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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27条记录   A Medicinal Chemist's Guide to Molecular Interactions [作者：BISSANTZ CATERINA; KUHN BERND; STAHL MARTIN,期刊：Journal of Medicinal Chemistry, 页码：5061-5084 , 文章类型： Article，,卷期：2010年53-14] Transient Receptor Potential Ankyrin 1 (TRPA1) Channel as Emerging Target for Novel Analgesics and Anti-Inflammatory Agents [作者：BARALDI PIER GIOVANNI; PRETI DELIA; MATERAZZI SERENA; GEPPETTI PIERANGELO,期刊：Journal of Medicinal Chemistry, 页码：5085-5107 , 文章类型： Article，,卷期：2010年53-14] Design and Syntheses of Permethyl Ningalin B Analogues: Potent Multidrug Resistance (MDR) Reversal Agents of Cancer Cells [作者：ZHANG PU YONG; WONG IRIS L K; YAN CLARE S W; ZHANG XIAO YU; JIANG TAO; CHOW LARRY M C; WAN SHENG BIAO,期刊：Journal of Medicinal Chemistry, 页码：5108-5120 , 文章类型： Article，,卷期：2010年53-14] A series of novel N-arylalkyl-3,4-diaryl-substituted pyrrole-2,5-diones were synthesized. They exhibited promising P-gp modulating activity in a P-gp overexpressing breast cancer cell line (LCC6MDR). Compound 6 (with thr... Isolation, Structure, and Functional Elucidation of a Modified Pentapeptide, Cysteine Protease Inhibitor (CPI-2081) from Streptomyces Species 2081 that Exhibit Inhibitory Effect on Cancer Cell Migration [作者：SINGH JAY PRAKASH; TAMANG SUDARSAN; RAJAMOHANAN P R; JIMA N C; CHAKRABORTY GOUTAM; KUNDU GOPAL C; GAIKWAD SUSHMA M; KHAN MOHAMAD I,期刊：Journal of Medicinal Chemistry, 页码：5121-5128 , 文章类型： Article，,卷期：2010年53-14] Cysteine proteases play an important role in cell migration and tumor metastasis. Therefore, their inhibitors are of colossal interest, having potential to be developed as effective antimetastatic drugs for tumor chemoth... Synthesis, Inhibitory Activity of Cholinesterases, and Neuroprotective Profile of Novel 1,8-Naphthyridine Derivatives [作者：DE LOS RIOS CRISTOBAL; EGEA JAVIER; MARCOCONTELLES JOSE; LEON RAFAEL; SAMADI ABDELOUAHID; IRIEPA ISABEL; MORALEDA IGNACIO; GALVEZ ENRIQUE; GARCIA ANTONIO G; LOPEZ MANUELA G; VILLARROYA MERCEDES; ROMERO ALEJANDRO,期刊：Journal of Medicinal Chemistry, 页码：5129-5143 , 文章类型： Article，,卷期：2010年53-14] 1,8-Naphthyridine derivatives related to 17 (ITH4012), a neuroprotective compound reported by our research group, have been synthesized. In general, they have shown better inhibition of acetylcholinesterase (AChE) and bu... Platinum(II) Complexes with Bioactive Carrier Ligands Having High Affinity for the Translocator Protein [作者：MARGIOTTA NICOLA; DENORA NUNZIO; OSTUNI ROSA; LAQUINTANA VALENTINO; ANDERSON AMY; JOHNSON STEVEN W; TRAPANI GIUSEPPE; NATILE GIOVANNI,期刊：Journal of Medicinal Chemistry, 页码：5144-5154 , 文章类型： Article，,卷期：2010年53-14] Peripheral benzodiazepine receptors (PBRs, also named TSPO) are overexpressed in many tumor types, with the grade of TSPO overexpression correlating with the malignancy of the tumor. For this reason, TSPO-binding ligands... Spirotetrahydro beta-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria [作者：YEUNG BRYAN K S; ZOU BIN; ROTTMANN MATTHIAS; LAKSHMINARAYANA SURESH B; ANG SHI HUA; LEONG SEH YONG; TAN JOCELYN; WONG JOSEPHINE; KELLERMAERKI SONJA; FISCHLI CHRISTOPH; GOH ANNE; SCHMITT ESTHER K; KRASTEL PHILIPP; FRANCOTTE ERIC; KUHEN KELLI; PLOUFFE DAVID; HENSON KERSTIN; WAGNER TRIXIE; WINZELER ELIZABETH A; PETERSEN FRANK; BRUN RETO; DARTOIS VERONIQUE; DIAGANA THIERRY T; KELLER THOMAS H,期刊：Journal of Medicinal Chemistry, 页码：5155-5164 , 文章类型： Article，,卷期：2010年53-14] The antiplasmodial activity of a series of spirotetrahydro beta-carbolines is described. Racemic spiroazepineindole (1) was identified from a phenotypic screen on wild type Plasmodium falciparum with an in vitro IC50 of ... 1-(5-Carboxyindol-1-yl)propan-2-one Inhibitors of Human Cytosolic Phospholipase A(2)alpha with Reduced Lipophilicity: Synthesis, Biological Activity, Metabolic Stability, Solubility, Bioavailability, And Topical in Vivo Activity [作者：DREWS ANDREAS; BOVENS STEFANIE; ROEBROCK KIRSTEN; SUNDERKOETTER CORD; REINHARDT DIRK; SCHAEFERS MICHAEL; VAN DER VELDE ANDREA; ELFRINGHOFF ALWINE SCHULZE; FABIAN JOERG; LEHR MATTHIAS,期刊：Journal of Medicinal Chemistry, 页码：5165-5178 , 文章类型： Article，,卷期：2010年53-14] Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent inhibitors of human cytosolic phospholipase A(2)alpha (cPLA(2)alpha). In continuation of our attempts to