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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42条记录   Novel N-2-Substituted Pyrazolo[3,4-d]pyrimidine Adenosine A(3) Receptor Antagonists: Inhibition of A(3)-Mediated Human Glioblastoma Cell Proliferation [作者：TALIANI SABRINA; LA MOTTA CONCETTINA; MUGNAINI LAURA; SIMORINI FRANCESCA; SALERNO SILVIA; MARINI ANNA MARIA; DA SETTIMO FEDERICO; COSCONATI SANDRO; COSIMELLI BARBARA; GRECO GIOVANNI; LIMONGELLI VITTORIO; MARINELLI LUCIANA; NOVELLINO ETTORE; CIAMPI OSELE; DANIELE SIMONA; TRINCAVELLI MARIA LETIZIA; MARTINI CLAUDIA,期刊：Journal of Medicinal Chemistry, 页码：3954-3963 , 文章类型： Article，,卷期：2010年53-10] Adenosine induces glioma cell proliferation by means of an antiapoptotic effect, which is blocked by cotreatment with selective A(3) AR antagonists. In this study, a novel series of N-2-substituted pyrazolo[3,4-d]pyrimid... Phenylcinnamides as Novel Antimitotic Agents [作者：LESLIE BENJAMIN J; HOLADAY CLINTON R; NGUYEN TRAN; HERGENROTHER PAUL J,期刊：Journal of Medicinal Chemistry, 页码：3964-3972 , 文章类型： Article，,卷期：2010年53-10] Compound 8H is a phenylcinnamide that induces G2/M-phase cell cycle arrest and cell death in cancer cell lines. Here we show that 811 exerts its cytotoxic activity through disruption of microtubule dynamics in vitro and ... Discovery of GSK1070916, a Potent and Selective Inhibitor of Aurora B/C Kinase [作者：ADAMS NICHOLAS D; ADAMS JERRY L; BURGESS JOELLE L; CHAUDHARI AMITA M; COPELAND ROBERT A; DONATELLI CARLA A; DREWRY DAVID H; FISHER KELLY E; HAMAJIMA TOSHIHIRO; HARDWICKE MARY ANN; HUFFMAN WILLIAM F; KORETKEBROWN KRISTIN K; LAI ZHIHONG V; MCDONALD OCTERLONEY B; NAKAMURA HIROKO; NEWLANDER KEN A; OLEYKOWSKI CATHERINE A; PARRISH CYNTHIA A; PATRICK DENIS R; PLANT RAMONA; SARPONG MARTHA A; SASAKI KOSUKE; SCHMIDT STANLEY J; SILVA DOMINGOS J; SUTTON DAVID; TANG JUN; THOMPSON CHRISTINE S; TUMMINO PETER J; WANG JAMIN C; XIANG HONG; YANG JINGSONG; DHANAK DASHYANT,期刊：Journal of Medicinal Chemistry, 页码：3973-4001 , 文章类型： Article，,卷期：2010年53-10] The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora ki... Structural Evidence That Human Acetylcholinesterase Inhibited by Tabun Ages through O-Dealkylation [作者：CARLETTI EUGENIE; COLLETIER JACQUESPHILIPPE; DUPEUX FLORINE; TROVASLET MARIE; MASSON PATRICK; NACHON FLORIAN,期刊：Journal of Medicinal Chemistry, 页码：4002-4008 , 文章类型： Article，,卷期：2010年53-10] Tabun is a warfare agent that inhibits human acetylcholinesterase (hAChE) by rapid phosphylation of the catalytic serine. A time-dependent reaction occurs on the tabun adduct, leading to an "aged" enzyme, resistant to ox... Structure-Activity Relationships of Fluorinated (E)-3-((6-Methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) Derivatives and the Discovery of a High Affinity Analogue as a Potential Candidate for Imaging Metabotropic Glutamate Recepors Subtype 5 (mGluR5) with Positron Emission Tomography (PET) [作者：BAUMANN CINDY A; MU LINJING; JOHANNSEN SINJA; HONER MICHAEL; SCHUBIGER PIUS A; AMETAMEY SIMON M,期刊：Journal of Medicinal Chemistry, 页码：4009-4017 , 文章类型： Article，,卷期：2010年53-10] The metabotropic glutamate receptor subtype 5 (mGluR5) is recognized to be involved in numerous brain disorders. In an effort to obtain a fluorine-18 labeled analogue of the mGluR5 PET tracer [C-11]ABP688, 13 novel ligan... In Vitro Photodynamic Therapy and Quantitative Structure-Activity Relationship Studies with