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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18条记录   Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding [作者：MENICHINCHERI MARIA; ALBANESE CLARA; ALLI CRISTINA; BALLINARI DARIO; BARGIOTTI ALBERTO; CALDARELLI MARINA; CIAVOLELLA ANTONELLA; CIRLA ALESSANDRA; COLOMBO MARISTELLA; COLOTTA FRANCESCO; CROCI VALTER; DALESSIO ROBERTO; DANELLO MATTEO; ERMOTI ANTONELLA; FIORENTINI FRANCESCO; FORTE BARBARA; GALVANI ARTURO; GIORDANO PATRIZIA; ISACCHI ANTONELLA; MARTINA KATIA; MOLINARI ANTONIO; MOLL JUEGEN K; MONTAGNOLI ALESSIA; ORSINI PAOLO; ORZI FABRIZIO; PESENTI ENRICO; PILLAN ANTONIO; ROLETTO FULVIA; SCOLARO ALESSANDRA; TATO MARCO; TIBOLLA MARCELLINO; VALSASINA BARBARA; VARASI MARIO; VIANELLO PAOLA; VOLPI DANIELE; SANTOCANALE CORRADO; VANOTTIT ERMES,期刊：Journal of Medicinal Chemistry, 页码：7296-7315 , 文章类型： Article，,卷期：2010年53-20] Cdc7 serine/threonine kinase is a key regulator of DNA synthesis in eukaryotic organisms. Cdc7 inhibition through siRNA or prototype small molecules causes p53 independent apoptosis in tumor cells while reversibly arrest... Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency [作者：WU CHIAHSIEN; COUMAR MOHANE SELVARAJ; CHU CHANGYING; LIN WENHSING; CHEN YIRONG; CHEN CHIUNGTONG; SHIAO HUIYI; RAFI SHAIK; WANG SINGYI; HSU HUI; CHEN CHUNHWA; CHANG CHUNYU; CHANG TENGYUAN; LIEN TZUWEN; FANG MINGYU; YEH KAICHIA; CHEN CHINGPING; YEH TENGKUANG; HSIEH SUHUEI; HSU JOHN T A; LIAO CHUNCHEN; CHAO YUSHENG; HSIEH HSINGPANG,期刊：Journal of Medicinal Chemistry, 页码：7316-7326 , 文章类型： Article，,卷期：2010年53-20] HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 or... Positive Allosteric Modulators of the alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor [作者：GROVE SIMON J A; JAMIESON CRAIG; MACLEAN JOHN K F; MORROW JOHN A; RANKOVIC ZORAN,期刊：Journal of Medicinal Chemistry, 页码：7271-7279 , 文章类型： Article，,卷期：2010年53-20] ATPases as Drug Targets: Insights from Heat Shock Proteins 70 and 90 [作者：MASSEY ANDREW J,期刊：Journal of Medicinal Chemistry, 页码：7280-7286 , 文章类型： Article，,卷期：2010年53-20] Design, Synthesis, and Evaluation of Indolinones as Inhibitors of the Transforming Growth Factor beta Receptor I (TGF beta RI) [作者：ROTH GERALD J; HECKEL ARMIN; BRANDL TRIXI; GRAUERT MATTHIAS; HOERER STEFAN; KLEY JOERG T; SCHNAPP GISELA; BAUM PATRICK; MENNERICH DETLEV; SCHNAPP ANDREAS; PARK JOHN E,期刊：Journal of Medicinal Chemistry, 页码：7287-7295 , 文章类型： Article，,卷期：2010年53-20] Inhibition of transforming growth factor beta (TGF beta) type I receptor (Alk5) offers a novel approach for the treatment of fibrotic diseases and cancer. I ndolinones substituted in position 6 were identified as a new c... Targeted Mutations of Bacillus anthracis Dihydrofolate Reductase Condense Complex Structure-Activity Relationships [作者：BEIERLEIN JENNIFER M; KARRI NANDA G; ANDERSON AMY C,期刊：Journal of Medicinal Chemistry, 页码：7327-7336 , 文章类型： Article，,卷期：2010年53-20] Several antifolates, including trimethoprim (TMP) and a series of propargyl-linked analogues, bind dihydrofolate reductase