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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23条记录   Oral Oxytocin Antagonists [作者：BORTHWICK ALAN D,期刊：Journal of Medicinal Chemistry, 页码：6525-6538 , 文章类型： Article，,卷期：2010年53-18] Novel Approaches for Targeting Thymidylate Synthase To Overcome the Resistance and Toxicity of Anticancer Drugs [作者：GARG DIVITA; HENRICH STEFAN; SALOAHEN OUTI M H; MYLLYKALLIO HANNU; COSTI MARIA P; WADE REBECCA C,期刊：Journal of Medicinal Chemistry, 页码：6539-6549 , 文章类型： Article，,卷期：2010年53-18] Effects of Conformational Restriction of 2-Amino-3-benzoylthiophenes on A(1) Adenosine Receptor Modulation [作者：AURELIO LUIGI; VALANT CELINE; FLYNN BERNARD L; SEXTON PATRICK M; WHITE JONATHAN M; CHRISTOPOULOS ARTHUR; SCAMMELLS PETER J,期刊：Journal of Medicinal Chemistry, 页码：6550-6559 , 文章类型： Article，,卷期：2010年53-18] 2-Amino-3-benzoylthiophenes (2A3BTs) have been widely reported to act as allosteric enhancers (A Es) at the A(1) adenosine receptor (A(1)AR). Herein we describe the synthesis of a series of 1-aminoindeno[1,2-c]thiophen-8... Synthesis, Anti-Inflammatory Activity, and in Vitro Antitumor Effect of a Novel Class of Cyclooxygenase Inhibitors: 4-(Aryloyl)phenyl Methyl Sulfones [作者：HARRAK YOUSSEF; CASULA GIOVANNI; BASSET JOAN; ROSELL GLORIA; PLESCIA SALVATORE; RAFFA DEMETRIO; GRAZIA CUSIMANO MARIA; POUPLANA RAMON; DOLORS PUJOL MARIA,期刊：Journal of Medicinal Chemistry, 页码：6560-6571 , 文章类型： Article，,卷期：2010年53-18] Following our previous research on anti-inflammatory drugs (NSAIDs), we report on the design and synthesis of 4-(aryloyl)phenyl methyl sulfones. These substances were characterized for their capacity to inhibit cyclooxyg... Substituted 4-Carboxymethylpyroglutamic Acid Diamides as Potent and Selective Inhibitors of Fibroblast Activation Protein [作者：TSAI TINGYUEH; YEH TENGKUANG; CHEN XIN; HSU TSU; JAO YUCHEN; HUANG CHIHHSIANG; SONG JENSHIN; HUANG YUCHEN; CHIEN CHIAHUI; CHIU JINGHUAI; YEN SHIHCHIEH; TANG HUNGKUAN; CHAO YUSHENG; JIAANG WEIRTORN,期刊：Journal of Medicinal Chemistry, 页码：6572-6583 , 文章类型： Article，,卷期：2010年53-18] Fibroblast activation protein (FAP) belongs to the prolyl peptidase family. FAP inhibition is expected to become a new antitumor target. Most known FAP inhibitors often resemble the dipeptide cleavage products, with a bo... Discovery of Novel 5-Benzylidenerhodanine and 5-Benzylidenethiazolidine-2,4-dione Inhibitors of MurD Ligase [作者：ZIDAR NACE; TOMASIC TIHOMIR; SINK ROMAN; RUPNIK VERONIKA; KOVAC ANDREJA; TURK SAMO; PATIN DELPHINE; BLANOT DIDIER; MARTEL CARLOS CONTRERAS; DESSEN ANDREA; PREMRU MANICA MUELLER; ZEGA ANAMARIJA; GOBEC STANISLAV; MASIC LUCIJA PETERLIN; KIKELJ DANIJEL,期刊：Journal of Medicinal Chemistry, 页码：6584-6594 , 文章类型： Article，,卷期：2010年53-18] We have designed, synthesized, and evaluated 5-benzylidenerhodanine- and 5-benzylidenethiazolidine-2,4-dione-based compounds as inhibitors of bacterial enzyme MurD with E. coli IC50 in the range 45-206 mu M. The high-res... 4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles That Are Cytotoxic against Combretastatin A Resistant Tumor Cells and Vascular Disrupting in a Cisplatin Resistant Germ Cell