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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32条记录   Development of Second-Generation Indole-Based Dynamin GTPase Inhibitors [作者：GORDON CHRISTOPHER P; VENNBROWN BARBARA; ROBERTSON MARK J; YOUNG KELLY A; CHAU NGOC; MARIANA ANNA; WHITING AINSLIE; CHIRCOP MEGAN; ROBINSON PHILLIP J; MCCLUSKEY ADAM,期刊：Journal of Medicinal Chemistry, 页码：46-59 , 文章类型： Article，,卷期：2013年56-1] Focused library development of our lead 2-cyano-3-(1-(3-(dimethylamino)-propyl)-2-methyl-1H-indol-3-yl)-N-octylacrylamide (2) confirmed the tertiary dimethylamino-propyl moiety as critical for inhibition of dynamin GTPas... New 2-(Aryloxy)-3-phenylpropanoic Acids as Peroxisome Proliferator-Activated Receptor alpha/gamma Dual Agonists Able To Upregulate Mitochondrial Carnitine Shuttle System Gene Expression [作者：LAGHEZZA A; POCHETTI G; LAVECCHIA A; FRACCHIOLLA G; FALITI S; PIEMONTESE L; DI GIOVANNI C; IACOBAZZI V; INFANTINO V; MONTANARI R; CAPELLI D; TORTORELLA P; LOIODICE F,期刊：Journal of Medicinal Chemistry, 页码：60-72 , 文章类型： Article，,卷期：2013年56-1] The preparation of a series of 2-(aryloxy)-3-phenylpropanoic acids, resulting from the introduction of different substituents into the biphenyl system of the previously reported peroxisome proliferator-activated receptor... Incorporation of a 3-(2,2,2-Trifluoroethyl)-gamma-hydroxy-gamma-lactam Motif in the Side Chain of 4-Aminoquinolines. Syntheses and Antimalarial Activities [作者：CORNUT DAMIEN; LEMOINE HUGUES; KANISHCHEV OLEKSANDR; OKADA ETSUJI; ALBRIEUX FLORIAN; BEAVOGUI ABDOUL HABIB; BIENVENU ANNELISE; PICOT STEPHANE; BOUILLON JEANPHILIPPE; MEDEBIELLE MAURICE,期刊：Journal of Medicinal Chemistry, 页码：73-83 , 文章类型： Article，,卷期：2013年56-1] In this paper we report the synthesis and antimalarial properties of two series of fluoroalkylated gamma-lactams derived from 4-aminoquinoline as potent chemotherapeutic agents for malaria treatment. These molecules obta... Optimization of Inhibitors of the Tyrosine Kinase EphB4. 2. Cellular Potency Improvement and Binding Mode Validation by X-ray Crystallography [作者：LAFLEUR KARINE; DONG JING; HUANG DANZHI; CAFLISCH AMEDEO; NEVADO CRISTINA,期刊：Journal of Medicinal Chemistry, 页码：84-96 , 文章类型： Article，,卷期：2013年56-1] Inhibition of the tyrosine kinase erythropoietin-producing human hepatocellular carcinoma receptor B4 (EphB4) is an effective strategy for the treatment of solid tumors. We have previously reported a low nanomolar ATP-co... Synthesis, Biological Evaluation, and Molecular Modeling of Glycyrrhizin Derivatives as Potent High-Mobility Group Box-1 Inhibitors with Anti-Heart-Failure Activity in Vivo [作者：DU DAN; YAN JUN; REN JINHONG; LV HAINING; LI YONG; XU SONG; WANG YADAN; MA SHUANGGANG; QU JING; TANG WEIBIN; HU ZHUOWEI; YU SHISHAN,期刊：Journal of Medicinal Chemistry, 页码：97-108 , 文章类型： Article，,卷期：2013年56-1] Novel glycyrrhizin (GL) derivatives were designed and synthesized by introducing various amine or amino acid residues into the carbohydrate chain and at C-30. Their inhibitory effects on high-mobility group box 1 (HMGB1)... Plagiarism [作者：GEORG GUNDA I; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：1-1 , 文章类型： Editorial Material，,卷期：2013年56-1] Discovery of Coumarin-Dihydropyridine Hybrids as Bone Anabolic Agents [作者：SASHIDHARA KONENI V; KUMAR MANOJ; KHEDGIKAR VIKRAM; KUSHWAHA PRIYANKA; MODUKURI RAM K; KUMAR ABDHESH; GAUTAM JYOTI; SINGH DIVYA; SRIDHAR BALASUBRAMANIAM; TRIVEDI RITU,期刊：Journal of Medicinal Chemistry, 页码：109-122 , 文章类型： Article，,卷期：2013年56-1] The concept of molecular hybridization led us to discover a novel series of coumarin- dihydropyridine hybrids that have potent osteoblastic bone formation in vitro and that prevent ovariectomy-induced bone loss in vivo. ... Toward Highly Potent Cancer Agents by Modulating the C-2 Group of the Arylthioindole Class of Tubulin Polymerization Inhibitors [作者：LA REGINA GIUSEPPE; BAI RUOLI; RENSEN WHILELMINA MARIA; DI CESARE ERICA; COLUCCIA ANTONIO; PISCITELLI FRANCESCO; FAMIGLINI VALERIA; REGGIO ALESSIA; NALLI MARIANNA; PELLICCIA SVEVA; DA POZZO ELEONORA; COSTA BARBARA; GRANATA ILARIA; PORTA AMALIA; MARESCA BRUNO; SORIANI ALESSANDRA; IANNITTO MARIA LUISA; SANTONI ANGELA; LI JUNJIE; CONA MARLEIN MIRANDA; CHEN FENG; NI YICHENG; BRANCALE ANDREA; DONDIO GIULIO; VULTAGGIO STEFANIA; VARASI MARIO; MERCURIO CIRO; MARTINI