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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33条记录   Structure-Activity Relationships of Cycloalkylamide Derivatives as Inhibitors of the Soluble Epoxide Hydrolase [作者：KIM INHAE; PARK YONGKYU; HAMMOCK BRUCE D; NISHI KOSUKE,期刊：Journal of Medicinal Chemistry, 页码：1752-1761 , 文章类型： Article，,卷期：2011年54-6] Structure-activity relationships of cycloalkylamide compounds as inhibitors of human sEH were investigated. When the left side of amide function was modified by a variety of cycloalkanes, at least a C6 like cyclohexane w... Tricyclic Compounds Containing Nonenolizable Cyano Enones. A Novel Class of Highly Potent Anti-Inflammatory and Cytoprotective Agents [作者：HONDA TADASHI; YOSHIZAWA HIDENORI; SUNDARARAJAN CHITRA; DAVID EMILIE; LAJOIE MARC J; FAVALORO FRANK G JR; JANOSIK TOMASZ; SU XIAOBO; HONDA YUKIKO; ROEBUCK BILL D; GRIBBLE GORDON W,期刊：Journal of Medicinal Chemistry, 页码：1762-1778 , 文章类型： Article，,卷期：2011年54-6] Forty-four novel tricycles containing nonenolizable cyano enones (TCEs) were designed and synthesized on the basis of a semisynthetic pentacyclic triterpenoid, bardoxolone methyl, which is currently being developed in ph... Zwitterionic CRTh2 Antagonists [作者：LUKER TIM; BONNERT ROGER; PAINE STUART W; SCHMIDT JERZY; SARGENT CAROL; COOK ANTHONY R; COOK ANDREW; GARDINER PHILIP; HILL STEVE; WEYMANJONES CAROL; PATEL ANIL; THOM STEPHEN; THORNE PHILIP,期刊：Journal of Medicinal Chemistry, 页码：1779-1788 , 文章类型： Article，,卷期：2011年54-6] A novel series of zwitterions is reported that contains potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A high quality lead compound 2 was di... Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors [作者：DANGELO NOEL D; KIM TAESEONG; ANDREWS KRISTIN; BOOKER SHON K; CAENEPEEL SEAN; CHEN KUI; DAMICO DERIN; FREEMAN DAN; JIANG JIAN; LIU LONGBIN; MCCARTER JOHN D; MIGUEL TISHA SAN; MULLADY ERIN L; SCHRAG MICHAEL; SUBRAMANIAN RAJU; TANG JIN; WAHL ROBERT C; WANG LING; WHITTINGTON DOUGLAS A; WU TIAN; XI NING; XU YANG; YAKOWEC PETER; YANG KEVIN; ZALAMEDA LEEANNE P; ZHANG NANCY; HUGHES PAUL; NORMAN MARK H,期刊：Journal of Medicinal Chemistry, 页码：1789-1811 , 文章类型： Article，,卷期：2011年54-6] Phosphoinositide 3-kinase alpha (Pi3K alpha) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of m... Magnesium Chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-diones, as Inhibitors of HIV-1 Integrase and/or the HIV-1 Reverse Transcriptase Ribonuclease H Domain: Discovery of a Novel Selective Inhibitor of the Ribonuclease H Function [作者：BILLAMBOZ MURIEL; BAILLY FABRICE; LION CEDRIC; TOUATI NADIA; VEZIN HERVE; CALMELS CHRISTINA; ANDREOLA MARIELINE; CHRIST FRAUKE; DEBYSER ZEGER; COTELLE PHILIPPE,期刊：Journal of Medicinal Chemistry, 页码：1812-1824 , 文章类型： Article，,卷期：2011年54-6] 2-Hydroxyisoquinoline-1,3(2H,4H)-dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction wit... Peptide-Based Imaging Agents Targeting Phosphatidylserine for the Detection of Apoptosis [作者：XIONG CHIYI; BREWER KARI; SONG SHAOLI; ZHANG RUI; LU WEI; WEN XIAOXIA; LI CHUN,期刊：Journal of Medicinal Chemistry, 页码：1825-1835 , 文章类型： Article，,卷期：2011年54-6] A 14-residue phosphatidylserine (PS)-binding peptide FNFRLKAGQIURFG (PSBP-0) was scanned with Ala. In addition, a radiometal chelator (SAAC) was introduced at