d... Analysis of the Binding of Mixed Lineage Leukemia 1 (MLL1) and Histone 3 Peptides to WD Repeat Domain 5 (WDR5) for the Design of Inhibitors of the MLL1-WDR5 Interaction [作者：KARATAS HACER; TOWNSEND ELIZABETH C; BERNARD DENZIL; DOU YALI; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：5179-5185 , 文章类型： Article，,卷期：2010年53-14] MLL1 is a histone 3 lysine 4 (H3K4) methyltransferase and a promising new cancer therapeutic target. The catalytic activity of MLL1 is regulated by the formation of a core complex consisting of MLL1, WDR5, RbBP5, and Ash... (3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: Potent and Selective Antagonists of the Serotonin 5-HT6 Receptor [作者：IVACHTCHENKO ALEXANDRE V; DMITRIEV DMITRI E; GOLOVINA ELENA S; KADIEVA MADINA G; KORYAKOVA ANGELA G; KYSIL VOLODYMYR M; MITKIN OLEG D; OKUN ILYA M; TKACHENKO SERGEY E; VOROBIEV ANTON A,期刊：Journal of Medicinal Chemistry, 页码：5186-5196 , 文章类型： Article，,卷期：2010年53-14] 5-HT6 receptors are exclusively localized in the CNS and have high affinity with many psychotropic agents. Though the role of this receptor in many CNS diseases is widely anticipated, lack of definite progress in the dev... (Bis)urea and (Bis)thiourea Inhibitors of Lysine-Specific Demethylase 1 as Epigenetic Modulators [作者：SHARMA SHIV K; WU YU; STEINBERGS NORA; CROWLEY MICHAEL L; HANSON ALLISON S; CASERO ROBERT A JR; WOSTER PATRICK M,期刊：Journal of Medicinal Chemistry, 页码：5197-5212 , 文章类型： Article，,卷期：2010年53-14] 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 overexpression is thought to contrib... Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidates [作者：BAVETSIAS VASSILIOS; LARGE JONATHAN M; SUN CHONGBO; BOULOC NATHALIE; KOSMOPOULOU MAGDA; MATTEUCCI MIZIO; WILSHER NICOLA E; MARTINS VANESSA; REYNISSON JOHANNES; ATRASH BUTRUS; FAISAL AMIR; URBAN FREDERIQUE; VALENTI MELANIE; BRANDON ALEXIS DE HAVEN; BOX GARY; RAYNAUD FLORENCE I; WORKMAN PAUL; ECCLES SUZANNE A; BAYLISS RICHARD; BLAGG JULIAN; LINARDOPOULOS SPIROS; MCDONALD EDWARD,期刊：Journal of Medicinal Chemistry, 页码：5213-5228 , 文章类型： Article，,卷期：2010年53-14] Lead optimization studies using 7 as the starting point led to a new class of imidazo[4,5-b]pyridine-based inhibitors of Aurora kinases that possessed the l-benzylpiperazinyl motif at the 7-position, and displayed favora... Complexes of Bacterial Nicotinate Mononucleotide Adenylyltransferase with Inhibitors: Implication for Structure-Based Drug Design and Improvement [作者：HUANG NIAN; KOLHATKAR ROHIT; EYOBO YVONNE; SORCI LEONARDO; RODIONOVA IRINA; OSTERMAN ANDREI L; MACKERELL ALEXANDER D JR; ZHANG HONG,期刊：Journal of Medicinal Chemistry, 页码：5229-5239 , 文章类型： Article，,卷期：2010年53-14] Bacterial nicotinate mononucleotide adenylyltransferase encoded by the essential gene nadD plays a central role in the synthesis of the redox cofactor NAD(+). The NadD enzyme is conserved in the majority of bacterial spe... Oncocin (VDKPPYLPRPRPPRRIYNR-NH2): A Novel Antibacterial Peptide Optimized against Gram-Negative Human Pathogens [作者：KNAPPE DANIEL; PIANTAVIGNA STEFANIA; HANSEN ANNE; MECHLER ADAM; BINAS ANNEGRET; NOLTE OLIVER; MARTIN LISANDRA L; HOFFMANN RALF,期刊：Journal of Medicinal Chemistry, 页码：5240-5247 , 文章类型： Article，,卷期：2010年53-14] Small proline-rich antimicrobial peptides (AMP) have attracted considerable interest, as they target specific intracellular bacterial components and do not act by lytic mechanisms. Here, a novel peptide, termed oncocin (... Click Chemistry Approach to New N-Substituted Aminocyclitols as Potential Pharmacological Chaperones for Gaucher Disease [作者：DIAZ LUCIA; BUJONS JORDI; CASAS JOSEFINA; LLEBARIA AMADEU; DELGADO ANTONIO,期刊：Journal of Medicinal Chemistry, 页码：5248-5255 , 文章类型： Article，,卷期：2010年53-14] New N-alkylaminocyclitols bearing a 1,2,3-triazole system at different positions of the alkyl chain have been prepared as potential GCase pharmacological chaperones using click chemistry approaches. Among them, compounds... Ligand Specificity in Fragment-Based Drug Design [作者：BARELIER SARAH; PONS JULIEN; GEHRING KALLE; LANCELIN JEANMARC; KRIMM ISABELLE,期刊：Journal of Medicinal Chemistry, 页码：5256-5266 , 文章类型： Article，,卷期：2010年53-14] Fragment-based drug design consists of identifying low-molecular weight compounds that weakly bind to a target macromolecule and will then be modified or linked to yield potent inhibitors. The specificity of these low-co...