个性化文献订阅>文章检索

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24条记录   How Well Can Fragments Explore Accessed Chemical Space? A Case Study from Heat Shock Protein 90 [作者：ROUGHLEY STEPHEN D; HUBBARD RODERICK E,期刊：Journal of Medicinal Chemistry, 页码：3989-4005 , 文章类型： Editorial Material，,卷期：2011年54-12] Structure-Based Design of Potent Aromatase Inhibitors by High-Throughput Docking [作者：CAPORUSCIO FABIANA; RASTELLI GIULIO; IMBRIANO CAROL; DEL RIO ALBERTO,期刊：Journal of Medicinal Chemistry, 页码：4006-4017 , 文章类型： Article，,卷期：2011年54-12] Cytochrome P450 aromatase catalyzes the conversion of androgen substrates into estrogens. Aromatase inhibitors (AIs) have been used as first-line drugs in the treatment of estrogen-dependent breast cancer in postmenopaus... Pyrimidine Nucleotides with 4-Alkyloxyimino and Terminal Tetraphosphate delta-Ester Modifications as Selective Agonists of the P2Y(4) Receptor [作者：MARUOKA HIROSHI; JAYASEKARA M P SURESH; BARRETT MATTHEW O; FRANKLIN DEREK A; DE CASTRO SONIA; KIM NATHANIEL; COSTANZI STEFANO; HARDEN T KENDALL; JACOBSON KENNETH A,期刊：Journal of Medicinal Chemistry, 页码：4018-4033 , 文章类型： Article，,卷期：2011年54-12] P2Y(2) and P2Y(4) receptors are G protein-coupled receptors, activated by UTP and dinudeoside tetraphosphates, which are difficult to distinguish pharmacologically for lack of potent and selective ligands. We structurall... Adenosine-Derived Inhibitors of 78 kDa Glucose Regulated Protein (Grp78) ATPase: Insights into Isoform Selectivity [作者：MACIAS ALBA T; WILLIAMSON DOUGLAS S; ALLEN NICOLA; BORGOGNONI JENIFER; CLAY ALEXANDRA; DANIELS ZOE; DOKURNO PAWEL; DRYSDALE MARTIN J; FRANCIS GERAINT L; GRAHAM CHRISTOPHER J; HOWES ROB; MATASSOVA NATALIA; MURRAY JAMES B; PARSONS RACHEL; SHAW TERRY; SURGENOR ALLAN E; TERRY LINDSEY; WANG YIKANG; WOOD MIKE; MASSEY ANDREW J,期刊：Journal of Medicinal Chemistry, 页码：4034-4041 , 文章类型： Article，,卷期：2011年54-12] 78 kDa glucose-regulated protein (Grp78) is a heat shock protein (HSP) involved in protein folding that plays a role in cancer cell proliferation. Binding of adenosine-derived inhibitors to Grp78 was characterized by sur... Switching Reversibility to Irreversibility in Glycogen Synthase Kinase 3 Inhibitors: Clues for Specific Design of New Compounds [作者：PEREZ DANIEL I; PALOMO VALLE; PEREZ CONCEPCION; GIL CARMEN; DANS PABLO D; JAVIER LUQUE F; CONDE SANTIAGO; MARTINEZ ANA,期刊：Journal of Medicinal Chemistry, 页码：4042-4056 , 文章类型： Article，,卷期：2011年54-12] Development of kinase-targeted therapies for central nervous system (CNS) diseases is a great challenge. Glycogen synthase kinase 3 (GSK-3) offers a great potential for severe CNS unmet diseases, being one of the inhibit... Akt-Dependent Anabolic Activity of Natural and Synthetic Brassinosteroids in Rat Skeletal Muscle Cells [作者：ESPOSITO DEBORA; RATHINASABAPATHY THIRUMURUGAN; POULEV ALEXANDER; KOMARNYTSKY SLAVKO; RASKIN ILYA,期刊：Journal of Medicinal Chemistry, 页码：4057-4066 , 文章类型： Article，,卷期：2011年54-12] Brassinosteroids are plant-derived polyhydroxylated derivatives of Sa-cholestane, structurally similar to cholesterol-derived animal steroid hormones and insect ecdysteroids. In this study, we synthesized a set of brassi... Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma [作者：RAOUANE MOUNA; DESMAELE DIDIER; GILBERTSIRIEIX MARIE; GUEUTIN CLAIRE; ZOUHIRI FATIMA; BOURGAUX CLAUDIE; LEPELTIER ELISE; GREF RUXANDRA; BEN SALAH RIDHA; CLAYMAN GARY; MASSAADMASSADE LILIANE; COUVREUR PATRICK,期刊：Journal of Medicinal Chemistry, 页码：4067-4076 , 文章类型： Article，,卷期：2011年54-12] We report the conjugation of the natural lipid squalene (SQ) with a small interfering RNA (siRNA), against the junction oncogene RET/PTC1, usually found in papillary thyroid carcinoma (PTC). The acyclic isoprenoid chain ... Design, Synthesis, and Cytotoxic Evaluation of Acyl Derivatives of 3-Aminonaphtho[2,3-b]thiophene-4,9-dione, a Quinone-Based System [作者：GOMEZMONTERREY ISABEL; CAMPIGLIA PIETRO; AQUINO CLAUDIO; BERTAMINO ALESSIA; GRANATA ILARIA; CAROTENUTO ALFONSO; BRANCACCIO DIEGO; STIUSO PAOLA; SCOGNAMIGLIO ILARIA; RUSCIANO M ROSARIA; MAIONE ANGELA SERENA; ILLARIO MADDALENA; GRIECO PAOLO; MARESCA BRUNO; NOVELLINO ETTORE,期刊：Journal of Medicinal Chemistry, 页码：4077-4091 , 文章类型： Article，,卷期：2011年54-12] A series of 3-acyl derivatives of the dihydronaphtho[2,3-b]thiophen-4,9-dione system were studied with respect to cytotoxicity and topoisomerase II inhibitory activity. These analogues were designed as electron-deficient... Discovery of a 5H-Benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) Inhibitor of c-Met Kinase for the Treatment of Cancer [作者：KATZ JASON D; JEWELL JAMES P; GUERIN DAVID J; LIM JONGWON; DINSMORE CHRISTOPHER J; DESHMUKH SUJAL V; PAN BOSHENG; MARSHALL C GARY; LU WEI; ALTMAN MICHAEL D; DAHLBERG WILLIAM K; DAVIS LENORA; FALCONE DANIELLE; GABARDA ANA E; HANG GAOZHEN; HATCH HAROLD; HOLMES RACHAEL; KUNII KAIKO; LUMB KEVIN J; LUTTERBACH BART; MATHVINK ROBERT; NAZEF NAIM; PATEL SANGITA B; QU XIANLU; REILLY JOHN F; RICKERT KEITH W; ROSENSTEIN CRAIG; SOISSON STEPHEN M; SPENCER KERRIE B; SZEWCZAK ALEXANDER A; WALKER DEBORAH; WANG WENXIAN; YOUNG JONATHAN; ZENG QINWEN,期刊：Journal of Medicinal Chemistry, 页码：4092-4108 , 文章类型： Article，,卷期：2011年54-12] c-Met is a transmembrane tyrosine kinase that mediates activation of several signaling pathways implicated in aggressive cancer phenotypes. In recent years, research into this area has highlighted c-Met as an attractive ... 17(R),18(S)-Epoxyeicosatetraenoic Acid, a Potent Eicosapentaenoic Acid (EPA) Derived Regulator of Cardiomyocyte Contraction: Structure-Activity Relationships and Stable Analogues [作者：FALCK JOHN R; WALLUKAT GERD; PULI NARENDER; GOLI MOHAN; ARNOLD COSIMA; KONKEL ANNE; ROTHE MICHAEL; FISCHER ROBERT; MUELLER DOMINIK N; SCHUNCK WOLFHAGEN,期刊：Journal of Medicinal Chemistry, 页码：4109-4118 , 文章类型： Article，,卷期：2011年54-12] 17(R),18 (S)-Epoxyeicosatetraenoic acid [17(R),18(S)-EETeTr], a cytochrome P450 epoxygenase metabolite of eicosapentaenoic acid (EPA), exerts negative chronotropic effects and protects neonatal rat cardiomyocytes against... Thiazolides as Novel Antiviral Agents. 