selected sites of the lead peptides. Substitution of the Gln(... Design and Optimization of Potent and Orally Bioavailable Tetrahydronaphthalene Raf Inhibitors [作者：GOULD ALEXANDRA E; ADAMS RUTH; ADHIKARI SHARMILA; AERTGEERTS KATHLEEN; AFROZE ROUSHAN; BLACKBURN CHRISTOPHER; CALDERWOOD EMILY F; CHAU RYAN; CHOUITAR JOUHARA; DUFFEY MATTHEW O; ENGLAND DYLAN B; FARRER CHERYL; FORSYTH NANCY; GARCIA KHRISTOFER; GAULIN JEFFERY; GREENSPAN PAUL D; GUO RIBO; HARRISON SEAN J; HUAN SHIHCHUNG; IARTCHOUK NATALIA; JANOWICK DAVE; KIM MISOOK; KULKARNI BHEEMASHANKAR; LANGSTON STEVEN P; LIU JANE X; MA LITING; MENON SAURABH; MIZUTANI HIROTAKE; PASKE ERIN; RENOU CHRISTELLE C; REZAEI MANSOUREH; ROWLAND R SCOTT; SINTCHAK MICHAEL D; SMITH MICHAEL D; STROUD STEPHEN G; TREGAY MING; TIAN YUAN; VEIBY OLE P; VOS TRICIA J; VYSKOCIL STEPAN; WILLIAMS JULIET; XU TIANLIN; YANG JOHNNY J; YANO JASON; ZENG HONGBO; ZHANG DONG MEI; ZHANG QIN; GALVIN KATHERINE M,期刊：Journal of Medicinal Chemistry, 页码：1836-1846 , 文章类型： Article，,卷期：2011年54-6] Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatmen... Nucleoside Transport Inhibitors: Structure-Activity Relationships for Pyrimido[5,4-d]pyrimidine Derivatives That Potentiate Pemetrexed Cytotoxicity in the Presence of alpha(1)-Acid Glycoprotein [作者：SARAVANAN KAPPUSAMY; BARLOW HANNAH C; BARTON MARION; CALVERT A HILARY; GOLDING BERNARD T; NEWELL DAVID R; NORTHEN JULIAN S; CURTIN NICOLA J; THOMAS HUW D; GRIFFIN ROGER J,期刊：Journal of Medicinal Chemistry, 页码：1847-1859 , 文章类型： Article，,卷期：2011年54-6] Membrane transport of nucleosides or nucleobases is mediated by transporters including the equilibrative nucleoside transporters (ENTs), and resistance to antitumor antimetabolite drugs may arise via salvage of exogenous... Radiosynthesis and Biological Evaluation of L- and D-S-(3-[F-18]Fluoropropyl)homocysteine for Tumor Imaging Using Positron Emission Tomography [作者：BOURDIER THOMAS; SHEPHERD RACHAEL; BERGHOFER PAULA; JACKSON TIMOTHY; FOOKES CHRISTOPHER J R; DENOYER DELPHINE; DOROW DONNA S; GREGURIC IVAN; GREGOIRE MARIECLAUDE; HICKS RODNEY; KATSIFIS ANDREW,期刊：Journal of Medicinal Chemistry, 页码：1860-1870 , 文章类型： Article，,卷期：2011年54-6] Interest in radiolabeled amino acids for metabolic imaging of cancer and limitations with [C-11]methionine has prompted the development of a new F-18-labeled methionine derivative S-(3-[F-18]fluoropropyl)homocysteine ([F... Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors [作者：MEDINA JESUS R; BECKER CHRISTOPHER J; BLACKLEDGE CHARLES W; DUQUENNE CELINE; FENG YANHONG; GRANT SETH W; HEERDING DIRK; LI WILLIAM H; MILLER WILLIAM H; ROMERIL STUART P; SCHERZER DARYL; SHU ARTHUR; BOBKO MARK A; CHADDERTON ANTONY R; DUMBLE MELISSA; GARDINER CHRISTINE M; GILBERT SETH; LIU QI; RABINDRAN SRIDHAR K; SUDAKIN VALERY; XIANG HONG; BRADY PAT G; CAMPOBASSO NINO; WARD PARIS; AXTEN JEFFREY M,期刊：Journal of Medicinal Chemistry, 页码：1871-1895 , 文章类型： Article，,卷期：2011年54-6] Phosphoinositide-dependent protein kinase-1 (PDK1) is a master regulator of the AGC family of kinases and an integral component of the PI3K/AKT/mTOR pathway. As this pathway is among the most commonly deregulated across ... Ureido-Substituted Benzenesulfonamides Potently Inhibit Carbonic Anhydrase IX and Show Antimetastatic Activity in a Model of Breast Cancer Metastasis [作者：PACCHIANO FABIO; CARTA FABRIZIO; MCDONALD PAUL C; LOU YUANMEI; VULLO DANIELA; SCOZZAFAVA ANDREA; DEDHAR SHOUKAT; SUPURAN CLAUDIU T,期刊：Journal of Medicinal Chemistry, 页码：1896-1902 , 文章类型： Article，,卷期：2011年54-6] A series of ureido-substituted benzenesulfonamides was prepared that showed a very interesting profile for the inhibition of several human carbonic anhydrases (hCAs, EC 4.2.1.1), such as hCAs land II (cytosolic: isoforms... Aminothiazolomorphinans with Mixed kappa and mu Opioid Activity [作者：ZHANG TANGZHI; YAN ZHAOHUA; SROMEK ANNA; KNAPP BRIAN I; SCRIMALE THOMAS; BIDLACK JEAN M; NEUMEYER JOHN L,期刊：Journal of Medicinal Chemistry, 页码：1903-1913 , 文章类型： Article，,卷期：2011年54-6] A series of N-substituted and N'-substituted aminothiazole-derived morphinans (5) were synthesized for expanding the structure activity relationships of aminothiazolo-morphinans. Although their affinities were somewhat l... Quinazoline Sulfonamides as Dual Binders of the Proteins B-Cell Lymphoma 2 and B-Cell Lymphoma Extra Long with Potent Proapoptotic Cell-Based Activity [作者：SLEEBS BRAD E; CZABOTAR PETER E; FAIRBROTHER WAYNE J; FAIRLIE W DOUGLAS; FLYGARE JOHN A; HUANG DAVID C S; KERSTEN WILHELMUS J A; KOEHLER MICHAEL F T; LESSENE GUILLAUME; LOWES KYM; PARISOT JOHN P; SMITH BRIAN J; SMITH MOREY L; SOUERS ANDREW J; STREET IAN P; YANG HONG; BAELL JONATHAN B,期刊：Journal of Medicinal Chemistry, 页码：1914-1926 , 文章类型： Article，,卷期：2011年54-6] ABT-737 and ABT-263 are potent inhibitors of the BH3 antiapoptotic proteins, Bcl-x(L) and Bcl-2. This class of putative anticancer agents invariantly contains an acylsulfonamide core. We have designed and synthesized a s... Dipeptidyl Peptidase IV Dependent Water-Soluble Prodrugs of Highly Lipophilic Bicyclic Nucleoside Analogues [作者：DIEZTORRUBIA ALBERTO; BALZARINI JAN; ANDREI GRACIELA; SNOECK ROBERT; DE MEESTER INGRID; CAMARASA MARIAJOSE; VELAZQUEZ SONSOLES,期刊：Journal of Medicinal Chemistry, 页码：1927-1942 , 文章类型： Article，,卷期：2011年54-6] We present the first report of the application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to hydroxy-containing drug derivatives. In particular, we applied this strategy to the highly lipophilic a... A Class of 5-Benzylidene-2-phenylthiazolinones with High Potency as Direct 5-Lipoxygenase Inhibitors [作者：HOFMANN BETTINA; BARZEN SEBASTIAN; ROEDL CARMEN B; KIEHL ANDREAS; BORIG JULIA; ZIVKOVIC ALEKSANDRA; STARK HOLGER; SCHNEIDER GISBERT; STEINHILBER DIETER,期刊：Journal of Medicinal Chemistry, 页码：1943-1947 , 文章类型： Article，,卷期：2011年54-6] A novel class of potent direct 5-lipoxygenase (5-LO) inhibitors bearing a thiazolinone-scaffold identified by virtual screening is presented. A range of substitutions and the importance of the 2-phenyl moiety were evalua... Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response [作者：MCCLURE KIM F; DAROUT ETZER; GUIMARAES CRISTIANO R W; DENINNO MICHAEL P; MASCITTI VINCENT; MUNCHHOF MICHAEL J; ROBINSON RALPH P; KOHRT JEFFREY; HARRIS ANTHONY R; MOORE DIANNA E; LI BRYAN; SAMP LACEY; LEFKER BRUCE A; FUTATSUGI KENTARO; KUNG DANIEL; BONIN PAUL D; CORNELIUS PETER; WANG RUDUAN; SALTER EBEN; HORNBY SAM; KALGUTKAR AMIT S; CHEN YUE,期刊：Journal of Medicinal Chemistry, 页码：1948-1952 , 文章类型： Article，,卷期：2011年54-6] The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These result...