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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49条记录   The Sugar Ring of the Nucleoside Is Required for Productive Substrate Positioning in the Active Site of Human Deoxycytidine Kinase (dCK): Implications for the Development of dCK-Activated Acyclic Guanine Analogues [作者：HAZRA SAUGATA; KONRAD MANFRED; LAVIE ARNON,期刊：Journal of Medicinal Chemistry, 页码：5792-5800 , 文章类型： Article，,卷期：2010年53-15] The low toxicity of acyclovir (ACV) is mainly due to the fact that human nucleoside kinases have undetectable phosphorylation rates with this acyclic guanine analogue. In contrast, herpes virus thymidine kinase (HSV1-TK)... Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a Novel Clinical AMPA Receptor Positive Modulator [作者：WARD SIMON E; HARRIES MARK; ALDEGHERI LAURA; ANDREOTTI DANIELE; BALLANTINE STUART; BAX BENJAMIN D; HARRIS ANDREW J; HARKER ANDY J; LUND JESPER; MELARANGE ROSEMARY; MINGARDI ANNA; MOOKHERJEE CLAUDETTE; MOSLEY JULIE; NEVE MARTA; OLIOSI BEATRICE; PROFETA ROBERTO; SMITH KATHRINE J; SMITH PAUL W; SPADA SIMONE; THEWLIS KEVIN M; YUSAF SHAHNAZ P,期刊：Journal of Medicinal Chemistry, 页码：5801-5812 , 文章类型： Article，,卷期：2010年53-15] A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i,... Potent Antagonist for the Vitamin D Receptor: Vitamin D Analogues with Simple Side Chain Structure [作者：SAKAMAKI YUTA; INABA YUKA; YOSHIMOTO NOBUKO; YAMAMOTO KEIKO,期刊：Journal of Medicinal Chemistry, 页码：5813-5826 , 文章类型： Article，,卷期：2010年53-15] We previously reported that 22S-butyl-25,26,27-trinor-1 alpha,24-dihydroxyvitamin D-3 2 was a potent VDR antagonist. The X-ray crystal structure of the ligand binding domain of VDR complexed with 2 indicated that this li... Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo-[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045) [作者：BROMIDGE STEVEN M; ARBAN ROBERTO; BERTANI BARBARA; BISON SILVIA; BORRIELLO MANUELA; CAVANNI PAOLO; DAL FORNO GIOVANNA; DIFABIO ROMANO; DONATI DANIELE; FONTANA STEFANO; GIANOTTI MASSIMO; GORDON LAURIE J; GRANCI ENRICA; LESLIE COLIN P; MOCCIA LUCA; PASQUARELLO ALESSANDRA; SARTORI ILARIA; SAVA ANNA; WATSON JEANNETTE M; WORBY ANGELA; ZONZINI LAURA; ZUCCHELLI VALERIA,期刊：Journal of Medicinal Chemistry, 页码：5827-5843 , 文章类型： Article，,卷期：2010年53-15] Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of fused tricyclic benzoxazines which are potent 5-HT1A/B/D rec... Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines. [作者：LIU FENG; CHEN XIN; ALLALIHASSANI ABDELLAH; QUINN AMY M; WIGLE TIM J; WASNEY GREGORY A; DONG AIPING; SENISTERRA GUILLERMO; CHAU IRENE; SIARHEYEVA ALENA; NORRIS JACQUELINE L; KIREEV DMITRI B; JADHAV AJIT; HEROLD J MARTIN; JANZEN WILLIAM P; ARROWSMITH CHERYL H; FRYE STEPHEN V; BROWN PETER J; SIMEONOV ANTON; VEDADI MASOUD; JIN JIAN,期刊：Journal of Medicinal Chemistry, 页码：5844-5857 , 文章类型： Article，,卷期：2010年53-15] Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic knockdown of G9a inhibits cancer cell growth, an... Understanding and Predicting Druggability. A High-Throughput Method for Detection of Drug Binding Sites [作者：SCHMIDTKE PETER; BARRIL XAVIER,期刊：Journal of Medicinal Chemistry, 页码：5858-5867 , 文章类型： Article，,卷期：2010年53-15] Druggability predictions are important to avoid intractable targets and to focus drug discovery efforts on sites offering better prospects. However, few druggability prediction tools have been released and none has been ... alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Antagonists: From Bench to Bedside [作者：MATTES HENRI; CARCACHE DAVID; KALKMAN HANS O; KOLLER MANUEL,期刊：Journal of Medicinal Chemistry, 页码：5367-5382 , 文章类型： Article，,卷期：2010年53-15] Bradykinin B1 Receptor Antagonists as Potential Therapeutic Agents for Pain [作者：HUANG HUI; PLAYER MARK R,期刊：Journal of Medicinal Chemistry, 页码：5383-5399 , 文章类型： Article，,卷期：2010年53-15] Identification of Orally Available Naphthyridine Protein Kinase D Inhibitors [作者：MEREDITH ERIK L; ARDAYFIO OPHELIA; BEATTIE KIMBERLY; DOBLER MARKUS R; ENYEDY ISTVAN; GAUL CHRISTOPH; HOSAGRAHARA VINAYAK; JEWELL CHARLES; KOCH KEITH; LEE WENDY; LEHMANN HANSJOERG; MCKINSEY TIMOTHY A; MIRANDA KARL; PAGRATIS NIKOS; PANCOST