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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   Design, Synthesis, and Biological Evaluation of Novel Transrepression-Selective Liver X Receptor (LXR) Ligands with 5,11-Dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one Skeleton [作者：AOYAMA ATSUSHI; ENDOUMEDA KAORI; KISHIDA KENJI; OHGANE KENJI; NOGUCHIYACHIDE TOMOMI; AOYAMA HIROSHI; ISHIKAWA MINORU; MIYACHI HIROYUKI; MAKISHIMA MAKOTO; HASHIMOTO YUICHI,期刊：Journal of Medicinal Chemistry, 页码：7360-7377 , 文章类型： Article，,卷期：2012年55-17] To obtain novel transrepression-selective liver X receptor (LXR) ligands, we adopted a strategy of reducing the transactivational agonistic activity of the 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one de... Low Molecular Weight Amidoximes that Act as Potent Inhibitors of Lysine-Specific Demethylase 1 [作者：HAZELDINE STUART; PACHAIYAPPAN BOOBALAN; STEINBERGS NORA; NOWOTARSKI SHANNON; HANSON ALLISON S; CASERO ROBERT A JR; WOSTER PATRICK M,期刊：Journal of Medicinal Chemistry, 页码：7378-7391 , 文章类型： Article，,卷期：2012年55-17] The recently discovered enzyme lysine-specific demethylase 1 (LSD1) plays an important role in the epigenetic control of gene expression, and aberrant gene silencing secondary to LSD1 dysregulation is thought to contribu... Development of o-Chlorophenyl Substituted Pyrimidines as Exceptionally Potent Aurora Kinase Inhibitors [作者：LAWRENCE HARSHANI R; MARTIN MATHEW P; LUO YUNTING; PIREDDU ROBERTA; YANG HUA; GEVARIYA HARSUKH; OZCAN SEVIL; ZHU JINYI; KENDIG ROBERT; RODRIGUEZ MERCEDES; ELIAS ROY; CHENG JIN Q; SEBTI SAID M; SCHONBRUNN ERNST; LAWRENCE NICHOLAS J,期刊：Journal of Medicinal Chemistry, 页码：7392-7416 , 文章类型： Article，,卷期：2012年55-17] The o-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC50 = 6.1 +/- 1.0 nM) from in-house screening. Detailed structure-activity relationship (SAR) studies indicated that pola... Selective Inhibitors of Aldo-Keto Reductases AKR1C1 and AKR1C3 Discovered by Virtual Screening of a Fragment Library [作者：BROZIC PETRA; TURK SAMO; ADENIJI ADEGOKE O; KONC JANEZ; JANEZIC DUSANKA; PENNING TREVOR M; RIZNER TEA LANISNIK; GOBEC STANISLAV,期刊：Journal of Medicinal Chemistry, 页码：7417-7424 , 文章类型： Article，,卷期：2012年55-17] Human aldo-keto reductases 1C1-1C4 (AKR1C1-AKR1C4) function in vivo as 3-keto-, 17-keto-, and 20-ketosteroid reductases and regulate the activity of androgens, estrogens, and progesterone and the occupancy and transactiv... Bioisosteric Transformations and Permutations in the Triazolopyrimidine Scaffold To Identify the Minimum Pharmacophore Required for Inhibitory Activity against Plasmodium falciparum Dihydroorotate Dehydrogenase [作者：MARWAHA ALKA; WHITE JOHN; EL MAZOUNI FARAH; CREASON SHARON A; KOKKONDA SREEKANTH; BUCKNER FREDERICK S; CHARMAN SUSAN A; PHILLIPS MARGARET A; RATHOD PRADIPSINH K,期刊：Journal of Medicinal Chemistry, 页码：7425-7436 , 文章类型： Article，,卷期：2012年55-17] Plasmodium falciparum causes approximately 1 million deaths annually. However, increasing resistance imposes a continuous threat to existing drug therapies. We previously reported a number of potent and selective triazol... An Aromatic Region To Induce a Switch between Agonism and Inverse Agonism at the Ghrelin Receptor [作者：ELS SYLVIA; SCHILD ENRICO; PETERSEN