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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18条记录   Cracking the Code: The Promise of Epigenetics [作者：DHANAK DASHYANT,期刊：ACS Medicinal Chemistry Letters, 页码：521-523 , 文章类型： Editorial Material，,卷期：2012年3-7] Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors [作者：LIN HONG; SCHULZ MARK J; XIE REN; ZENG JIN; LUENGO JUAN I; SQUIRE MICHAEL D; TEDESCO ROSANNA; QU JUNYA; ERHARD KARL; MACK JAMES F; RAHA KAUSHIK; PLANT RAMONA; ROMINGER CYNTHIA M; ARIAZI JENNIFER L; SHERK CHRISTIAN S; SCHABER MICHAEL D; MCSURDYFREED JEANELLE; SPENGLER MICHAEL D; DAVIS CHARLES B; HARDWICKE MARY ANN; RIVERO RALPH A,期刊：ACS Medicinal Chemistry Letters, 页码：524-529 , 文章类型： Article，,卷期：2012年3-7] A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast can... Design and Synthesis of Potent, Selective Inhibitors of Matriptase [作者：COLOMBO ELOIC; DESILETS ANTOINE; DUCHENE DOMINIC; CHAGNON FELIX; NAJMANOVICH RAFAEL; LEDUC RICHARD; MARSAULT ERIC,期刊：ACS Medicinal Chemistry Letters, 页码：530-534 , 文章类型： Article，,卷期：2012年3-7] Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a... Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect [作者：DEL BELLO FABIO; DIAMANTI ELEONORA; GIANNELLA MARIO; MAMMOLI VALERIO; MARCHIORO CARLA; MATTIOLI LAURA; TITOMANLIO FEDERICA; PIERGENTILI ALESSANDRO; QUAGLIA WILMA; BENEDETTI GIOVANNI; VARRONE MAURIZIO; PIGINI MARIA,期刊：ACS Medicinal Chemistry Letters, 页码：535-539 , 文章类型： Article，,卷期：2012年3-7] This study demonstrated that cyclomethyline (2) and the corresponding enantiomers (R)-(-)-2 and (S)-(+)-2, displaying alpha(2C)-adrenoreceptor. (AR) agonism/alpha(2A)-AR antagonism, similarly to allyphenyline (1) and its... Identification of New Snake Venom Metalloproteinase Inhibitors Using Compound Screening and Rational Peptide Design [作者：VILLATAROMERO FABIAN; GORTAT ANNA; HERRERA ANDRES E; ARGUEDAS REBECA; QUESADA JAVIER; LOPES DE MELO ROBSON; CALVETE JUAN J; MONTERO MAVIS; MURILLO RENATO; RUCAVADO ALEXANDRA; MARIA GUTIERREZ JOSE; PEREZPAYA ENRIQUE,期刊：ACS Medicinal Chemistry Letters, 页码：540-543 , 文章类型： Article，,卷期：2012年3-7] The majority of snakebite envenomations in Central America are caused by the viperid species Bothrops asper, whose venom contains a high proportion of zinc dependent metalloproteinases that play a relevant role in the pa... Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators as Novel Tools for in Vivo Investigation [作者：KECK THOMAS M; ZOU MUFA; ZHANG PENG; RUTLEDGE REBECCA P; NEWMAN AMY HAUCK,期刊：ACS Medicinal Chemistry Letters, 页码：544-549 , 文章类型： Article，,卷期：2012年3-7] Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGluR5) have shown promising results in preclinical models for anxiety and drug abuse. Here, we describe a series of aryl substituted al... Synthesis and Agonistic Activity at the GPR35 of 5,6-Dihydroxyindole-2-carboxylic Acid Analogues [作者：DENG HUAYUN; FANG YE,期刊：ACS Medicinal Chemistry Letters, 页码：550-554 , 文章类型： Article，,卷期：2012年3-7] 5,6-Dihydroxyindole-2-carboxylic acid (DHICA), an intermediate of melanin synthesis and an eumelanin building block, was recently discovered to be a GPR35 agonist with moderate potency. Here, we report the synthesis and ... Novel 4-Aminoquinoline-Pyrimidine Based Hybrids with Improved in Vitro and in Vivo Antimalarial Activity [作者：MANOHAR SUNNY; RAJESH U CHINNA; KHAN SHABANA I; TEKWANI BABU L; RAWAT DIWAN S,期刊：ACS Medicinal Chemistry Letters, 页码：555-559 , 文章类型： Article，,卷期：2012年3-7] A class of hybrid molecules consisting of 4-aminoquinoline and pyrimidine were synthesized and tested for antimalarial activity against both chloroquine (CQ)-sensitive (D6) and chloroquine (CQ)-resistant (W2) strains of ... Diaminopyridine-Based Potent and Selective Mps1 Kinase Inhibitors Binding to an Unusual Flipped-Peptide Conformation [作者：KUSAKABE KENICHI; IDE NOBUYUKI; DAIGO YATARO; ITOH TAKESHI; HIGASHINO KENICHI; OKANO YOUSUKE; TADANO GENTA; TACHIBANA YUKI; SATO YUJI; INOUE MAKIKO; WADA TOORU; IGUCHI MOTOFUMI; KANAZAWA TAKAYUKI; ISHIOKA YUKICHI; DOHI KEIJI; TAGASHIRA SACHIE; KIDO YASUTO; SAKAMOTO SHINGO; YASUO KAZUYA; MAEDA MASAHIRO; YAMAMOTO