-aminosugars (1,6-anAS) are typical structural moieties of enoxaparin, it low-molecular-weight heparin (LMWH) widely used for prevention and treatment of thrombotic disorders. In the enoxaparin manufa... Design of Three-Component Vaccines against Group A Streptococcal Infections: Importance of Spatial Arrangement of Vaccine Components [作者：ABDELAAL ABUBAKER M; ZAMAN MEHFUZ; FUJITA YOSHIO; BATZLOFF MICHAEL R; GOOD MICHAEL F; TOTH ISTVAN,期刊：Journal of Medicinal Chemistry, 页码：8041-8046 , 文章类型： Article，,卷期：2010年53-22] Immunological assessment of group A streptococcal (GAS) branched lipopeptides demonstrated the impact of spatial arrangement of vaccine components on both the quality and quantity of their immune responses. Each lipopept... Design, Synthesis, and Preclinical Evaluation of New 5,6-(or 6,7-) Disubstituted-2-(fluorophenyl)quinolin-4-one Derivatives as Potent Antitumor Agents [作者：CHOU LICHEN; TSAI MENGTUNG; HSU MEIHUA; WANG SHENGHUNG; WAY TZONGDER; HUANG CHIHUNG; LIN HUIYI; QIAN KEDUO; DONG YIZHOU; LEE KUOHSIUNG; HUANG LIJIAU; KUO SHENGCHU,期刊：Journal of Medicinal Chemistry, 页码：8047-8058 , 文章类型： Article，,卷期：2010年53-22] Our previous exploration of 2-phenylquinolin-4-ones (2-PQs) has led to an anticancer drug candidate 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na). In order to develop additional ne... Disulfide Cyclized Tripeptide Analogues of Angiotensin IV as Potent and Selective Inhibitors of Insulin-Regulated Aminopeptidase (IRAP) [作者：ANDERSSON HANNA; DEMAEGDT HEIDI; VAUQUELIN GEORGES; LINDEBERG GUNNAR; KARLEN ANDERS; HALLBERG MATHIAS; ERDELYI MATE; HALLBERG ANDERS,期刊：Journal of Medicinal Chemistry, 页码：8059-8071 , 文章类型： Article，,卷期：2010年53-22] The insulin-regulated aminopeptidase (I RAP) localized in areas of the brain associated with memory and learning is emerging as a new promising therapeutic target for the treatment of memory dysfunctions. The angiotensin... Side Chain Cyclization Based on Serine Residues: Synthesis, Structure, and Activity of a Novel Cyclic Analogue of the Parathyroid Hormone Fragment 1-11 [作者：CAPORALE ANDREA; STURLESE MATTIA; GESIOT LORENZO; ZANTA FABRIZIO; WITTELSBERGER ANGELA; CABRELE CHIARA,期刊：Journal of Medicinal Chemistry, 页码：8072-8079 , 文章类型： Article，,卷期：2010年53-22] The N-terminal region of the parathyroid hormone (PTH) is sufficient to activate the G-protein-coupled PTH receptor 1 (PTH 1). The shortest PTH analogue displaying nanomolar potency is the undecapeptide H-Aib-Val-Aib-Glu... Virtual Screening to Identify Novel Antagonists for the C Protein-Coupled NK3 Receptor [作者：GELDENHUYS WERNER J; KUZENKO STEPHANIE R; SIMMONS MARK A,期刊：Journal of Medicinal Chemistry, 页码：8080-8088 , 文章类型： Article，,卷期：2010年53-22] The NK3 subtype of tachykinin receptor is a G protein-coupled receptor that is a potential therapeutic target for several neurological diseases, including schizophrenia. In this study, we have screened compound databases...