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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22条记录   Pyrimidine Ribonucleotides with Enhanced Selectivity as P2Y(6) Receptor Agonists: Novel 4-Alkyloxyimino, (S)-Methanocarba, and 5 '-Triphosphate gamma-Ester Modifications [作者：MARUOKA HIROSHI; BARRETT MATTHEW O; KO HYOJIN; TOSH DILIP K; MELMAN ARTEM; BURIANEK LAUREN E; BALASUBRAMANIAN RAMACHANDRAN; BERK BARKIN; COSTANZI STEFANO; HARDEN T KENDALL; JACOBSON KENNETH A,期刊：Journal of Medicinal Chemistry, 页码：4488-4501 , 文章类型： Article，,卷期：2010年53-11] The P2Y(6) receptor is a cytoprotective G-protein-coupled receptor (GPCR) activated by UDP (EC50 = 0.30 mu M). We compared and combined modifications to enhance P2Y(6) receptor agonist selectivity, including ribose ring ... Analysis of Kinase Inhibitor Selectivity using a Thermodynamics-Based Partition Index [作者：CHENG ALAN C; EKSTEROWICZ JOHN; GEUNSMEYER STEPHANIE; SUN YAXIONG,期刊：Journal of Medicinal Chemistry, 页码：4502-4510 , 文章类型： Article，,卷期：2010年53-11] In the quest for safe, efficacious kinase inhibitors as drugs, selectivity is often assessed early using kinase profiling panels. Here we present a selectivity index based on thermodynamics principles that can help in an... Discovery of Novel Selective Norepinephrine Reuptake Inhibitors: 4-[3-Aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231) [作者：ONEILL DAVID J; ADEDOYIN ADEDAYO; ALFINITO PETER D; BRAY JENIFER A; COSMI SCOTT; DEECHER DARLENE C; FENSOME ANDREW; HARRISON JIM; LEVENTHAL LIZA; MANN CHARLES; MCCOMAS CASEY C; SULLIVAN NICOLE R; SPANGLER TAYLOR B; UVEGES ALBERT J; TRYBULSKI EUGENE J; WHITESIDE GARTH T; ZHANG PUWEN,期刊：Journal of Medicinal Chemistry, 页码：4511-4521 , 文章类型： Article，,卷期：2010年53-11] Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)bu tan-2-ols which are potent and selective inhibitors ... Synthesis and Structure-Activity Relationships of Long-acting beta(2) Adrenergic Receptor Agonists Incorporating Metabolic Inactivation: An Antedrug Approach [作者：PROCOPIOU PANAYIOTIS A; BARRETT VICTORIA J; BEVAN NICOLA J; BIGGADIKE KEITH; BOX PHILIP C; BUTCHERS PETER R; COE DIANE M; CONROY RICHARD; EMMONS AMANDA; FORD ALISON J; HOLMES DUNCAN S; HORSLEY HELEN; KERR FERN; LIKWAICHEUNG ANNEMARIE; LOOKER BRIAN E; MANN INDERJIT S; MCLAY IAIN M; MORRISON VALERIE S; MUTCH PETER J; SMITH CLAIRE E; TOMLIN PAULA,期刊：Journal of Medicinal Chemistry, 页码：4522-4530 , 文章类型： Article，,卷期：2010年53-11] A series of saligenin beta(2) adrenoceptor agonist antedrugs having high clearance were prepared by reacting a protected saligenin oxazolidinone with protected hydroxyethoxyalkoxyalkyl bromides, followed by removal of th... Structure Guided Design of 5-Arylindazole Glucocorticoid Receptor Agonists and Antagonists [作者：YATES CHRISTOPHER M; BROWN PETER J; STEWART EUGENE L; PATTEN CHRISTOPHER; AUSTIN ROBERT J H; HOLT JASON A; MAGLICH JODI M; ANGELL DAVINA C; SASSE ROSEMARY Z; TAYLOR SIMON J; UINGS IAIN J; TRUMP RYAN P,期刊：Journal of Medicinal Chemistry, 页码：4531-4544 , 文章类型： Article，,卷期：2010年53-11] Glucocorticoid receptor (GR) agonists have been used for more than half a century as the most effective treatment or acute and chronic inflammatory conditions despite serious side effects that accompany their extended us... Design and Synthesis of alpha-Ketoamides as Cathepsin