MARGARET; PATNAIK ANUP; PHAN DILLON; PLATO CRAIG; MING QIAN; RAJARAMAN VASUMATHY; RAO CHANG; ROZHITSKAYA OLGA; RUPPEN THOMAS; SHI JIE; SISKA SARAH J; SPRINGER CLAYTON; VAN EIS MAURICE; VEGA RICHARD B; VON MATT ANETTE; YANG LIHUA; YOON TAEYOUNG; ZHANG JIHU; ZHU NA; MONOVICH LAUREN G,期刊：Journal of Medicinal Chemistry, 页码：5400-5421 , 文章类型： Article，,卷期：2010年53-15] A novel 2,6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with applicati... Identification of Potent and Selective Amidobipyridyl Inhibitors of Protein Kinase D [作者：MEREDITH ERIK L; BEATTIE KIMBERLY; BURGIS ROBIN; CAPPARELLI MICHAEL; CHAPO JOSEPH; DIPIETRO LUCIAN; GAMBER GABRIEL; ENYEDY ISTVAN; HOOD DAVID B; HOSAGRAHARA VINAYAK; JEWELL CHARLES; KOCH KEITH A; LEE WENDY; LEMON DOUGLAS D; MCKINSEY TIMOTHY A; MIRANDA KARL; PAGRATIS NIKOS; PHAN DILLON; PLATO CRAIG; RAO CHANG; ROZHITSKAYA OLGA; SOLDERMANN NICOLAS; SPRINGER CLAYTON; VAN EIS MAURICE; VEGA RICHARD B; YAN WANLIN; ZHU QINGMING; MONOVICH LAUREN G,期刊：Journal of Medicinal Chemistry, 页码：5422-5438 , 文章类型： Article，,卷期：2010年53-15] The synthesis and biological evaluation of potent and selective PKD inhibitors are described herein. The compounds described in the present study selectively inhibit PKD among other putative HDAC kinases. The PKD inhibit... Synthesis and Structure-Activity Relationships of Novel 8a-Aza-8a-homoerythromycin A Ketolides [作者：PAVLOVIC DRAZEN; MUTAK STJEPAN,期刊：Journal of Medicinal Chemistry, 页码：5868-5880 , 文章类型： Article，,卷期：2010年53-15] A series of novel 6-O-substituted 8a-aza-8a-homoerythromycin A ketolides was synthesized and evaluated for in vitro antibacterial activity. Key strategic elements of the synthesis include the base-induced E-Z isomerizati... Synthesis and Resolution of cis-(+/-)-Methyl (1R,2S/1S,2R)-2-[(4-Hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: New sigma Receptor Ligands with Neuroprotective Effect [作者：PREZZAVENTO ORAZIO; CAMPISI AGATA; PARENTI CARMELA; RONSISVALLE SIMONE; ARICO GIUSEPPINA; ARENA EMANUELA; PISTOLOZZI MARCO; SCOTO GIOVANNA M; BERTUCCI CARLO; VANELLA ANGELO; RONSISVALLE GIUSEPPE,期刊：Journal of Medicinal Chemistry, 页码：5881-5885 , 文章类型： Article，,卷期：2010年53-15] The enantiomers of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylp henyl)cyclopropanecarboxylate [1, (+/-)-PPCC], a selective sigma ligand, were synthesized. The (+)-and (-)-enant... Glucosylated Deferiprone and Its Brain Uptake: Implications for Developing Glucosylated Hydroxypyridinone Analogues Intended to Cross the Blood-Brain Barrier [作者：ROY SOURAV; PRESTON JANE E; HIDER ROBERT C; MA YONG MIN,期刊：Journal of Medicinal Chemistry, 页码：5886-5889 , 文章类型： Article，,卷期：2010年53-15] This report presents that Deferiprone, the only clinically used 3-hydroxypyridin-4-one (HPO), is able to penetrate the blood-brain barrier (BBB) in guinea pigs, whereas its glucosylated analogue is unable to do so. This ... Structural Basis for the Interaction of Lactivicins with Serine beta-Lactamases [作者：BROWN TOM JR; CHARLIER PAULETTE; HERMAN RAPHAEL; SCHOFIELD CHRISTOPHER J; SAUVAGE ERIC,期刊：Journal of Medicinal Chemistry, 页码：5890-5894 , 文章类型： Article，,卷期：2010年53-15] Lactivicin (LTV) is a natural non-beta-lactam antibiotic that inhibits penicillin-binding proteins and serine beta-lactamases. A crystal structure of a BS3-LTV complex reveals that, as for its reaction with PBPs, LTV rea... "Viologen" Dendrimers as Antiviral Agents: The Effect of Charge Number and Distance (vol 53, pg 3480, 2010) [作者：ASAFTEI SIMONA; DE CLERCQ ERIK,期刊：Journal of Medicinal Chemistry, 页码：5895-5895 , 文章类型： Correction，,卷期：2010年53-15] Design of Selective, ATP-Competitive Inhibitors of Akt (vol 53, pg 4615, 2010) [作者：FREEMANCOOK KEVIN D; AUTRY CHRISTOPHER; BORZILLO GARY; GORDON DEBORAH; BARBACCITOBIN ELSA; BERNARDO VINCENT; BRIERE DAVID; CLARK TRACEY; CORBETT MATTHEW; JAKUBCZAK JOHN; KAKAR SHEFALI; KNAUTH ELIZABETH; LIPPA BLAISE; LUZZIO MICHAEL J; MANSOUR MAHMOUD; MARTINELLI GARY; MARX MATTHEW; NELSON KENDRA; PANDIT JAYVARDHAN; RAJAMOHAN FRANCIS; ROBINSON SHAUGHNESSY; SUBRAMANYAM CHAKRAPANI; WEI LIUQING; WYTHES MARTIN; MORRIS JOEL,期刊：Journal of Medicinal Chemistry, 页码：5895-5895 , 文章类型： Correction，,卷期：2010年53-15]