from Bacillus anthracis (BaDHFR) with lower affinity than is typical in other bacterial species. ... Light Induced Antimicrobial Properties of a Brominated Boron Difluoride (BF2) Chelated Tetraarylazadipyrromethene Photosensitizer [作者：FRIMANNSSON DANIEL O; GROSSI MARCO; MURTAGH JULIE; PARADISI FRANCESCA; OSHEA DONAL F,期刊：Journal of Medicinal Chemistry, 页码：7337-7343 , 文章类型： Article，,卷期：2010年53-20] Herein we describe a new antimicrobial photodynamic therapeutic (PDT) agent based upon the brominated BF2 chelated tetraarylazadipyrromethene photosensitizer class. Bis-ammonium salt substitution of the photosensitizer p... Design, Synthesis, Radiolabeling, and in Vivo Evaluation of Carbon-11 Labeled N-[2-[4-(3-Cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a Potential Positron Emission Tomography Tracer for the Dopamine D-4 Receptors [作者：LACIVITA ENZA; DE GIORGIO PAOLA; LEE IRENE T; RODEHEAVER SEAN I; WEISS BRYAN A; FRACASSO CLAUDIA; CACCIA SILVIO; BERARDI FRANCESCO; PERRONE ROBERTO; ZHANG MINGRONG; MAEDA JUN; HIGUCHI MAKOTO; SUHARA TETSUYA; SCHETZ JOHN A; LEOPOLDO MARCEL,期刊：Journal of Medicinal Chemistry, 页码：7344-7355 , 文章类型： Article，,卷期：2010年53-20] Here we describe the design, synthesis, and evaluation of physicochemical and pharmacological properties of D-4 dopamine receptor ligands related to N-[2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (2). S... {(1R,2R,4R)-4-Methyl-1,2-cyclohexanediamine}oxalatoplatinum(II): A Novel Enantiomerically Pure Oxaliplatin Derivative Showing Improved Anticancer Activity in Vivo [作者：ABRAMKIN SERGEY A; JUNGWIRTH UTE; VALIAHDI SEIED M; DWORAK CLAUDIA; HABALA LADISLAV; MEELICH KRISTOF; BERGER WALTER; JAKUPEC MICHAEL A; HARTINGER CHRISTIAN G; NAZAROV ALEXEY A; GALANSKI MARKUS; KEPPLER BERNHARD K,期刊：Journal of Medicinal Chemistry, 页码：7356-7364 , 文章类型： Article，,卷期：2010年53-20] Novel derivatives of the clinically established anticancer drug oxaliplatin were synthesized. Cytotoxicity of the compounds was studied in six human cancer cell lines by means of the MTT assay. Additionally, most promisi... Preventive Oral Treatment with Resveratrol Pro-prodrugs Drastically Reduce Colon Inflammation in Rodents [作者：LARROSA MAR; TOMECARNEIRO JOAO; YANEZGASCON MARIA J; ALCANTARA DAVID; SELMA MARIA V; BELTRAN DAVID; GARCIACONESA MARIA T; URBAN CRISTINA; LUCAS RICARDO; TOMASBARBERAN FRANCISCO; MORALES JUAN C; ESPIN JUAN CARLOS,期刊：Journal of Medicinal Chemistry, 页码：7365-7376 , 文章类型： Article，,卷期：2010年53-20] There is no pharmaceutical or definitive surgical cure for inflammatory bowel diseases (IBDs). The naturally occurring polyphenol resveratrol exerts anti-inflammatory properties. However, its rapid metabolism diminishes ... Carbocycles Related to Oseltamivir as Influenza Virus Group-1-Specific Neuraminidase Inhibitors. Binding to N1 Enzymes in the Context of Virus-like Particles [作者：MOHAN SANKAR; MCATAMNEY SARAH; HASELHORST THOMAS; VON ITZSTEIN MARK; PINTO BRIAN MARIO,期刊：Journal of Medicinal Chemistry, 页码：7377-7391 , 文章类型： Article，,卷期：2010年53-20] We report here the exploitation of