Tumor Model [作者：SCHOBERT RAINER; BIERSACK BERNHARD; DIETRICH ANDREA; EFFENBERGER KATHARINA; KNAUER SEBASTIAN; MUELLER THOMAS,期刊：Journal of Medicinal Chemistry, 页码：6595-6602 , 文章类型： Article，,卷期：2010年53-18] New combretastatin A analogues featuring oxazole or N-methylimidazole bridged Z-alkenes and haloor amino-substituted A-rings were tested against various cancer cell lines and in testicular germ cell tumor xenografts in m... (R,S)-anti-1-Amino-2-[F-18]Fluorocyclopentyl-1-carboxylic Acid: Synthesis from Racemic 2-Benzyloxycyclopentanone and Biological Evaluation for Brain Tumor Imaging with Positron Emission Tomography [作者：JARKAS NACHWA; VOLL RONALD J; WILLIAMS LARRY; CAMP VERNON M; GOODMAN MARK M,期刊：Journal of Medicinal Chemistry, 页码：6603-6607 , 文章类型： Article，,卷期：2010年53-18] (R,S)-anti-1-Amino-2-fluorocyclopentyl-1-carboxylic acid (2-FACPC, 4b) was radiolabeled in 39% yield starting from cyclic sulfamidate 12. The 9L gliosarcoma cells assays showed that 4b is mainly a substrate for the L-typ... 3 '-Deoxy Phosphoramidate Dinucleosides as Improved Inhibitors of Hepatitis C Virus Subgenomic Replicon and NS5B Polymerase Activity [作者：PRIET STEPHANE; ZLATEV IVAN; BARVIK IVAN JR; GEERTS KATRIEN; LEYSSEN PIETER; NEYTS JOHAN; DUTARTRE HELENE; CANARD BRUNO; VASSEUR JEANJACQUES; MORVAN FRANCOIS; ALVAREZ KARINE,期刊：Journal of Medicinal Chemistry, 页码：6608-6617 , 文章类型： Article，,卷期：2010年53-18] Phosphoramidate dinucleosides named "GC 3'-OH" series, carrying various phosphoramidate linkages have been previously reported as hepatitis C virus (HCV) inhibitors. To enhance the efficacy of these dinucleotides, we syn... Discovery of Mitogen-Activated Protein Kinase-Interacting Kinase 1 Inhibitors by a Comprehensive Fragment-Oriented Virtual Screening Approach [作者：OYARZABAL JULEN; ZARICH NATASHA; ISABEL ALBARRAN MARIA; PALACIOS IRENE; URBANOCUADRADO MANUEL; MATEOS GENOVEVA; REYMUNDO ISABEL; RABAL OBDULIA; SALGADO ANTONIO; CORRIONERO ANA; FOMINAYA JESUS; PASTOR JOAQUIN; BISCHOFF JAMES R,期刊：Journal of Medicinal Chemistry, 页码：6618-6628 , 文章类型： Article，,卷期：2010年53-18] Mitogen-activated protein kinase-interacting kinases 1 and 2 (MNK 1 and MNK 2) phosphorylate the oncogene eI F4E on serine 209. This phosphorylation has been reported to be required for its oncogenic activity. To investi... Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38 alpha MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases [作者：LIU CHUNJIAN; LIN JAMES; WROBLESKI STEPHEN T; LIN SHUQUN; HYNES JOHN JR; WU HONG; DYCKMAN ALARIC J; LI TIANLE; WITYAK JOHN; GILLOOLY KATHLEEN M; PITT SIDNEY; SHEN DING REN; ZHANG ROSEMARY F; MCINTYRE KIM W; SALTERCID LUISA; SHUSTER DAVID J; ZHANG HONGJIAN; MARATHE PUNIT H; DOWEYKO ARTHUR M; SACK JOHN S; KIEFER SUSAN E; KISH KEVIN F; NEWITT JOHN A; MCKINNON MURRAY; DODD JOHN H; BARRISH JOEL C; SCHIEVEN GARY L; LEFTHERIS KATERINA,期刊：Journal of Medicinal Chemistry, 页码：6629-6639 , 文章类型： Article，,卷期：2010年53-18] The discovery and characterization of 7k (BMS-582949), a highly selective p38 alpha, MAP kinase inhibitor that is currently in phase H clinical trials for the treatment of rheumatoid arthritis, is described, A key to