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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22条记录   Poly-N-methylated Amyloid beta-Peptide (A beta) C-Terminal Fragments Reduce A beta Toxicity in Vitro and in Drosophila melanogaster [作者：BOSE PARTHA PRATIM; CHATTERJEE URMIMALA; NERELIUS CHARLOTTE; GOVENDER THAVENDRAN; NORSTROM THOMAS; GOGOLL ADOLF; SANDEGREN ANNA; GOTHELID EMMANUELLE; JOHANSSON JAN; ARVIDSSON PER I,期刊：Journal of Medicinal Chemistry, 页码：8002-8009 , 文章类型： Article，,卷期：2009年52-24] Alzheimer's disease (AD), an age related neurodegenerative disorder, threatens to become a major health-economic problem. Assembly of 40- or 42-residue amyloid beta-peptides (A beta) into neurotoxic oligo-/polymeric beta... Discovery of 4-Morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as Highly Potent and Selective ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin (mTOR): Optimization of the 6-Aryl Substituent [作者：VERHEIJEN JEROEN C; RICHARD DAVID J; CURRAN KEVIN; KAPLAN JOSHUA; LEFEVER MARK; NOWAK PAWEL; MALWITZ DAVID J; BROOIJMANS NATASJA; TORALBARZA LOURDES; ZHANG WEIGUO; LUCAS JUDY; HOLLANDER IRWIN; AYRALKALOUSTIAN SEMIRAMIS; MANSOUR TAREK S; YU KER; ZASK ARIE,期刊：Journal of Medicinal Chemistry, 页码：8010-8024 , 文章类型： Article，,卷期：2009年52-24] Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of the 6-aryl substituent l... Design, Synthesis, and Characterization of Peptide-Based Rab Geranylgeranyl Transferase Inhibitors [作者：TAN KUITHONG; GUIUROZAS ESTER; BON ROBIN S; GUO ZHONG; DELON CHRISTINE; WETZEL STEFAN; ARNDT SABINE; ALEXANDROV KIRILL; WALDMANN HERBERT; GOODY ROGER S; WU YAOWEN; BLANKENFELDT WULF,期刊：Journal of Medicinal Chemistry, 页码：8025-8037 , 文章类型： Article，,卷期：2009年52-24] Rab geranylgeranyl transferase (RabGGTase) catalyzes the attachment of geranylgeranyl isoprenoids to Rab guanine triphosphatases, which Lire key regulators in vesicular transport. Because geranylgeranylation is required ... Drug Effects Viewed from a Signal Transduction Network Perspective [作者：FLIRI ANTON F; LOGING WILLIAM T; VOLKMANN ROBERT A,期刊：Journal of Medicinal Chemistry, 页码：8038-8046 , 文章类型： Article，,卷期：2009年52-24] Understanding how drugs affect cellular network Structures and how resulting signals are translated into drug effects holds the key to the discovery of medicines. Herein we examine this cause-effect relationship by deter... Carbamate Analogues of Fumagillin as Potent, Targeted Inhibitors of Methionine Aminopeptidase-2 [作者：ARICOMUENDEL CHRISTOPHER C; BENJAMIN DENNIS R; CAIAZZO TERESA M; CENTRELLA PAOLO A; CONTONIO BROOKE D; COOK CHARLES M; DOYLE ELISABETH G; HANNIG GERHARD; LABENSKI MATTHEW T; SEARLE LILY L; LIND KENNETH; MORGAN BARRY A; OLSON GARY; PARADISE CHRISTOPHER L; SELF CHRISTOPHER; SKINNER STEVEN R; SLUBOSKI BARBARA; SVENDSEN JENNIFER L; THOMPSON CHARLES D; WESTLIN WILLIAM; WHITE KERRY F,期刊：Journal of Medicinal Chemistry, 页码：8047-8056 , 文章类型： Article，,卷期：2009年52-24] Inhibition of