S Inhibitors with Potential Applications against Tumor Invasion and Angiogenesis [作者：CHEN JOCHUN; UANG BIINGJIUN; LYU PINGCHIANG; CHANG JANGYANG; LIU KOJIUNN; KUO CHINGCHUAN; HSIEH HSINGPANG; WANG HSINCHIEH; CHENG CHAOSHENG; CHANG YIHSUN; CHANG MARGARET DAHTSYR; CHANG WUNSHAING WAYNE; LIN CHUNCHENG,期刊：Journal of Medicinal Chemistry, 页码：4545-4549 , 文章类型： Article，,卷期：2010年53-11] A series of small molecules bearing an alpha-ketoamide warhead were synthesized and evaluated for their ability to inhibit cathepsin S, a key proteolytic enzyme upregulated in many cancers during tumor progression and me... Synthesis and Evaluation of New Endomorphin-2 Analogues Containing (Z)-alpha,beta-Didehydrophenylalanine (Delta(Z)Phe) Residues [作者：TORINO DOMENICA; MOLLICA ADRIANO; PINNEN FRANCESCO; FELICIANI FEDERICA; LUCENTE GINO; FABRIZI GIANCARLO; PORTALONE GUSTAVO; DAVIS PEG; LAI JOSEPHINE; MA SHOUWU; PORRECA FRANK; HRUBY VICTOR J,期刊：Journal of Medicinal Chemistry, 页码：4550-4554 , 文章类型： Article，,卷期：2010年53-11] New endomorphin-2 (EM-2) analogues incorporating (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) in place of the native phenylalanine in EM-2 are reported. Tyr-Pro-Delta(Z)Phe-Phe-NH2 {[Delta(Z)Phe(3)]EM-2} (1), Tyr-... Rationale Design of Biotinylated Antimalarial Endoperoxide Carbon Centered Radical Prodrugs for Applications in Proteomics [作者：BARTON VICTORIA; WARD STEVEN A; CHADWICK JAMES; HILL ALASDAIR; ONEILL PAUL M,期刊：Journal of Medicinal Chemistry, 页码：4555-4559 , 文章类型： Article，,卷期：2010年53-11] The semisynthetic artemisinin derivatives such as artesunate and artemether, along with the fully synthetic endoperoxide antimalarials (e.g., OZ277, Nature 2004, 430, 900-904), are believed to mediate their antimalarial ... Current and Future Medical Approaches To Combat the Anthrax Threat [作者：BOUZIANAS DIMITRIOS G,期刊：Journal of Medicinal Chemistry, 页码：4305-4331 , 文章类型： Article，,卷期：2010年53-11] Emerging Targets in Osteoporosis Disease Modification [作者：ALLEN JOHN G; FOTSCH CHRISTOPHER; BABIJ PHILIP,期刊：Journal of Medicinal Chemistry, 页码：4332-4353 , 文章类型： Article，,卷期：2010年53-11] Structural Insight into Peroxisome Proliferator-Activated Receptor gamma Binding of Two Ureidofibrate-Like Enantiomers by Molecular Dynamics, Cofactor Interaction Analysis, and Site-Directed Mutagenesis [作者：POCHETTI GIORGIO; MITRO NICO; LAVECCHIA ANTONIO; GILARDI FEDERICA; BESKER NEVA; SCOTTI ELENA; ASCHI MASSIMILIANO; RE NAZZARENO; FRACCHIOLLA GIUSEPPE; LAGHEZZA ANTONIO; TORTORELLA PAOLO; MONTANARI ROBERTA; NOVELLINO ETTORE; MAZZA FERNANDO; CRESTANI MAURIZIO; LOIODICE FULVIO,期刊：Journal of Medicinal Chemistry, 页码：4354-4366 , 文章类型： Article，,卷期：2010年53-11] Molecular dynamics simulations were performed on two ureidofibrate-like enantiomers to gain insight into their different potency and efficacy against PPAR gamma. The partial agonism of the Senantiomer seems to be due to ... Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine Aurora Kinase Inhibitors [作者：WANG SHUDONG; MIDGLEY CAROL A; SCAEROU FREDERIC; GRABAREK JOANNA B; GRIFFITHS GARY; JACKSON WAYNE; KONTOPIDIS GEORGE; MCCLUE STEVEN J; MCINNES CAMPBELL; MEADES CHRISTOPHER; MEZNA MOKDAD; PLATER ANDY; STUART IAIN; THOMAS MARK P; WOOD GAVIN; CLARKE ROSEMARY G; BLAKE DAVID G; ZHELEVA DANIELLA I; LANE DAVID P; JACKSON ROBERT C; GLOVER DAVID M; FISCHER PETER M,期刊：Journal of Medicinal Chemistry, 页码：4367-4378 , 文章类型： Article，,卷期：2010年53-11] Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yppyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitoti... Novel Alpha-7 Nicotinic Acetylcholine Receptor Agonists Containing a Urea Moiety: Identification and Characterization of the Potent, Selective, and Orally Efficacious Agonist 1[6-(4-Fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) Urea (SEN34625/WYE-103914) [作者：GHIRON CHIARA; HAYDAR SIMON N; ASCHMIES SUZAN; BOTHMANN HENDRICK; CASTALDO CRISTIANA; COCCONCELLI GIUSEPPE; COMERY THOMAS A; DI LI; DUNLOP JOHN; LOCK TIM; KRAMER ANGELA; KOWAL DIANNE; JOW FLORA; GRAUER STEVE; HARRISON BOYD; LA ROSA SALVATORE; MACCARI LAURA; MARQUIS KAREN L; MICCO IOLANDA; NENCINI ARIANNA; QUINN JOANNA; ROBICHAUD ALBERT J; RONCARATI RENZA; SCALI CARLA; TERSTAPPEN GEORG C; TURLIZZI ELISA; VALACCHI MICHELA; VARRONE MAURIZIO; ZANALETTI RICCARDO; ZANELLI UGO,期刊：Journal of Medicinal Chemistry, 页码：4379-4389 , 文章类型： Article，,卷期：2010年53-11] Alpha-7 nicotinic acetylcholine receptor (alpha 7 nAChR) agonists are promising therapeutic candidates for the treatment of cognitive impairment. We report a series of novel, potent small molecule agonists (4-18) of the ... Turning off Transcription of the bcl-2 Gene by Stabilizing the bcl-2 Promoter Quadruplex with Quindoline Derivatives [作者：WANG XIAODONG; OU TIANMIAO; LU YUJING; LI ZENG; XU ZHENG; XI CHEN; TAN JIAHENG; HUANG SHILIANG; AN LINKUN; LI DING; GU LIANQUAN; HUANG ZHISHU,期刊：Journal of Medicinal Chemistry, 页码：4390-4398 , 文章类型： Article，,卷期：2010年53-11] Human bcl-2 gene is an apoptosis-related oncogene containing a GC-rich sequence which is located upstream from PI promoter and has the potential to form G-quadruplex structures. However, the regulatory role of the quadru... Discovery of Imidazo[1,5-a]pyrido[3,2-e]pyrazines as a New Class of Phosphodiesterase 10A Inhibitiors [作者：HOEFGEN NORBERT; STANGE HANS; SCHINDLER RUDOLF; LANKAU HANSJOACHIM; GRUNWALD CHRISTIAN; LANGEN BARBARA; EGERLAND UTE; TREMMEL PETER; PANGALOS MENELAS N; MARQUIS KAREN L; HAGE THORSTEN; HARRISON BOYD L; MALAMAS MICHAEL S; BRANDON NICHOLAS J; KRONBACH THOMAS,期刊：Journal of Medicinal Chemistry, 页码：4399-4411 , 文章类型： Article，,卷期：2010年53-11] Novel imidazo[1,5-a]pyrido[3,2-e]pyrazines have been synthesized and characterized as both potent and selective phosphodiesterase 10A (PDE 10A) inhibitors. For in vitro characterization, inhibition of PDE10A mediated cAM... Discovery and Structure-Activity Relationship of 3-Methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine(2A) Receptor Inverse Agonist for the Treatment of Arterial Thrombosis [作者：XIONG YIFENG; TEEGARDEN BRADLEY R; CHOI JINSUN KAROLINE; STRAHPLEYNET SONJA; DECAIRE MARC; JAYAKUMAR HONNAPPA; DOSA PETER I; CASPER MARTIN D; PHAM LAN; FEICHTINGER KONRAD; ULLMAN BRETT; ADAMS JOHN; YUSKIN DIANE; FRAZER JOHN; MORGAN MICHAEL; SADEQUE ABU; CHEN WEICHAO; WEBB ROBERT R; CONNOLLY DANIEL T; SEMPLE GRAEME; ALSHAMMA HUSSIEN,期刊：Journal of Medicinal Chemistry, 页码：4412-4421 , 文章类型： Article，,卷期：2010年53-11] Serotonin, which is stored in platelets and is released during thrombosis, activates platelets via the 5-HT2A receptor. 5-HT2A receptor inverse agonists thus represent a potential new class of antithrombotic agents. Our ...