1. Inhibition of Hepatitis B Virus Replication [作者：STACHULSKI ANDREW V; PIDATHALA CHANDRAKALA; ROW ELEANOR C; SHARMA RAMAN; BERRY NEIL G; IQBAL MAZHAR; BENTLEY JOANNE; ALLMAN SARAH A; EDWARDS GEOFFREY; HELM ALISON; HELLIER JENNIFER; KORBA BRENT E; SEMPLE J EDWARD; ROSSIGNOL JEANFRANCOIS,期刊：Journal of Medicinal Chemistry, 页码：4119-4132 , 文章类型： Article，,卷期：2011年54-12] We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, n... Irreversible Nek2 Kinase Inhibitors with Cellular Activity [作者：HENISE JEFFREY C; TAUNTON JACK,期刊：Journal of Medicinal Chemistry, 页码：4133-4146 , 文章类型： Article，,卷期：2011年54-12] A structure-based approach was used to design irreversible, cysteine-targeted inhibitors of the human centrosomal kinase, Nek2. Potent inhibition of Nek2 kinase activity in biochemical and cell-based assays required a no... Novel Chalcone Derivatives as Potent Nrf2 Activators in Mice and Human Lung Epithelial Cells [作者：KUMAR VINEET; KUMAR SARVESH; HASSAN MOHAMMAD; WU HAILONG; THIMMULAPPA RAJESH K; KUMAR AMIT; SHARMA SUNIL K; PARMAR VIRINDER S; BISWAL SHYAM; MALHOTRA SANJAY V,期刊：Journal of Medicinal Chemistry, 页码：4147-4159 , 文章类型： Article，,卷期：2011年54-12] Nrf2-mediated activation of antioxidant response element is a central part of molecular mechanisms governing the protective function of phase II detoxification and antioxidant enzymes against carcinogenesis, oxidative st... Factors Determining the Superior Performance of Lipid/DNA/Protammine Nanoparticles over Lipoplexes [作者：CARACCIOLO GIULIO; POZZI DANIELA; CAPRIOTTI ANNA LAURA; MARIANECCI CARLOTTA; CARAFA MARIA; MARCHINI CRISTINA; MONTANI MAURA; AMICI AUGUSTO; AMENITSCH HEINZ; DIGMAN MICHELLE A; GRATTON ENRICO; SANCHEZ SUSANA S; LAGANA ALDO,期刊：Journal of Medicinal Chemistry, 页码：4160-4171 , 文章类型： Article，,卷期：2011年54-12] The utility of using a protammine/DNA complex coated with a lipid envelope made of cationic 1,2-dioleoyl-3-trimethylammonium propane (DOTAP) for transfecting CHO (Chinese hamster ovary cells), HEK293 (human embryonic kid... Leucettines, a Class of Potent Inhibitors of cdc2-Like Kinases and Dual Specificity, Tyrosine Phosphorylation Regulated Kinases Derived from the Marine Sponge Leucettamine B: Modulation of Alternative Pre-RNA Splicing [作者：DEBDAB MANSOUR; CARREAUX FRANCOIS; RENAULT STEVEN; SOUNDARARAJAN MEERA; FEDOROV OLEG; FILIPPAKOPOULOS PANAGIS; LOZACH OLIVIER; BABAULT LUCIE; TAHTOUH TANIA; BARATTE BLANDINE; OGAWA YASUSHI; HAGIWARA MASATOSHI; EISENREICH ANDREAS; RAUCH URSULA; KNAPP STEFAN; MEIJER LAURENT; BAZUREAU JEANPIERRE,期刊：Journal of Medicinal Chemistry, 页码：4172-4186 , 文章类型： Article，,卷期：2011年54-12] We here report on the synthesis, optimization, and biological characterization of leucettines, a family of kinase inhibitors derived from the marine sponge leucettamine B. Stepwise synthesis of analogues starting from th... Discovery of N-(1-Ethylpropyl)-(3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-me thyl-pyrazin-2-yl)amine 59 (NGD 98-2): An Orally Active Corticotropin Releasing Factor-1 (CRF-1) Receptor Antagonist [作者：HODGETTS KEVIN J; GE PING; YOON TAEYOUNG; DE LOMBAERT STEPHANE; BRODBECK ROBBIN; GULIANELLO MICHAEL; KIELTYKA ANDRZEJ; HORVATH RAYMOND F; KEHNE JOHN H; KRAUSE JAMES E; MAYNARD GEORGE D; HOFFMAN DIANE; LEE YOUNGLIM; FUNG LAURENCE; DOLLER DARIO,期刊：Journal of Medicinal Chemistry, 页码：4187-4206 , 文章类型： Article，,卷期：2011年54-12] The design, synthesis, and structure-activity relationships of a novel series of pyrazines, acting as corticotropin releasing factor-1 (CRF-1) receptor antagonists, are described. Synthetic methodologies were developed t...