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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25条记录   Inhibition of Myosin ATPase Activity by Halogenated Pseudilins: A Structure-Activity Study [作者：PRELLER MATTHIAS; CHINTHALAPUDI KRISHNA; MARTIN RENE; KNOELKER HANSJOACHIM; MANSTEIN DIETMAR J,期刊：Journal of Medicinal Chemistry, 页码：3675-3685 , 文章类型： Article，,卷期：2011年54-11] Myosin activity is crucial for many biological functions. Strong links have been established between changes in the activity of specific myosin isoforms and diseases such as cancer, cardiovascular failure, and disorders ... Quercetin Diacylglycoside Analogues Showing Dual Inhibition of DNA Gyrase and Topoisomerase IV as Novel Antibacterial Agents [作者：HOSSION ABUGAFAR M L; ZAMAMI YOSHITO; KANDAHARY RAFIYA K; TSUCHIYA TOMOFUSA; OGAWA WAKANO; IWADO AKIMASA; SASAKI KENJI,期刊：Journal of Medicinal Chemistry, 页码：3686-3703 , 文章类型： Article，,卷期：2011年54-11] A structure-guided molecular design approach was used to optimize quercetin diacylglycoside analogues that inhibit bacterial DNA gyrase and topoisomerase IV and show potent antibacterial activity against a wide spectrum ... Synthesis and Antibacterial Activity of Pentacyclines: A Novel Class of Tetracycline Analogs [作者：SUN CUIXIANG; HUNT DIANA K; CLARK ROGER B; LOFLAND DENENE; OBRIEN WILLIAM J; PLAMONDON LOUIS; XIAO XIAOYI,期刊：Journal of Medicinal Chemistry, 页码：3704-3731 , 文章类型： Article，,卷期：2011年54-11] Employing a highly efficient total synthesis approach, we synthesized and evaluated for antibacterial activity diverse and novel pentacycline analogs with systematic variations at C7, C8, C9, and C10. Certain substitutio... Acenaphtho[1,2-b]pyrrole-Based Selective Fibroblast Growth Factor Receptors 1 (FGFR1) Inhibitors: Design, Synthesis, and Biological Activity [作者：CHEN ZHUO; WANG XIN; ZHU WEIPING; CAO XIANWEN; TONG LINJIANG; LI HONGLIN; XIE HUA; XU YUFANG; TAN SHAOYING; KUANG DONG; DING JIAN; QIAN XUHONG,期刊：Journal of Medicinal Chemistry, 页码：3732-3745 , 文章类型： Article，,卷期：2011年54-11] A novel series of acenaphtho[1,2-b]pyrrole derivatives as potent and selective inhibitors of fibroblast growth factor receptor 1 (FGFR1) were designed and synthesized. In silico target prediction revealed that tyrosine k... Nobilamides A-H, Long-Acting Transient Receptor Potential Vanilloid-1 (TRPV1) Antagonists from Mollusk-Associated Bacteria [作者：LIN ZHENJIAN; REILLY CHRISTOPHER A; ANTEMANO ROWENA; HUGHEN RONALD W; MARETT LENNY; CONCEPCION GISELA P; HAYGOOD MARGO G; OLIVERA BALDOMERO M; LIGHT ALAN; SCHMIDT ERIC W,期刊：Journal of Medicinal Chemistry, 页码：3746-3755 , 文章类型： Article，,卷期：2011年54-11] New compounds nobilamides A-H and related known compounds A-3302-A and A-3302-B were isolated based upon their suppression of capsaicin-induced calcium uptake in a mouse dorsal root ganglion primary cell culture assay. T... Novel 4,4-Disubstituted Piperidine-Based C-C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile [作者：KAZMIERSKI WIESLAW M; ANDERSON DON L; AQUINO CHRISTOPHER; CHAUDER BRIAN A; DUAN MAOSHENG; FERRIS ROBERT; KENAKIN TERRENCE; KOBLE CECILIA S; LANG DAN G; MCINTYRE MAGGIE S; PECKHAM JENNIFER; WATSON CHRISTIAN; WHEELAN PAT; SPALTENSTEIN ANDREW; WIRE MARY B; SVOLTO ANGILIQUE; YOUNGMAN MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：3756-3767 , 文章类型： Article，,卷期：2011年54-11] We recently described (J. Med. Chem. 2008, 51, 6538-6546) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting leads 1 and 2 to druglike molecules. The pivotal structural motif... A Novel Monocarbonyl Analogue of Curcumin, (1E,4E)-1,5-Bis(2,3-dimethoxyphenyl)penta-1,4-dien-3-one, Induced Cancer Cell H460 Apoptosis via Activation of Endoplasmic Reticulum Stress Signaling Pathway [作者：WANG YI; XIAO JIAN; ZHOU HUIPING; YANG SHULIN; WU XIAOPING; JIANG CHENGXI; ZHAO YUNJIE; LIANG DONGLOU; LI XIAOKUN; LIANG GUANG,期刊：Journal of Medicinal Chemistry, 页码：3768-3778 , 文章类型： Article，,卷期：2011年54-11] Endoplasmic reticulum (ER) stress-induced cancer cell apoptosis has become a novel signaling target for development of cancer therapeutic drugs. Curcumin exhibits growth-suppressive activity against a variety of cancer c... Potent Macrocyclic Inhibitors of Insulin-Regulated Aminopeptidase (IRAP) by Olefin Ring-Closing Metathesis [作者：ANDERSSON HANNA; DEMAEGDT HEIDI; JOHNSSON ANDERS; VAUQUELIN GEORGES; LINDEBERG GUNNAR; HALLBERG MATHIAS; ERDELYI MATE; KARLEN ANDERS; HALLBERG ANDERS,期刊：Journal of Medicinal Chemistry, 页码：3779-3792 , 文章类型： Article，,卷期：2011年54-11] Macrocyclic analogues of angiotensin IV (Ang IV, Val(1)-Tyr(2)-Ile(3)-His(4)-Pro(5)-Phe(6)) targeting the insulin-regulated aminopeptidase (TRAP) have been designed, synthesized, and evaluated biologically. Replacement o... Heteroatom-Substituted Analogues of Orphan Nuclear Receptor Small Heterodimer Partner Ligand and Apoptosis Inducer (E)-4-[3-(1-Adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic Acid [作者：XIA ZEBIN; FARHANA LULU; CORREA RICARDO G; DAS JAYANTA K; CASTRO DAVID J; YU JINGHUA; OSHIMA ROBERT G; REED JOHN C; FONTANA JOSEPH A; DAWSON MARCIA I,期刊：Journal of Medicinal Chemistry, 页码：3793-3816 , 文章类型： Article，,卷期：2011年54-11] (E)-4[3'-(1-Adamantyl)-4'-hydroxyphenyl]-3-chlorocinnamic acid (3-Cl-AHPC) induces the cell cycle arrest and apoptosis of cancer cells. Because its pharmacologic properties solubility, bioavailability, and toxicity requi... Use of a HEHEHE Purification Tag Instead of a Hexahistidine Tag Improves Biodistribution of Affibody Molecules Site-Specifically Labeled with Tc-99m, In-111 and I-125 [作者：HOFSTROM CAMILLA; ORLOVA ANNA; ALTAI MOHAMED; WANGSELL FREDRIK; GRASLUND TORBJORN; TOLMACHEV VLADIMIR,期刊：Journal of Medicinal Chemistry, 页码：3817-3826 , 文章类型： Article，,卷期：2011年54-11] Affibody molecules are a class of small (similar to 7 kDa) robust scaffold proteins suitable for radionuclide molecular imaging in vivo. The attachment of a hexahistidine (His(6))-tag to the Affibody molecule allows faci... Discovery and Characterizatlion of Small Molecule Inhibitors of the BET Family Bromodomains [作者：CHUNG CHUNWA; COSTE HERVE; WHITE JULIA H; MIRGUET OLIVIER; WILDE JONATHAN; GOSMINI ROMAIN L; DELVES CHRIS; MAGNY SYLVIE M; WOODWARD ROBERT; HUGHES STEPHEN A; BOURSIER ERIC V; FLYNN HELEN; BOUILLOT ANNE M; BAMBOROUGH PAUL; BRUSQ JEANMARIE G; GELLIBERT FRANCOISE J; JONES EMMA J; RIOU ALIZON M; HOMES PAUL; MARTIN SANDRINE L; UINGS IAIN J; TOUM JEROME; CLEMENT CATHERINE A; BOULLAY ANNEBENEDICTE; GRIMLEY RACHEL L; BLANDE FLORENCE M; PRINJHA RAB K; LEE KEVIN; KIRILOVSKY JORGE; NICODEME EDWIGE,期刊：Journal of Medicinal Chemistry, 页码：3827-3838 , 文章类型： Article，,卷期：2011年54-11] Epigenetic mechanisms of gene regulation have a profound role in normal development and disease processes. An integral part of this mechanism occurs through lysine acetylation of histone tails which are recognized by bro... Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-proliferative Agents [作者：ZHAO HUIPING; DONNELLY ALISON C; KUSUMA BHASKAR R; BRANDT GARY E L; BROWN DOUGLAS; RAJEWSKI ROGER A; VIELHAUER GEORGE; HOLZBEIERLEIN JEFFREY; COHEN MARK S; BLAGG BRIAN S J,期刊：Journal of Medicinal Chemistry, 页码：3839-3853 , 文章类型： Article，,卷期：2011年54-11] Development of the DNA gyrase inhibitor, novobiocin, into a selective Hsp90 inhibitor was accomplished through structural modifications to the amide side chain, coumarin ring, and sugar moiety. These species exhibit simi... Discovery and Characterization of a Nonphosphorylated Cyclic Peptide Inhibitor of the Peptidylprolyl Isomerase, Pin1 [作者：DUNCAN KELLY E; DEMPSEY BRIAN R; KILLIP LAUREN E; ADAMS JARRETT; BAILEY MELANIE L; LAJOIE GILLES A; LITCHFIELD DAVID W; BRANDL CHRISTOPHER J; SHAW GARY S; SHILTON BRIAN H,期刊：Journal of Medicinal Chemistry, 页码：3854-3865 , 文章类型： Article，,卷期：2011年54-11] Phage panning led to the discovery of a disulfide-cyclized peptide CRYPEVEIC that inhibits Pin1 activity with a K-I of 0.5 mu M. NMR chemical shift perturbation experiments show that cyclic CRYPEVEIC binds to the active ... Highly Potent Activity of (1R,2R,6S)-3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in Animal Models of Parkinson's Disease [作者：ARDASHOV OLEG V; PAVLOVA ALLA V; ILINA IRINA V; MOROZOVA EKATERINA A; KORCHAGINA DINA V; KARPOVA ELENA V; VOLCHO KONSTANTIN P; TOLSTIKOVA TATYANA G; SALAKHUTDINOV NARIMAN F,期刊：Journal of Medicinal Chemistry, 页码：3866-3874 , 文章类型： Article，,卷期：2011年54-11] (1R,2R,6S)-3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol 1 possesses potent antiparkinsonian activity in both MPTP and haloperidol animal models. The use of compound 1 resulted in nearly full recovery of the locomot... Development of the Fluorescent Biosensor hCalmodulin (hCaM)L39C-monobromobimane(mBBr)/V91C-mBBr, a Novel Tool for Discovering New Calmodulin Inhibitors and Detecting Calcium [作者：GONZALEZANDRADE MARTIN; RIVERACHAVEZ JOSE; SOSAPEINADO ALEJANDRO; FIGUEROA MARIO; RODRIGUEZSOTRES ROGELIO; MATA RACHEL,期刊：Journal of Medicinal Chemistry, 页码：3875-3884 , 文章类型： Article，,卷期：2011年54-11] A novel, sensible, and specific fluorescent biosensor of human calmodulin (hCaM), namely hCaM L39C-mBBr/V91C-mBBr, was constructed. The biosensor was useful for detecting ligands with opposing fluorescent signals, calciu... Cystic Fibrosis: A New Target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines [作者：BUDRIESI ROBERTA; IOAN PIERFRANCO; LEONI ALBERTO; PEDEMONTE NICOLETTA; LOCATELLI ALESSANDRA; MICUCCI MATTEO; CHIARINI ALBERTO; GALIETTA LUIS J V,期刊：Journal of Medicinal Chemistry, 页码：3885-3894 , 文章类型： Article，,卷期：2011年54-11] The pharmacology of the cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channel has attracted significant interest in recent years with the aim to search for rational new therapies for diseases caused by C...