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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16条记录   Optimization of the First Selective Steroid-11 beta-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases [作者：HILLE ULRIKE E; ZIMMER CHRISTINA; HAUPENTHAL JOERG; HARTMANN ROLF W,期刊：ACS Medicinal Chemistry Letters, 页码：559-564 , 文章类型： Article，,卷期：2011年2-8] CYP11B1 is the key enzyme in cortisol biosynthesis, and its inhibition with selective compounds is a promising strategy for the treatment of diseases associated with elevated cortisol levels, such as Cushing's syndrome o... Rigid Analogues of Antimitotic Indolobenzazepinones: New Insights into Tubulin Binding via Molecular Modeling [作者：PONS VALERIE; BEAUMONT STEPHANE; DAU MARIE ELISE TRAN HUU; IORGA BOGDAN I; DODD ROBERT H,期刊：ACS Medicinal Chemistry Letters, 页码：565-570 , 文章类型： Article，,卷期：2011年2-8] Two rigid analogues of 5-ethylindolobenzazepinone 4, a potent c-ytotoxic agent and inhibitor of tubulin polymerization, were prepared. The first was the indane derivative 5, in which the ethyl group is attached to the be... Bivalent Ligands for the Serotonin 5-HT(3) Receptor [作者：CAPPELLI ANDREA; MANINI MONICA; PAOLINO MARCO; GALLELLI ANDREA; ANZINI MAURIZIO; MENNUNI LAURA; DEL CADIA MARTA; DE RIENZO FRANCESCA; MENZIANI M CRISTINA; VOMERO SALVATORE,期刊：ACS Medicinal Chemistry Letters, 页码：571-576 , 文章类型： Article，,卷期：2011年2-8] The serotonin 5-HT(3) receptor is a ligand-gated ion channel, which by virtue of its pentameric architecture, can be considered to be an intriguing example of intrinsically multivalent biological receptors. This paper de... Identification of NAE Inhibitors Exhibiting Potent Activity in Leukemia Cells: Exploring the Structural Determinants of NAE Specificity [作者：LUKKARILA JULIE L; DA SILVA SARA R; ALI MOHSIN; SHAHANI VIJAY M; XU G WEI; BERMAN JUDD; ROUGHTON ANDREW; DHEPAGANON SIRANO; SCHIMMER AARON D; GUNNING PATRICK T,期刊：ACS Medicinal Chemistry Letters, 页码：577-582 , 文章类型： Article，,卷期：2011年2-8] MLN4924 is a selective inhibitor of the NEDD8-activating enzyme (NAE) and has advanced into clinical trials for the treatment of both solid and hematological malignancies. In contrast, the structurally similar compound 1... Combination of a Beta Adrenoceptor Modulator and a Norepinephrine-Serotonin Uptake Inhibitor for the Treatment of Obesity [作者：JESUDASON CYNTHIA D; BAKER JAMES E; BRYANT ROBERT D; FISHER JACK W; OFARRELL LIBBEY S; GAICH GREGORY A; HE MINXIA M; KAHL STEVEN D; KRIAUCIUNAS AIDAS V; HEIMAN MARK L; PETERS MARY A; RITO CHRISTOPHER J; SATTERWHITE JULIE H; TINSLEY FRANK C; TRANKLE WILLIAM G; SHUKER ANTHONY J,期刊：ACS Medicinal Chemistry Letters, 页码：583-586 , 文章类型： Article，,卷期：2011年2-8] We report the novel combination of a selective beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor (sibutrarnine) with potential for the treatment of obesity. The synthesis and characterization of... Quantification of Interactions between Serum Albumin and Endogenous Free Fatty Acids or Exogenous Chemicals by Stable Isotope-Coded Mass Spectrometry [作者：LI TINGTING; YUE YINGXIA; LI JIANJIAN; WANG XIAOLI; FU JIEYING; ZHONG HONGYING,期刊：ACS Medicinal Chemistry Letters, 页码：587-591 , 文章类型： Article，,卷期：2011年2-8] As primary endogenous ligands of serum albumin, free fatty acids exert versatile effects on the albumin conformation through cooperative or competitive interactions with exogenous chemicals. Based on equilibrium partitio... Screening for Dimethylarginine Dimethylaminohydrolase Inhibitors Reveals Ebselen as a Bioavailable Inactivator [作者：LINSKY THOMAS; WANG YUN; FAST WALTER,期刊：ACS Medicinal Chemistry Letters, 页码：592-596 , 文章类型： Article，,卷期：2011年2-8] Dimethylarginine dimethylaminohydrolase (DDAH) is an endogenous regulator of nitric oxide production and represents a potential therapeutic target. However, only a small number of biologically useful inhibitors have been... Agonists for the Chemokine Receptor CXCR4 [作者：LEFRANCOIS MARILOU; LEFEBVRE MARIEREINE; SAINTONGE GENEVIEVE; BOULAIS PHILIP E; LAMOTHE SIMON; LEDUC RICHARD; LAVIGNE PIERRE; HEVEKER NIKOLAUS; ESCHER EMANUEL,期刊：ACS Medicinal Chemistry Letters, 页码：597-602 , 文章类型： Article，,卷期：2011年2-8] The