the... Inhalation by Design: Novel Ultra-Long-Acting beta(2)-Adrenoreceptor Agonists for Inhaled Once-Daily Treatment of Asthma and Chronic Obstructive Pulmonary Disease That Utilize a Sulfonamide Agonist Headgroup [作者：GLOSSOP PAUL A; LANE CHARLOTTE A L; PRICE DAVID A; BUNNAGE MARK E; LEWTHWAITE RUSSELL A; JAMES KIM; BROWN ALAN D; YEADON MICHAEL; PERROSHUGUET CHRISTELLE; TREVETHICK MICHAEL A; CLARKE NICHOLAS P; WEBSTER ROBERT; JONES RHYS M; BURROWS JANE L; FEEDER NEIL; TAYLOR STEFAN C J; SPENCE FIONA J,期刊：Journal of Medicinal Chemistry, 页码：6640-6652 , 文章类型： Article，,卷期：2010年53-18] A novel series of potent and selective sulfonamide derived beta(2)-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstruc... Orally Active MMP-1 Sparing alpha-Tetrahydropyranyl and alpha-Piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease [作者：BECKER DANIEL P; BARTA THOMAS E; BEDELL LOUIS J; BOEHM TERRI L; BOND BRIAN R; CARROLL JEFFERY; CARRON CHRIS P; DECRESCENZO GARY A; EASTON ALAN M; FRESKOS JOHN N; FUNCKESSHIPPY CHRIS L; HERON MARCIA; HOCKERMAN SUSAN; HOWARD CAROL PEARCY; KIEFER JAMES R; LI MADELEINE H; MATHIS KARL J; MCDONALD JOSEPH J; MEHTA PRAMOD P; MUNIE GRACE E; SUNYER TERESA; SWEARINGEN CRAIG A; VILLAMIL CLARA I; WELSCH DEAN; WILLIAMS JENNIFER M; YU YING; YAO JUN,期刊：Journal of Medicinal Chemistry, 页码：6653-6680 , 文章类型： Article，,卷期：2010年53-18] alpha-Sulfone-alpha-piperidine and alpha-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP's-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ve... Nonsteroidal Dissociated Glucocorticoid Agonists Containing Azaindoles as Steroid A-Ring Mimetics [作者：RIETHER DORIS; HARCKEN CHRISTIAN; RAZAVI HOSSEIN; KUZMICH DANIEL; GILMORE THOMAS; BENTZIEN JOERG; PACK EDWARD J JR; SOUZA DONALD; NELSON RICHARD M; KUKULKA ALISON; FADRA TAZMEEN N; ZUVELAJELASKA LJILJANA; PELLETIER JOSEPHINE; DINALLO ROGER; PANZENBECK MARK; TORCELLINI CAROL; NABOZNY GERALD H; THOMSON DAVID S,期刊：Journal of Medicinal Chemistry, 页码：6681-6698 , 文章类型： Article，,卷期：2010年53-18] Syntheses and structure activity relationships (SA R) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in v... Antitumor Agents. 280. Multidrug Resistance-Selective Desmosdumotin B Analogues [作者：NAKAGAWAGOTO KYOKO; CHANG POCHENG; LAI CHINYU; HUNG HSINYI; CHEN TZUHSUAN; WU PEICHI; ZHU HAO; SEDYKH ALEXANDER; BASTOW KENNETH F; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：6699-6705 , 文章类型： Article，,卷期：2010年53-18] 6,6,8-Triethyldesmosdumotin B (2) was discovered as a MDR-selective flavonoid with significant in vitro anticancer activity against a multidrug resistant (MDR) cell line (KB-VIN) but without activity against the parent c... Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor [作者：LAVIERI ROBERT R; SCOTT SARAH A; SELVY PAIGE E; KIM KWANGHO; JADHAV SATYAWAN; MORRISON RYAN I; DANIELS J SCOTT; BROWN H ALEX; LINDSLEY CRAIG W,期刊：Journal of Medicinal Chemistry, 页码：6706-6719 , 文章类型： Article，,卷期：2010年53-18] Phospholipase D (PLD) catalyzes the conversion of phosphatidylcholine to the lipid second messenger phosphatidic acid. Two mammalian isoforms of PLD have been identified, PLD I and PLD2, which share 53% sequence identity...