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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57条记录   Nucleoside-5 '-monophosphates as Prodrugs of Adenosine A(2A) Receptor Agonists Activated by ecto-5 '-Nucleotidase [作者：ELTAYEB ALI; IQBAL JAMSHED; BEHRENSWERTH ANDREA; ROMIO MICHAEL; SCHNEIDER MARION; ZIMMERMANN HERBERT; SCHRADER JUERGEN; MUELLER CHRISTA E,期刊：Journal of Medicinal Chemistry, 页码：7669-7677 , 文章类型： Article，,卷期：2009年52-23] Prodrugs of adenosine A(2A) receptor agonists were developed that are activated by ecto-5'-nucleotidase (ecto-5'-NT, CD73). Because ecto-5'-NT is upregulated in inflamed tissue, the A(2A) agonists are expected to be rele... Preclinical Efficacy of a Carboxylesterase 2-Activated Prodrug of Doxazolidine [作者：BARTHEL BENJAMIN L; ZHANG ZHIYONG; RUDNICKI DANIEL L; COLDREN CHRISTOPHER D; POLINKOVSKY MARGARET; SUN HENGRUI; KOCH GARY G; CHAN DANIEL C F; KOCH TAD H,期刊：Journal of Medicinal Chemistry, 页码：7678-7688 , 文章类型： Article，,卷期：2009年52-23] Doxazolidine (Doxaz) is a functionally distinct formaldehyde conjugate or doxorubicin (Dox) that induces cancer cell death in Dox-sensitive and resistant cells. Pentyl PABC-Doxaz (PPD) is a prodrug or Doxaz that is activ... Design, Synthesis, Protein-Ligand X-ray Structure, and Biological Evaluation of a Series of Novel Macrocyclic Human Immunodeficiency Virus-1 Protease Inhibitors to Combat Drug Resistance [作者：GHOSH ARUN K; KULKARNI SARANG; ANDERSON DAVID D; HONG LIN; BALDRIDGE ABIGAIL; WANG YUANFANG; CHUMANEVICH ALEXANDER A; KOVALEVSKY ANDREY Y; TOJO YASUSHI; AMANO MASAYUKI; KOH YASUHIRO; TANG JORDAN; WEBER IRENE T; MITSUYA HIROAKI,期刊：Journal of Medicinal Chemistry, 页码：7689-7705 , 文章类型： Article，,卷期：2009年52-23] The structure-based design, synthesis, and biological evaluation of a series of nonpeptidic macrocyclic HIV protease inhibitors are described. The inhibitors are designed to effectively fill in the hydrophobic pocket in ... Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites [作者：SHAMOVSKY IGOR; DE GRAAF CHRIS; ALDERIN LISA; BENGTSSON MALENA; BLADH HAKAN; BORJESSON LENA; CONNOLLY STEPHEN; DYKE HAZEL J; VAN DEN HEUVEL MARCO; JOHANSSON HENRIK; JOSEFSSON BOGOERAN; KRISTOFFERSSON ANNA; LINNANEN TERO; LISIUS ANNEA; MANNIKKO ROOPE; NORDEN BO; PRICE STEVE; RIPA LENA; ROGNAN DIDIER; ROSENDAHL ALEXANDER; SKRINJAR MARCO; URBAHNS KLAUS,期刊：Journal of Medicinal Chemistry, 页码：7706-7723 , 文章类型： Article，,卷期：2009年52-23] The metabolic stability and selectivity of a series of CCR8 antagonists against binding to the hERG ion channel and cytochrome Cyp2D6 are studied by principal component analysis. It is demonstrated that an efficient way ... Pentapeptides Displaying mu Opioid Receptor Agonist and delta Opioid Receptor Partial Agonist/Antagonist Properties [作者：PURINGTON LAUREN C; POGOZHEVA IRINA D; TRAYNOR JOHN R; MOSBERG HENRY I,期刊：Journal of Medicinal Chemistry, 