the 150-cavity in the active sites of group-1 neuraminidases for the design of new triazole-containing carbocycles related to oseltamivir. Inhibition studies with virus-like particles (... Discovery of Potent and Selective Inhibitors of Human Reticulocyte 15-Lipoxygenase-1 [作者：RAI GANESHA; KENYON VICTOR; JADHAV AJIT; SCHULTZ LENA; ARMSTRONG MICHELLE; JAMESON J BRIAN II; HOOBLER ERIC; LEISTER WILLIAM; SIMEONOV ANTON; HOLMAN THEODORE R; MALONEY DAVID J,期刊：Journal of Medicinal Chemistry, 页码：7392-7404 , 文章类型： Article，,卷期：2010年53-20] There are a variety of lipoxygenases in the human body (hLO), each having a distinct role in cellular biology. Human reticulocyte 15-lipoxygenase-1 (15-hLO-1), which catalyzes the dioxygenation of 1,4-cis,cis-pentadiene-... Antidiabetic and Antiobesity Effects of Ampkinone (6f), a Novel Small Molecule Activator of AMP-Activated Protein Kinase [作者：OH SANGMI; KIM SUNG JIN; HWANG JUNG HWAN; LEE HYANG YEON; RYU MIN JEONG; PARK JONGMIN; KIM SOUNG JUNG; JO YOUNG SUK; KIM YONG KYUNG; LEE CHULHO; KWEON KI RYANG; SHONG MINHO; PARK SEUNG BUM,期刊：Journal of Medicinal Chemistry, 页码：7405-7413 , 文章类型： Article，,卷期：2010年53-20] Adenosine 5'-monophosphate (AMP) activated protein kinase (AMPK) has emerged as an attractive target molecule for the treatment of metabolic disorders, including obesity and type 2 diabetes. In this study, we identified ... Discovery of Novel 2-Aryl-4-benzoyl-imidazoles Targeting the Colchicines Binding Site in Tubulin As Potential Anticancer Agents [作者：CHEN JIANJUN; WANG ZHAO; LI CHIENMING; LU YAN; VADDADY PAVAN K; MEIBOHM BERND; DALTON JAMES T; MILLER DUANE D; LI WEI,期刊：Journal of Medicinal Chemistry, 页码：7414-7427 , 文章类型： Article，,卷期：2010年53-20] A series of 2-aryl-4-benzoyl-imidazoles (ABI) was synthesized as a result of structural modifications based on the previous set of 2-aryl-imidazole-4-carboxylic amide (AICA) derivatives and 4-substituted methoxylbenzoyl-... Novel Agonists and Antagonists for Human Protease Activated Receptor 2 [作者：BARRY GRANT D; SUEN JACKY Y; LE GIANG T; COTTERELL ADAM; REID ROBERT C; FAIRLIE DAVID P,期刊：Journal of Medicinal Chemistry, 页码：7428-7440 , 文章类型： Article，,卷期：2010年53-20] Human protease activated receptor 2 (PAR2) is a G protein-coupled receptor that is associated with inflammatory diseases and cancers. PAR2 is activated by serine proteases that cleave its N-terminus and by synthetic pept... Assessment of Structurally Diverse Philanthotoxin Analogues for Inhibitory Activity on Ionotropic Glutamate Receptor Subtypes: Discovery of Nanomolar, Nonselective, and Use-Dependent Antagonists [作者：FROLUND SIDSEL; BELLA ANGELO; KRISTENSEN ANDERS S; ZIEGLER HANNE L; WITT MATTHIAS; OLSEN CHRISTIAN A; STROMGAARD KRISTIAN; FRANZYK HENRIK; JAROSZEWSKI JERZY W,期刊：Journal of Medicinal Chemistry, 页码：7441-7451 , 文章类型： Article，,卷期：2010年53-20] An array of analogues of the wasp toxin philanthotoxin-433, in which the asymmetric polyamine moiety was exchanged for spermine and the headgroup replaced with a variety of structurally diverse moieties, was prepared usi...