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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31条记录   Discovery of 2-(6-{[(6-Fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hyd roxypyrimidine-5-carboxamide (CHR-3996), a Class I Selective Orally Active Histone Deacetylase Inhibitor [作者：MOFFAT DAVID; PATEL SANJAY; DAY FRANCESCA; BELFIELD ANDREW; DONALD ALASTAIR; ROWLANDS MARTIN; WIBAWA JUDATA; BROTHERTON DEBORAH; STIMSON LINDSAY; CLARK VANESSA; OWEN JO; BAWDEN LINDSAY; BOX GARY; BONE ELISABETH; MORTENSON PAUL; HARDCASTLE ANTHEA; VAN MEURS SANDRA; ECCLES SUZANNE; RAYNAUD FLORENCE; AHERNE WYNNE,期刊：Journal of Medicinal Chemistry, 页码：8663-8678 , 文章类型： Article，,卷期：2010年53-24] A novel series of HDAC inhibitors demonstrating class I subtype selectivity and good oral bioavailability is described. The compounds are potent enzyme inhibitors (IC50 values less than 100 nM), and improved activity in ... Identification and Synthesis of Novel Inhibitors of Acetyl-CoA Carboxylase with in Vitro and in Vivo Efficacy on Fat Oxidation [作者：KEIL STEFANIE; MUELLER MARCO; ZOLLER GERHARD; HASCHKE GUIDO; SCHROETER KATRIN; GLIEN MAIKE; RUF SVEN; FOCKEN INGO; HERLING ANDREAS W; SCHMOLL DIETER,期刊：Journal of Medicinal Chemistry, 页码：8679-8687 , 文章类型： Article，,卷期：2010年53-24] Acetyl CoA carboxylase isoforms 1 and 2 (ACC1/2) are key enzymes of fat utilization and their inhibition is considered to improve aspects of the metabolic syndrome. To identify pharmacological inhibitors of ACC1/2, a hig... Potential Chemopreventive Agents Based on the Structure of the Lead Compound 2-Bromo-1-hydroxyphenazine, Isolated from Streptomyces Species, Strain CNS284 [作者：CONDASHERIDAN MARTIN; MARLER LAURA; PARK EUNJUNG; KONDRATYUK TAMARA P; JERMIHOV KATHERINE; MESECAR ANDREW D; PEZZUTO JOHN M; ASOLKAR RATNAKAR N; FENICAL WILLIAM; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：8688-8699 , 文章类型： Article，,卷期：2010年53-24] The isolation of 2-bromo-1-hydroxyphenazine from a marine Streptomyces species, strain CNS284, and its activity against NF-kappa B, suggested that a short and flexible route for the synthesis of this metabolite and a var... Antitumor Agents 286. Design, Synthesis, and Structure-Activity Relationships of 3 ' R,4 ' R-Disubstituted-2 ',2 '-dimethyldihydropyrano[2,3-f]chromone (DSP) Analogues as Potent Chemosensitizers to Overcome Multidrug Resistance [作者：ZHOU TING; SHI QIAN; BASTOW KENNETH F; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：8700-8708 , 文章类型： Article，,卷期：2010年53-24] In this study, various 3'R,4'R-disubstituted-2',2'-dimethydihydropyrano[2,3-f]chromone (DSP) derivatives were discovered as potent chemosensitizers in the treatment of multidrug resistant cancer cells. Twenty-four DSP an... Structure-Activity Relationships of Substituted 1-Pyridyl-2-phenyl-1,2-ethanediones: Potent, Selective Carboxylesterase Inhibitors [作者：YOUNG BRANDON M; HYATT JANICE L; BOUCK DAVID C; CHEN TAOSHENG; HANUMESH PARIMALA; PRICE JEANINE; BOYD VINCENT A; POTTER PHILIP M; WEBB THOMAS R,期刊：Journal of Medicinal Chemistry, 页码：8709-8715 , 文章类型： Article，,卷期：2010年53-24] Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione in... Design, Synthesis, and Evaluation of Dibenzo[c,h][1,6]naphthyridines as Topoisomerase I Inhibitors and Potential Anticancer Agents [作者：KISELEV EVGENY; DEXHEIMER THOMAS S; POMMIER YVES; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：8716-8726 , 文章类型： Article，,卷期：2010年53-24] Indenoisoquinoline topoisomerase I (Top 1) inhibitors are a novel class of anticancer agents. Modifications of the indenoisoquinoline A, B, and D rings have been extensively studied in order to optimize Top 1 inhibitory ... Design, Synthesis, and Pharmacological Activity of Nonallergenic Pyrazolone-Type Antipyretic Analgesics [作者：URAMARU NAOTO; SHIGEMATSU HIDENARI; TODA AKIHISA; EYANAGI REIKO; KITAMURA SHIGEYUKI; OHTA SHIGERU,期刊：Journal of Medicinal Chemistry, 页码：8727-8733 , 文章类型： Article，,卷期：2010年53-24] To develop novel nonallergenic pyrazolone analgesics, we synthesized a series of compounds in which position 1 of the pyrazolone ring was substituted in place of the original methyl group in order to block the formation ... Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N- (3-pyridylmethyl)benzamide (CB-30865) as Potent Inhibitors of Nicotinamide Phosphoribosyltransferase (Nampt) [作者：LOCKMAN JEFFREY W; MURPHY BRETT R; ZIGAR DANIEL F; JUDD WESTON R; SLATTUM PAUL M; GAO ZHONGHUA; OSTANIN KIRILL; GREEN JEREMY; MCKINNON RENA; TERRYLORENZO RYAN T; FLEISCHER TRACEY C; BONIFACE J JAY; SHENDEROVICH MARK; WILLARDSEN J ADAM,期刊：Journal of Medicinal Chemistry, 页码：8734-8746 , 文章类型： Article，,卷期：2010年53-24] We have shown previously that the target of the potent cytatoxic agent 4-[(7-bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N -(3-pyridylmethyl)benzamide (CB38065, 1) is nicotinamide phosphoribosyltrans... Structure-Based Design, Synthesis, and Pharmacological Evaluation of 3-(Aminoalkyl)-5-fluoroindoles as Myeloperoxidase Inhibitors [作者：SOUBHYE JALAL; PREVOST MARTINE; VAN ANTWERPEN PIERRE; BOUDJELTIA KARIM ZOUAOUI; ROUSSEAU ALEXANDRE; FURTMUELLER PAUL G; OBINGER CHRISTIAN; VANHAEVERBEEK MICHEL; DUCOBU JEAN; NEVE JEAN; GELBCKE MICHEL; DUFRASNE FRANCOIS,期刊：Journal of Medicinal Chemistry, 页码：8747-8759 , 文章类型： Article，,卷期：2010年53-24] Oxidized low-density lipoproteins (LDLs) accumulate in the vascular wall and promote local inflammation, which contributes to the progression of the atheromatous plaque. The key role of myeloperoxidase (MPO) in this proc... Discovery of Novel Benzopyranyl Tetracycles that Act as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-kappa B Ligand [作者：ZHU MINGYAN; KIM MYUNG HEE; LEE SANGHEE; BAE SU JUNG; KIM SEONG HWAN; PARK SEUNG BUM,期刊：Journal of Medicinal Chemistry, 页码：8760-8764 , 文章类型： Article，,卷期：2010年53-24] A novel benzopyran-fused molecular framework 7ai was discovered as a specific inhibitor of RANKL-induced osteoclastogenesis using a cell-based TRAP activity assay from drug-like small-molecule libraries constructed by di... Antiretroviral Activity of Thiosemicarbazone Metal Complexes [作者：PELOSI GIORGIO; BISCEGLIE FRANCO; BIGNAMI FABIO; RONZI PAOLA; SCHIAVONE PASQUALINA; RE MARIA CARLA; CASOLI CLAUDIO; PILOTTI ELISABETTA,期刊：Journal of Medicinal Chemistry, 页码：8765-8769 , 文章类型： Article，,卷期：2010年53-24] Thiosemicarbazones display a wide antimicrobial activity by targeting bacteria, fungi, and viruses. Here, we report our studies on the antiviral activity of two thiosemicarbazone metal complexes, [bis-(citronellalthiosem... Discovery of Non-Glycoside Sodium-Dependent Glucose Co-Transporter 2 (SGLT2) Inhibitors by Ligand-Based Virtual Screening [作者：WU JIANSUNG; PENG YIHUI; WU JIUNMING; HSIEH CHIEHJUI; WU SZUHUEI; COUMAR MOHANE SELVARAJ; SONG JENSHIN; LEE JINQCHYI; TSAI CHIHUI; CHEN CHIUNGTONG; LIU YUWEI; CHAO YUSHENG; WU SUYING,期刊：Journal of Medicinal Chemistry, 页码：8770-8774 , 文章类型： Article，,卷期：2010年53-24] A ligand-based virtual screening strategy (a combination of pharmacophore model generation, shape-based scoring, and structure clustering analysis) was developed to discover novel SGLT2 inhibitors. The best pharmacophore... Chemical Switch of a Metabotropic Glutamate Receptor 2 Silent Allosteric Modulator into Dual Metabotropic Glutamate Receptor 2/3 Negative/Positive Allosteric Modulators [作者：SCHANN STEPHAN; MAYER STANISLAS; FRANCHET CHRISTEL; FRAULI MELANIE; STEINBERG EDITH; THOMAS MIREILLE; BARON LUC; NEUVILLE PASCAL,期刊：Journal of Medicinal Chemistry, 页码：8775-8779 , 文章类型： Article，,卷期：2010年53-24] Using an mGluR2 FRET-based binding assay, binders of the transmembrane region devoid of functional activity were identified. It is reported that slight chemical modifications of these SAMs can dramatically change activit... DNA-Dependent Protein Kinase (DNA-PK) Inhibitors. Synthesis and Biological Activity of Quinolin-4-one and Pyridopyrimidin-4-one Surrogates for the Chromen-4-one Chemotype [作者：CANO CELINE; BARBEAU OLIVIER R; BAILEY CHRISTINE; COCKCROFT XIAOLING; CURTIN NICOLA J; DUGGAN HEATHER; FRIGERIO MARK; GOLDING BERNARD T; HARDCASTLE IAN R; HUMMERSONE MARC G; KNIGHTS CHARLOTTE; MENEAR KEITH A; NEWELL DAVID R; RICHARDSON CAROLINE J; SMITH GRAEME C M; SPITTLE BEN; GRIFFIN ROGER J,期刊：Journal of Medicinal Chemistry, 页码：8498-8507 , 文章类型： Article，,卷期：2010年53-24] Following the discovery of dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-one (NU7441) (Leahy, J. J. J.; Golding, B. T.; Griffin, R. J.; Hardcastle, I. R.; Richardson, C.; Rigoreau, L.; Smith, G. C. M. Bioorg. Med.... A Novel Pyrazolo[1,5-a]pyrimidine Is a Potent Inhibitor of Cyclin-Dependent Protein Kinases 1, 2, and 9, Which Demonstrates Antitumor Effects, in Human Tumor Xenografts Following Oral Administration [作者：HEATHCOTE DEAN A; PATEL HETAL; KROLL SEBASTIAN H B; HAZEL PASCALE; PERIYASAMY MANIKANDAN; ALIKIAN MARY; KANNEGANTI SESHU K; JOGALEKAR ASHUTOSH S; SCHEIPER BODO; BARBAZANGES MARION; BLUM ANDREAS; BRACKOW JAN; SIWICKA ALEKASANDRA; PACE ROBERT D M; FUCHTER MATTHEW J; SNYDER JAMES P; LIOTTA DENNIS C; FREEMONT PAUL S; ABOAGYE ERIC O; COOMBES R CHARLES; BARRETT ANTHONY G M; ALI SIMAK,期刊：Journal of Medicinal Chemistry, 页码：8508-8522 , 文章类型： Article，,卷期：2010年53-24] Cyclin-dependent protein kinases (CDKs) are central to the appropriate regulation of cell proliferation, apoptosis, and gene expression. Abnormalities in CDK activity and regulation are common features of cancer, making ...