Stable Synthetic Near-Infrared-Absorbing Bacteriochlorin Photosensitizers [作者：HUANG YINGYING; MROZ PAWEL; ZHIYENTAYEV TIMUR; SHARMA SULBHA K; BALASUBRAMANIAN THIAGARAJAN; RUZIE CHRISTIAN; KRAYER MICHAEL; FAN DAZHONG; BORBAS K ESZTER; YANG EUNKYUNG; KEE HOOI LING; KIRMAIER CHRISTINE; DIERS JAMES R; BOCIAN DAVID F; HOLTEN DEWEY; LINDSEY JONATHAN S; HAMBLIN MICHAEL R,期刊：Journal of Medicinal Chemistry, 页码：4018-4027 , 文章类型： Article，,卷期：2010年53-10] Photodynamic therapy (PDT) is a rapidly developing approach to treating cancer that combines harmless visible and near-infrared light with a nontoxic photoactivatable dye, which upon encounter with molecular oxygen gener... Discovery of N-[(4R)-6-(4-Chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a Novel Cannabinoid-1 Receptor (CB1R) Inverse Agonist for the Treatment of Obesity [作者：YAN LIN; HUO PEI; DEBENHAM JOHN S; MADSENDUGGAN CHRISTINA B; LAO JULIE; CHEN RICHARD Z; XIAO JING CHEN; SHEN CHUNPYN; STRIBLING D SLOAN; SHEARMAN LAUREN P; STRACK ALISON M; TSOU NANCY; BALL RICHARD G; WANG JUNYING; TONG XINCHUN; BATEMAN THOMAS J; REDDY VIJAY B G; FONG TUNG M; HALE JEFFREY J,期刊：Journal of Medicinal Chemistry, 页码：4028-4037 , 文章类型： Article，,卷期：2010年53-10] This paper describes the discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihy dro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596, 12c) as a novel cannabinoid-1 r... Conserved Structural Motif for Recognizing Nicotinamide Adenine Dinucleotide in Poly(ADP-ribose) Polymerases and ADP-Ribosylating Toxins: Implications for Structure-Based Drug Design [作者：LEE YUMING; BABU C SATHEESAN; CHEN YAO CHI; MILCIC MILOS; QU YUANYUAN; LIM CARMAY,期刊：Journal of Medicinal Chemistry, 页码：4038-4049 , 文章类型： Article，,卷期：2010年53-10] The ADP-ribosylating toxins (ADPRTs) and poly(ADP-ribose) polymerases (PARPs) are two important drug target protein families. Although the Y-X-10-Y motif for the diphtheria toxin group and the STS motif for the other ADP... Synthetic N-Acetyl-D-glucosamine Based Fully Branched Tetrasaccharide, a Mimetic of the Endogenous Ligand for CD69, Activates CD69(+) Killer Lymphocytes upon Dimerization via a Hydrophilic Flexible Linker [作者：KOVALOVA ANNA; LEDVINA MIROSLAV; SAMAN DAVID; ZYKA DANIEL; KUBICKOVA MONIKA; ZIDEK LUKAS; SKLENAR VLADIMIR; POMPACH PETR; KAVAN DANIEL; BILY JAN; VANEK ONDREJ; KUBINKOVA ZUZANA; LIBIGEROVA MARTINA; IVANOVA LJUBINA; ANTOLIKOVA MARIA; MRAZEK HYNEK; ROZBESKY DANIEL; HOFBAUEROVA KATERINA; KREN VLADIMIR; BEZOUSKA KAREL,期刊：Journal of Medicinal Chemistry, 页码：4050-4065 , 文章类型： Article，,卷期：2010年53-10] On the basis of the highly branched ovomucoid-type undecasaccharide that had been shown previously to be an endogenous ligand for CD69 leukocyte receptor, a systematic investigation of smaller oligosaccharide mimetics wa... The Synthesis and Biological Evaluation of Quinolyl-piperazinyl Piperidines as Potent Serotonin 5-HT1A Antagonists [作者：CHILDERS WAYNE E JR; HAVRAN LISA M; ASSELIN MAGDA; BICKSLER JAMES J; CHONG DAN C; GROSU GEORGE T; SHEN ZHONGQI; ABOUGHARBIA MAGID A; BACH ALVIN C III; HARRISON BOYD L; KAGAN NATASHA; KLEINTOP TERESA; MAGOLDA RONALD; MARATHIAS VASILIOS; ROBICHAUD ALBERT J; SABB ANNMARIE L; ZHANG MEIYI; ANDREE TERRANCE H; ASCHMIES SUSAN H; BEYER CHAD; COMERY THOMAS A; DAY MARK; GRAUER STEVEN M; HUGHES ZOE A; ROSENZWEIGLIPSON SHARON; PLATT BRIAN; PULICICCHIO CLAUDINE; SMITH DEBORAH E; SUKOFFRIZZO STACY J; SULLIVAN