methionine aminopeptidase-2 (MetAP2) represents a. novel approach to antiangiogenic therapy. We describe the synthesis and activity of fumagillin analogues that address the pharmacokinetic and safety liabil... Design, Synthesis, and Biological Evaluation of 6 alpha- and 6 beta-N-Heterocyclic Substituted Naltrexamine Derivatives as mu Opioid Receptor Selective Antagonists (vol 52, pg 1416, 2009) [作者：LI GUO; ASCHENBACH LINDSEY C; CHEN JIANYANG; CASSIDY MICHAEL P; STEVENS DAVID L; GABRA BICHOY H; SELLEY DANA E; DEWEY WILLIAM L; WESTKAEMPER RICHARD B; ZHANG YAN,期刊：Journal of Medicinal Chemistry, 页码：8057-8057 , 文章类型： Correction，,卷期：2009年52-24] Multidentate Small-Molecule Inhibitors of Vaccinia H1-Related (VHR) Phosphatase Decrease Proliferation of Cervix Cancer Cells (vol 52, pg 6716, 2009) [作者：WU SHUANGDING; VOSSIUS SOFIE; RAHMOUNI SOUAD; MILETIC ANA V; VANG TORKEL; VAZQUEZRODRIGUEZ JESUS; CERIGNOLI FABIO; ARIMURA YUTAKA; WILLIAMS SCOTT; HAYES TIKVA; MOUTSCHEN MICHEL; VASILE STEFAN; PELLECCHIA MAURIZIO; MUSTELIN TOMAS; TAUTZ LUTZ,期刊：Journal of Medicinal Chemistry, 页码：8058-8058 , 文章类型： Correction，,卷期：2009年52-24] The Medicinal Chemistry of Dengue Fever [作者：STEVENS ANDREW J; GAHAN MICHELLE E; MAHALINGAM SURESH; KELLER PAUL A,期刊：Journal of Medicinal Chemistry, 页码：7911-7926 , 文章类型： Review，,卷期：2009年52-24] Evaluation of Di-Sansalvamide A Derivatives: Synthesis, Structure-Activity Relationship, and Mechanism of Action [作者：ALEXANDER LESLIE D; SELLERS ROBERT P; DAVIS MELINDA R; ARDI VERONICA C; JOHNSON VICTORIA A; VASKO ROBERT C; MCALPINE SHELLI R,期刊：Journal of Medicinal Chemistry, 页码：7927-7930 , 文章类型： Article，,卷期：2009年52-24] Described is the SAR of 18 di-sansalvamide A derivatives and the mechanism of action of the most potent compound. We show that this scaffold is a promising lead in the development of novel cancer therapeutics because it ... Discovery of a New and Efficient Small Molecule for Neuronal Differentiation from Mesenchymal Stem Cell [作者：KIM NA RI; KANG SEUNG KYU; AHN HYUN HEE; KWON SUNG WOOK; PARK WOUL SEONG; KIM KI SUK; KIM SUNG SOO; JUNG HEE JUNG; CHOI SANG UN; AHN JIN HEE; KIM KWANG ROK,期刊：Journal of Medicinal Chemistry, 页码：7931-7933 , 文章类型： Article，,卷期：2009年52-24] A new synthetic small molecule. compound 1, which induced a neuronal differentiation from mesenchymal stein cells (MSCs) with an excellent efficiency, was identified. Furthermore the differentiated cell by 1 showed the n... N-Sulfonylanthranilic Acid Derivatives as Allosteric Inhibitors of Dengue Viral RNA-Dependent RNA Polymerase [作者：YIN ZHENG; CHEN YENLIANG; KONDREDDI RAVINDER REDDY; CHAN WAI LING; WANG GANG; NG RU HUI; LIM JOANNE Y H; LEE WAN YEN; JEYARAJ DURAISWAMY A; NIYOMRATTANAKIT PORNWARATT; WEN DAYING; CHAO ALEX; GLICKMAN J FRASER; VOSHOL HANS; MUELLER DIETER; SPANKA CARSTEN; DRESSLER SIGMAR; NILAR SHAHUL; VASUDEVAN SUBHASH G; SHI PEIYONG; KELLER THOMAS H,期刊：Journal of Medicinal Chemistry, 页码：7934-7937 , 文章类型： Article，,卷期：2009年52-24] A novel class of compounds containing N-sulfonylanthranilic acid was found to specifically inhibit dengue viral polymerase. The structural requirements for inhibition and it preliminary structure-activity relationship ar... Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole [作者：WANG TIANSHENG; DUFFY JOHN P; WANG JIAN; HALAS SUMMER; SALITURO FRANCESCO G; PIERCE ALBERT C; ZUCCOLA HARMON J; BLACK JAMES R; HOGAN JAMES K; JEPSON SCOTT; SHLYAKTER DINA; MAHAJAN SUDIPTA; GU YONG; HOOCK THOMAS; WOOD MARK; FUREY BRINLEY F; FRANTZ J DANIEL; DAUFFENBACH LISA M; GERMANN URSULA A; FAN BIN; NAMCHUK MARK; BENNANI YOUSSEF L; LEDEBOER MARK W,期刊：Journal of Medicinal Chemistry, 页码：7938-7941 , 文章类型： Article，,卷期：2009年52-24] The Synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further evaluated for its ability to block the EPO/JAK2 signaling ca... Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors [作者：ZASK ARIE; KAPLAN JOSHUA; VERHEIJEN JEROEN C; RICHARD DAVID J; CURRAN KEVIN; BROOIJMANS NATASJA; BENNETT ERIC M; TORALBARZA LOURDES; HOLLANDER IRWIN; AYRALKALOUSTIAN SEMIRAMIS; YU KER,期刊：Journal of Medicinal Chemistry, 页码：7942-7945 , 文章类型： Article，,卷期：2009年52-24] Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues with subnanomolar mTOR IC50 values and up to 26000-fold selec... Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy [作者：VERHOEST PATRICK R; PROULXLAFRANCE CAROLINE; CORMAN MICHAEL; CHENARD LOIS; HELAL CHRISTOPHER J; HOU XINJUN; KLEIMAN ROBIN; LIU SHENPING; MARR ERIC; MENNITI FRANK S; SCHMIDT CHRISTOPHER J; VANASEFRAWLEY MICHELLE; SCHMIDT ANNE W; WILLIAMS ROBERT D; NELSON FREDERICK R; FONSECA KARI R; LIRAS SPIROS,期刊：Journal of Medicinal Chemistry, 页码：7946-7949 , 文章类型： Article，,卷期：2009年52-24] By use of chemical enablement and prospective design, it novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP. Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a [作者：LIU FENG; CHEN XIN; ALLALIHASSANI ABDELLAH; QUINN AMY M; WASNEY GREGORY A; DONG AIPING; BARSYTE DALIA; KOZIERADZKI IVONA; SENISTERRA GUILLERMO; CHAU IRENE; SIARHEYEVA ALENA; KIREEV DMITRI B; JADHAV AJIT; HEROLD J MARTIN; FRYE STEPHEN V; ARROWSMITH CHERYL H; BROWN PETER J; SIMEONOV ANTON; VEDADI MASOUD; JIN JIAN,期刊：Journal of Medicinal Chemistry, 页码：7950-7953 , 文章类型： Article，,卷期：2009年52-24] SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as it potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the G9a-8 complex, the first... Enhancement of the Antimalarial Activity of Ciprofloxacin Using a Double Prodrug/Bioorganometallic Approach [作者：DUBAR FAUSTINE; ANQUETIN GUILLAUME; PRADINES BRUNO; DIVE DANIEL; KHALIFE JAMAL; BIOT CHRISTOPHE,期刊：Journal of Medicinal Chemistry, 页码：7954-7957 , 文章类型： Article，,卷期：2009年52-24] The derivatization of the fluoroquinolone ciprofloxacin greatly increases its antimalarial activity by combining bioorganometallic chemistry and the prodrug approach. Two new achiral compounds 2 and 4 were found to be 10...