PIA STEEN; KILIAN TOMMARTEN; MOKROSINSKI JACEK; FRIMURER THOMAS M; CHOLLET CONSTANCE; SCHWARTZ THUE W; HOLST BIRGITTE; BECKSICKINGER ANNETTE G,期刊：Journal of Medicinal Chemistry, 页码：7437-7449 , 文章类型： Article，,卷期：2012年55-17] The ghrelin receptor displays a high constitutive activity suggested to be involved in the regulation of appetite and food intake. Here, we have created peptides with small changes in the core binding motif -wFw- of the ... Design, Synthesis, and Evaluation of pH-Dependent Hydrolyzable Emetine Analogues as Treatment for Prostate Cancer [作者：AKINBOYE EMMANUEL S; ROSEN MARC D; DENMEADE SAMUEL R; KWABIADDO BERNARD; BAKARE OLADAPO,期刊：Journal of Medicinal Chemistry, 页码：7450-7459 , 文章类型： Article，,卷期：2012年55-17] The N-2' position of the natural product emetine has been derivatized to thiourea, urea, sulfonamide, dithiocarbamate, carbamate, and pH responsive hydrolyzable amide analogues. In vitro studies of these analogues in PC3... Stabilization and Structural Alteration of the G-Quadruplex DNA Made from the Human Telomeric Repeat Mediated by Troger's Base Based Novel Benzimidazole Derivatives [作者：PAUL ANANYA; MAJI BASUDEB; MISRA SANTOSH K; JAIN AKASH K; MUNIYAPPA K; BHATTACHARYA SANTANU,期刊：Journal of Medicinal Chemistry, 页码：7460-7471 , 文章类型： Article，,卷期：2012年55-17] Ligand-induced stabilization of the G-quadruplex DNA structure derived from the single-stranded 3'-overhang of the telomeric DNA is an attractive strategy for the inhibition of the telomerase activity. The agents that ca... Solubility-Driven Optimization of Phosphodiesterase-4 Inhibitors Leading to a Clinical Candidate [作者：PRESS NEIL J; TAYLOR ROGER J; FULLERTON JOSEPH D; TRANTER PAMELA; MCCARTHY CLIVE; KELLER THOMAS H; ARNOLD NICOLA; BEER DAVID; BROWN LYNDON; CHEUNG ROBERT; CHRISTIE JULIE; DENHOLM ALASTAIR; HABERTHUER SANDRA; HATTO JULIA D I; KEENAN MARK; MERCER MARK K; OAKMAN HELEN; SAHRI HELENE; TUFFNELL ANDREW R; TWEED MORRIS; TYLER JOHN W; WAGNER TRIXIE; FOZARD JOHN R; TRIFILIEFF ALEXANDRE,期刊：Journal of Medicinal Chemistry, 页码：7472-7479 , 文章类型： Article，,卷期：2012年55-17] The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic prop... Discovery of (2S)-1-[4-(2-{6-Amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-puri n-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a Purine-Based Hsp90 Inhibitor [作者：KIM SEHO; BAJJI ASHOK; TANGALLAPALLY RAJENDRA; MARKOVITZ BENJAMIN; TROVATO RICHARD; SHENDEROVICH MARK; BAICHWAL VIJAY; BARTEL PAUL; CIMBORA DANIEL; MCKINNON RENA; ROBINSON ROSANN; PAPAC DAMON; WETTSTEIN DANIEL; CARLSON ROBERT; YAGER KRAIG M,期刊：Journal of Medicinal Chemistry, 页码：7480-7501 , 文章类型： Article，,卷期：2012年55-17] Modulation of Hsp90 (heat shock protein 90) function has been recognized as an attractive approach for cancer treatment, since many cancer cells depend on Hsp90 to maintain cellular homeostasis. This has spurred the sear... Development of Novel Bisphosphonate Prodrugs of Doxorubicin for Targeting Bone Metastases That Are Cleaved pH Dependently or by Cathepsin B: Synthesis, Cleavage Properties, and Binding Properties to Hydroxyapatite As Well As Bone Matrix [作者：HOCHDOERFFER KATRIN; ABU AJAJ KHALID; SCHAEFEROBODOZIE CYNTHIA; KRATZ FELIX,期刊：Journal of Medicinal Chemistry, 页码：7502-7515 , 文章类型： Article，,卷期：2012年55-17] Bone