development of agonists for the chemokine receptor CXCR4 could provide promising therapeutic candidates. On the basis of previously forwarded two site model of chemoldne-receptor interactions, we hypothesized that li... Design and Synthesis of Benzenesulfonamide Derivatives as Potent Anti-Influenza Hemagglutinin Inhibitors [作者：TANG GUOZHI; LIN XIANFENG; QIU ZONGXING; LI WENTAO; ZHU LEI; WANG LISHA; LI SHAOHUA; LI HAODONG; LIN WENBIN; YANG MEI; GUO TAO; CHEN LI; LEE DANIEL; WU JIM Z; YANG WENGANG,期刊：ACS Medicinal Chemistry Letters, 页码：603-607 , 文章类型： Article，,卷期：2011年2-8] Structural optimization of salicylamide-based hemagglutinin (HA) inhibitor 1 resulted in the identification of cis-3-(5-hydroxy-1,3,3-timethylcyclohexylmethylamino)benzenesulfonamide 28 and its derivatives as potent anti... A Strategy for Suppressing Redox Stress within Mitochondria [作者：ARCE PABLO M; KHDOUR OMAR M; GOLDSCHMIDT RUTH; ARMSTRONG JEFFREY S; HECHT SIDNEY M,期刊：ACS Medicinal Chemistry Letters, 页码：608-613 , 文章类型： Article，,卷期：2011年2-8] An aza analogue (1) of the experimental neuroprotective drug idebenone has been prepared and evaluated. The compound quenches lipid peroxidation more effectively than a-tocopherol and potently suppresses reactive oxygen ... The myo-1,2-Diaminocyclitol Scaffold Defines Potent Glucocerebrosidase Activators and Promising Pharmacological Chaperones for Gaucher Disease [作者：TRAPERO ANA; LLEBARIA AMADEU,期刊：ACS Medicinal Chemistry Letters, 页码：614-619 , 文章类型： Article，,卷期：2011年2-8] A series of cyclitol derivatives with myo-configuration are beta-glucocerebrosidase (GCase) inhibitors and show excellent characteristics for the development of pharmacological chaperones for enzyme deficiency in Gaucher... CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist [作者：CHEN JIANYONG; COLLINS GREGORY T; LEVANT BETH; WOODS JAMES; DESCHAMPS JEFFREY R; WANG SHAOMENG,期刊：ACS Medicinal Chemistry Letters, 页码：620-625 , 文章类型： Article，,卷期：2011年2-8] We have identified several ligands with high binding affinities to the dopamine D3 receptor and excellent selectivity over the D2 and D1 receptors. CJ-1639 (17) binds to the D3 receptor with a K(i) value of 0.50 nM and d... Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element [作者：TOSH DILIP K; PHAN KHAI; DEFLORIAN FRANCESCA; WEI QIANG; GAO ZHANGUO; JACOBSON KENNETH A,期刊：ACS Medicinal Chemistry Letters, 页码：626-631 , 文章类型： Article，,卷期：2011年2-8] A(1) adenosine receptor (AR) agonists are neuroprotective, cardioprotective, and anxiolytic. (N)-Methanocarba adenine nucleosides designed to bind to human A(1)AR were truncated to eliminate 5'-CH(2)OH. This modification... Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors [作者：HUANG XIAOHUA; SHIPPS GERALD W JR; CHENG CLIFF C; SPACCIAPOLI PETER; ZHANG XINGMIN; MCCOY MARK A; WYSS DANIEL F; YANG XIANSHU; ACHAB ABDELGHANI; SOUCY KYLE; MONTAVON DONNA K; MURPHY DENISE M; WHITEHURST CHARLES E,期刊：ACS Medicinal Chemistry Letters, 页码：632-637 , 文章类型： Article，,卷期：2011年2-8] A novel series of non-ATP-competitive MK2 inhibitors based on a furan-2-carboxyamide scaffold was discovered through high-throughput screening using the affinity selection-mass spectrometry-based Automated Ligand Identif... Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design [作者：SUN HAO; SCOTT DENNIS O,期刊：ACS Medicinal Chemistry Letters, 页码：638-643 , 文章类型： Article，,卷期：2011年2-8] 4-Aminopiperidines are a variety of therapeutic agents that are extensively metabolized by cytochrome P450s with CYP3A4 as a major isoform catalyzing their N-dealkylation reaction. However, its catalytic mechanism has no... Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists [作者：CROSIGNANI STEFANO; JORANDLEBRUN CATHERINE; PAGE PATRICK; CAMPBELL GORDON; COLOVRAY VERONIQUE; MISSOTTEN MARC; HUMBERT YVES; CLEVA CHRISTOPHE; ARRIGHI JEANFRANCOIS; GAUDET MARILENE; JOHNSON ZOE; FERRO PAMELA; CHOLLET ANDRE,期刊：ACS Medicinal Chemistry Letters, 页码：644-649 , 文章类型： Article，,卷期：2011年2-8] New spiroindolinone antagonists of CRTH2 are described. Following identification of insufficient stability in human plasma as an important liability of the lead compounds, replacement of the spirosuccinimide core with a ...