CLAUDIA; HAMEL ERNEST; LAVIA PATRIZIA; NOVELLINO ETTORE; SILVESTRI ROMANO,期刊：Journal of Medicinal Chemistry, 页码：123-149 , 文章类型： Article，,卷期：2013年56-1] New arylthioindole derivatives having different cyclic substituents at position 2 of the indole were synthesized as anticancer agents. Several compounds inhibited tubulin polymerization at submicromolar concentration and... Antagonists of Protein-Protein Interactions Made Easy? [作者：PELLECCHIA MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：13-14 , 文章类型： Editorial Material，,卷期：2013年56-1] Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design [作者：FRIBERG ANDERS; VIGIL DOMINICO; ZHAO BIN; DANIELS R NATHAN; BURKE JASON P; GARCIABARRANTES PEDRO M; CAMPER DEMARCO; CHAUDER BRIAN A; LEE TAEKYU; OLEJNICZAK EDWARD T; FESIK STEPHEN W,期刊：Journal of Medicinal Chemistry, 页码：15-30 , 文章类型： Article，,卷期：2013年56-1] Myeloid cell leukemia 1 (Mcl-1), a member of the Bcl-2 family of proteins, is overexpressed and amplified in various cancers and promotes the aberrant survival of tumor cells that otherwise would undergo apoptosis. Here ... Total Synthesis of AMF-26, an Antitumor Agent for Inhibition of the Golgi System, Targeting ADP-Ribosylation Factor 1 [作者：SHIINA ISAMU; UMEZAKI YUMA; OHASHI YOSHIMI; YAMAZAKI YUTA; DAN SHINGO; YAMORI TAKAO,期刊：Journal of Medicinal Chemistry, 页码：150-159 , 文章类型： Article，,卷期：2013年56-1] An effective method for the total synthesis of 1 (AMF-26), a potentially promising new anticancer drug that disrupts the Golgi system by inhibiting the ADP-ribosylation factor 1 (Arf1) activation, has been developed for ... Increased Hydrophobicity and Estrogenic Activity of Simple Phenols with Silicon and Germanium-Containing Substituents [作者：FUJII SHINYA; MIYAJIMA YU; MASUNO HIROYUKI; KAGECHIKA HIROYUKI,期刊：Journal of Medicinal Chemistry, 页码：160-166 , 文章类型： Article，,卷期：2013年56-1] Here, we report the systematic synthesis and characterization of simple phenols bearing a trialkyl(aryl)silyl or trialkyl(aryl)germyl functional group as a hydrophobic substituent. These silicon and germanium analogues e... Structural Optimization of 2,5-Thiophene Amides as Highly Potent and Selective 17 beta-Hydroxysteroid Dehydrogenase Type 2 Inhibitors for the Treatment of Osteoporosis [作者：MARCHAISOBERWINKLER SANDRINE; XU KUIYING; WETZEL MARIE; PERSPICACE ENRICO; NEGRI MATTHIAS; MEYER ARNE; ODERMATT ALEX; MOELLER GABRIELE; ADAMSKI JERZY; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：167-181 , 文章类型： Article，,卷期：2013年56-1] Inhibition of 17 beta-HSD2 is an attractive mechanism for the treatment of osteoporosis. We report here the optimization of human 17 beta-HSD2 inhibitors in the 2,5-thiophene amide class by varying the size of the linker... Synthesis and Biological Evaluation of Indenoisoquinolines That Inhibit Both Tyrosyl-DNA Phosphodiesterase I (Tdp1) and Topoisomerase I (Top1) [作者：CONDASHERIDAN MARTIN; REDDY P V NARASIMHA; MORRELL ANDREW; COBB BROOKLYN T; MARCHAND CHRISTOPHE; AGAMA KELI; CHERGUI ADEL; RENAUD AMELIE; STEPHEN ANDREW G; BINDU LAKSHMAN K; POMMIER YVES; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：182-200 , 文章类型： Article，,卷期：2013年56-1] Tyrosyl-DNA phosphodiesterase I (Tdp1) plays a key role in the repair of damaged DNA resulting from the topoisomerase I (Top1) inhibitor camptothecin and a variety of other DNA-damaging anticancer agents. This report doc... Demystifying Brain Penetration in Central Nervous System Drug Discovery [作者：DI LI; RONG HAOJING; FENG BO,期刊：Journal of Medicinal Chemistry, 页码：2-12 , 文章类型： Article，,卷期：2013年56-1] This Perspective provides important concepts about the blood-brain barrier (BBB) in drug discovery and how they should be applied effectively in designing successful CNS drugs. Key parameters for brain penetration are di... Radiosynthesis and Evaluation of [C-11-Carbonyl]-Labeled Carbamates as Fatty Acid Amide Hydrolase Radiotracers for Positron Emission Tomography [作者：WILSON ALAN A; HICKS JUSTIN W; SADOVSKI OLEG; PARKES JUN; TONG JUNCHAO; HOULE SYLVAIN; FOWLER CHRISTOPHER J; VASDEV NEIL,期刊：Journal of Medicinal Chemistry, 页码：201-209 , 文章类型： Article，,卷期：2013年56-1] Fatty acid amide hydrolase (FAAH) plays a key role in regulating the tone of the endocannabinoid system. Radiotracers are required to image and quantify FAAH activity in vivo. We have synthesized a series of potent FAAH ...