metastases are a frequent cause of morbidity in cancer patients. The present palliative therapeutic options are chemotherapy, hormone therapy, and the administration of bisphosphonates. The affinity between bisphosp... Rational Design of a Low Molecular Weight, Stable, Potent, and Long-Lasting GPR103 Aza-beta(3)-pseudopeptide Agonist [作者：NEVEU CINDY; LEFRANC BENJAMIN; TASSEAU OLIVIER; DOREGO JEANCLAUDE; BOURMAUD ADELE; CHAN PHILIPPE; BAUCHAT PATRICK; LE MAREC OLIVIER; CHUQUET JULIEN; GUILHAUDIS LAURE; BOUTIN JEAN A; SEGALASMILAZZO ISABELLE; COSTENTIN JEAN; VAUDRY HUBERT; BAUDYFOCH MICHELE; VAUDRY DAVID; LEPRINCE JEROME,期刊：Journal of Medicinal Chemistry, 页码：7516-7524 , 文章类型： Article，,卷期：2012年55-17] 26RFa, a novel RFamide neuropeptide, is the endogenous ligand of the former orphan receptor GPR103. Intracerebroventricular injection of 26RFa and its C-terminal heptapeptide, 26RFa((20-26)), stimulates food intake in ro... Design, Synthesis, and Pharmacological Evaluation of N-Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase-4 Inhibitors [作者：KUEMMERLE ARTHUR E; SCHMITT MARTINE; CARDOZO SUZANA V S; LUGNIER CLAIRE; VILLA PASCAL; LOPES ALEXANDRA B; ROMEIRO NELILMA C; JUSTINIANO HELENE; MARTINS MARCO A; FRAGA CARLOS A M; BOURGUIGNON JEANJACQUES; BARREIRO ELIEZER J,期刊：Journal of Medicinal Chemistry, 页码：7525-7545 , 文章类型： Article，,卷期：2012年55-17] Among a small series of tested N-acylhydrazones (NAHs), the compound 8a was selected as a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor associated with anti-TNF-alpha properties measured both in vitro and ... Discovery of a Novel Noniminosugar Acid alpha Glucosidase Chaperone Series [作者：XIAO JINGBO; WESTBROEK WENDY; MOTABAR OMID; LEA WENDY A; HU XIN; VELAYATI ARASH; ZHENG WEI; SOUTHALL NOEL; GUSTAFSON ANN MARIE; GOLDIN EHUD; SIDRANSKY ELLEN; LIU KE; SIMEONOV ANTON; TAMARGO RAFAEL J; RIBES ANTONIA; MATALONGA LESLIE; FERRER MARC; MARUGAN JUAN J,期刊：Journal of Medicinal Chemistry, 页码：7546-7559 , 文章类型： Article，,卷期：2012年55-17] Pompe disease is an autosomal recessive lysosomal storage disorder (LSD) caused by deficiency of the lysosomal enzyme acid a-glucosidase (GAA). Many disease-causing mutated GAA retain enzymatic activity but are not trans... Noncyclam Tetraamines Inhibit CXC Chemokine Receptor Type 4 and Target Glioma-Initiating Cells [作者：ROSBLANCO LAIA; ANIDO JUDIT; BOSSER RAMON; ESTE JOSE; CLOTET BONAVENTURA; KOSOY ANA; RUIZAVILA LUIS; TEIXIDO JORDI; SEOANE JOAN; BORRELL JOSE I,期刊：Journal of Medicinal Chemistry, 页码：7560-7570 , 文章类型： Article，,卷期：2012年55-17] The three stereoisomers of the noncyclam compound 1 (1(R,R), 1(S,S), and the mesa form 1(S,R)) and their corresponding tetrahydrochlorides 11 were prepared from (S)- and (R)-2-methylpiperidine. We have evaluated their in... Tuning the Activity of Platinum(IV) Anticancer Complexes through Asymmetric Acylation [作者：CHIN CHEE FEI; TIAN QUAN; SETYAWATI MAGDIEL INGGRID; FANG WANRU; TAN EMELYN SUE QING; LEONG DAVID TAI; ANG WEE HAN,期刊：Journal of Medicinal Chemistry, 页码：7571-7582 , 文章类型： Article，,卷期：2012年55-17] Platinum(II) anticancer drug cisplatin is one of the most important chemotherapeutic agents in clinical use but is limited by its high toxicity and severe side effects. Platinum(IV) anticancer prodrugs can overcome these...