页码：7724-7731 , 文章类型： Article，,卷期：2009年52-23] Chronic use of mu-opioid agonists has been shown to cause neurochemical adaptations resulting in tolerance and dependence, While the analgesic effects of these drugs are mediated by mu-opioid receptors (MOR), several stu... Amide Linkage Isomerism As an Activity Switch for Organometallic Osmium and Ruthenium Anticancer Complexes [作者：VAN RIJT SABINE H; HEBDEN ANDREW J; AMARESEKERA THAKSHILA; DEETH ROBERT J; CLARKSON GUY J; PARSONS SIMON; MCGOWAN PATRICK C; SADLER PETER J,期刊：Journal of Medicinal Chemistry, 页码：7753-7764 , 文章类型： Article，,卷期：2009年52-23] We show that the binding mode adopted by picolinamide derivatives in organometallic Os-II and Ru-II half-sandwich complexes can lead to contrasting cancer cell cytotoxicity. N-Phenyl picolinamide derivatives (XY) in Os-I... Synthesis of New Alkylaminooxysterols with Potent Cell Differentiating Activities: Identification of Leads for the Treatment of Cancer and Neurodegenerative Diseases [作者：DE MEDINA PHILIPPE; PAILLASSE MICHAEL R; PAYRE BRUNO; SILVENTEPOIROT SANDRINE; POIROT MARC,期刊：Journal of Medicinal Chemistry, 页码：7765-7777 , 文章类型： Article，,卷期：2009年52-23] We describe here the syntheses and the biological properties of new alkylaminooxysterols. Compounds were synthesized through the trans-diaxial aminolysis of 5,6-alpha-epoxysterols with various natural amines including hi... Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects [作者：WANG TAO; YIN ZHIWEI; ZHANG ZHONGXING; BENDER JOHN A; YANG ZHONG; JOHNSON GRAHAM; YANG ZHENG; ZADJURA LISA M; DARIENO CELIA J; PARKER DAWN DIGIUGNO; GESENBERG CHRISTOPHE; YAMANAKA GREGORY A; GONG YIFEI; HO HSUTSO; FANG HUA; ZHOU NANNAN; MCAULIFFE BRIAN V; EGGERS BETSY J; FAN LI; NOWICKASANS BEATA; DICKER IRA B; GAO QI; COLONNO RICHARD J; LIN PINFANG; MEANWELL NICHOLAS A; KADOW JOHN F,期刊：Journal of Medicinal Chemistry, 页码：7778-7787 , 文章类型： Article，,卷期：2009年52-23] Azaindole derivatives derived from the screening lead 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1) were prepared and characterized to assess their potential as inhibitors of HIV-1 attachment. Systema... Eleven Amino Acid Glucagon-like Peptide-1 Receptor Agonists with Antidiabetic Activity [作者：MAPELLI CLAUDIO; NATARAJAN SESHA I; MEYER JEANPHILIPPE; BASTOS MARGARITA M; BERNATOWICZ MICHAEL S; LEE VING G; PLUSCEC JELKA; RIEXINGER DOUGLAS J; SIEBERMCMASTER ELLEN S; CONSTANTINE KEITH L; SMITHMONROY CONSTANCE A; GOLLA RAJASREE; MA ZHENGPING; LONGHI DANIEL A; SHI DAN; XIN LI; TAYLOR JOSEPH R; KOPLOWITZ BARRY; CHI CECILIA L; KHANNA ASHISH; ROBINSON GORDON W; SEETHALA RAMAKRISHNA; ANATALZIMANYI ILDIKO A; STOFFEL ROBERT H; HAN SONGPING; WHALEY JEAN M; HUANG CHRISTINE S; KRUPINSKI JOHN; EWING WILLIAM R,期刊：Journal of Medicinal Chemistry, 页码：7788-7799 , 文章类型： Article，,卷期：2009年52-23] Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 ami...