TAKAHIKO; HIGAKI MASAYO; ENDOH TAKESHI; UEDA KAZUO; SHIOTA TAKESHI; MURAI HITOSHI; NAKAMURA YUSUKE,期刊：ACS Medicinal Chemistry Letters, 页码：560-564 , 文章类型： Article，,卷期：2012年3-7] Monopolar spindle 1 (Mps1) is an attractive cancer drug target due to the important role that it plays in centrosome duplication, the spindle assembly checkpoint, and the maintenance of chromosomal stability. A design ba... Imidazo[1,2-a]pyridines That Directly Interact with Hepatitis C NS4B: Initial Preclinical Characterization [作者：SHOTWELL J BRAD; BASKARAN SUBRAMANIAN; CHONG PEK; CREECH KATRINA L; CROSBY RENAE M; DICKSON HAMILTON; FANG JING; GARRIDO DULCE; MATHIS AMANDA; MAUNG JACK; PARKS DEREK J; POULIOT JEFFREY J; PRICE DANIEL J; RAI ROOPA; SEAL JOHN W III; SCHMITZ ULI; TAI VINCENT W F; THOMSON MICHAEL; XIE MI; XIONG ZHIPING Z; PEAT ANDREW J,期刊：ACS Medicinal Chemistry Letters, 页码：565-569 , 文章类型： Article，,卷期：2012年3-7] A series of imidazo[1,2-a]pyridines which directly bind to HCV Non-Structural Protein 4B (NS4B) is described. This series demonstrates potent in vitro inhibition of HCV replication (EC50 < 10 nM), direct binding to purif... Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry [作者：EDLIN CHRIS D; MORGANS GARRETH; WINKS SUSAN; DUFFY SANDRA; AVERY VICKY M; WITTLIN SERGIO; WATERSON DAVID; BURROWS JEREMY; BRYANS JUSTIN,期刊：ACS Medicinal Chemistry Letters, 页码：570-573 , 文章类型： Article，,卷期：2012年3-7] Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains identified several novel chemo... Synthesis and Functionalization of Cyclic Sulfonimidamides: A Novel Chiral Heterocyclic Carboxylic Acid Bioisostere [作者：PEMBERTON NILS; GRADEN HENRIK; EVERTSSON EMMA; BRATT EMMA; LEPISTO MATTI; JOHANNESSON PETRA; SVENSSON PER H,期刊：ACS Medicinal Chemistry Letters, 页码：574-578 , 文章类型： Article，,卷期：2012年3-7] An efficient synthesis of aryl substituted cyclic sulfonimidamides designed as chiral nonplanar heterocyclic carboxylic acid bioisosteres is described. The cyclic sulfonimidamide ring system could be prepared in two step... Lipophilic Isosteres of a pi-pi Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction [作者：YUSUFF NAEEM; DORE MICHAEL; JOUD CAROL; VISSER MICHAEL; SPRINGER CLAYTON; XIE XIAOLING; HERLIHY KARA; PORTER DALE; TOURE B BARRY,期刊：ACS Medicinal Chemistry Letters, 页码：579-583 , 文章类型： Article，,卷期：2012年3-7] The discovery of new Bcl-2 protein-protein interaction antagonists is described. We replaced the northern fragment of ABT737 (pi-pi stacking interactions) with structurally simplified hydrophobic cage structures with muc... Chiral Cyclohexane 1,3-Diones as Inhibitors of Mutant SOD1-Dependent Protein Aggregation for the Treatment of ALS [作者：ZHANG YINAN; BENMOHAMED RADHIA; ZHANG WEI; KIM JINHO; EDGERLY CHRISTINA K; ZHU YAOQIU; MORIMOTO RICHARD I; FERRANTE ROBERT J; KIRSCH DONALD R; SILVERMAN RICHARD B,期刊：ACS Medicinal Chemistry Letters, 页码：584-587 , 文章类型： Article，,卷期：2012年3-7] Cyclohexane 1,3-diones were identified as a class of molecules exhibiting a protective effect against mutant SOD1 induced toxicity in PC-12 cells, but an optimized analogue had little or no effect on life extension in th... Optimized 5-Membered Heterocycle-Linked Pterins for the Inhibition of Ricin Toxin A [作者：PRUET JEFF M; SAITO RYOTA; MANZANO LAWRENCE A; JASHEWAY KARL R; WIGET PAUL A; KAMAT ISHAN; ANSLYN ERIC V; ROBERTUS JON D,期刊：ACS Medicinal Chemistry Letters, 页码：588-591 , 文章类型： Article，,卷期：2012年3-7] The optimization of a series of pterin amides for use as Ricin Toxin A (RTA) inhibitors is reported. On the basis of crystallographic data of a previous furan-linked pterin, various expanded furans were synthesized, link... 4-Quinolones as Noncovalent Inhibitors of High Molecular Mass Penicillin-Binding Proteins [作者：SHILABIN ABBAS G; DZHEKIEVA LIUDMILA; MISRA PUSHPA; JAYARAM B; PRATT R F,期刊：ACS Medicinal Chemistry Letters, 页码：592-595 , 文章类型： Article，,卷期：2012年3-7] Penicillin-binding proteins (PBPs) are important bacterial enzymes that carry out the final steps of bacterial cell wall assembly. Their DD-transpeptidase activity accomplishes the essential peptide cross linking step of...