KELLY M; ADEDOYIN ADEDAYO; HUSELTON CHRISTINE; HIRST WARREN D,期刊：Journal of Medicinal Chemistry, 页码：4066-4084 , 文章类型： Article，,卷期：2010年53-10] As part of an effort to identify 5-HT1A antagonists that did not possess typical arylalkylamine or keto/amido-alkyl aryl piperazine scaffolds, prototype compound 10a was identified from earlier work in a combined 5-HT1A ... Novel Irreversible Fluorescent Probes Targeting the 18 kDa Translocator Protein: Synthesis and Biological Characterization [作者：TALIANI SABRINA; DA POZZO ELEONORA; BELLANDI MARUSCA; BENDINELLI SARA; PUGLIESI ISABELLA; SIMORINI FRANCESCA; LA MOTTA CONCETTINA; SALERNO SILVIA; MARINI ANNA MARIA; DA SETTIMO FEDERICO; COSIMELLI BARBARA; GRECO GIOVANNI; NOVELLINO ETTORE; MARTINI CLAUDIA,期刊：Journal of Medicinal Chemistry, 页码：4085-4093 , 文章类型： Article，,卷期：2010年53-10] The 18 kDa translocator protein (TSPO) is a mitochondrial protein whose basal density is altered in several diseases, with the result that the evaluation of its expression levels by means of molecular imaging techniques ... Iminochromene Inhibitors of Dynamins I and II GTPase Activity and Endocytosis [作者：HILL TIMOTHY A; MARIANA ANNA; GORDON CHRISTOPHER P; ODELL LUKE R; ROBERTSON MARK J; MCGEACHIE ANDREW B; CHAU NGOC; DANIEL JAMES A; GORGANI NICK N; ROBINSON PHILLIP J; MCCLUSKEY ADAM,期刊：Journal of Medicinal Chemistry, 页码：4094-4102 , 文章类型： Article，,卷期：2010年53-10] Herein we report the synthesis of discrete iminochromene ("iminodyn") libraries (14-38) as potential inhibitors of dynamin GTPase. Thirteen iminodyns were active (IC50 values of 260 nM to 100 mu M), with N,N-(ethane-1,2-... Trioxaferroquines as New Hybrid Antimalarial Drugs [作者：BELLOT FRANCOIS; COSLEDAN FREDERIC; VENDIER LAURE; BROCARD JACQUES; MEUNIER BERNARD; ROBERT ANNE,期刊：Journal of Medicinal Chemistry, 页码：4103-4109 , 文章类型： Article，,卷期：2010年53-10] The synthesis, characterization, and antimalarial evaluation of a new series of potential antimalarial molecules, named trioxaferroquines, are reported. Trioxaferroquines are hybrid antimalarial drugs containing a 1,2,4-... 4-Hydroxy-1,2,5-oxadiazol-3-yl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Molecular Pharmacological Characterization at Ionotropic Glutamate Receptors of Compounds Related to Glutamate and Its Homologues [作者：LOLLI MARCO L; GIORDANO CECILIA; PICKERING DARRYL S; ROLANDO BARBARA; HANSEN KASPER B; FOTI ANTONIO; CONTRERASSANZ ALBERTO; AMIR AHMAD; FRUTTERO ROBERTA; GASCO ALBERTO; NIELSEN BIRGITTE; JOHANSEN TOMMY N,期刊：Journal of Medicinal Chemistry, 页码：4110-4118 , 文章类型： Article，,卷期：2010年53-10] In order to investigate the 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as a carboxylic acid bioisoster at ionotropic glutamate receptors (iGluRs), a series of acidic alpha-aminocarboxylic acids in which the distal carboxy gro... Sequence Inversion and Phenylalanine Surrogates at the beta-Turn Enhance the Antibiotic Activity of Gramicidin S [作者：SOLANAS CONCEPCION; DE LA TORRE BEATRIZ G; FERNANDEZREYES MARIA; SANTIVERI CLARA M; ANGELES JIMENEZ M; RIVAS LUIS; JIMENEZ ANA I; ANDREU DAVID; CATIVIELA CARLOS,期刊：Journal of Medicinal Chemistry, 页码：4119-4129 , 文章类型： Article，,卷期：2010年53-10] A series of gramicidin S (GS) analogues have been synthesized where the Phe (i + 1) and Pro (i + 2) residues of the beta-turn have been swapped while the respective chiralities (D-, L-) at each position are preserved, an... 3 '-Bromo Analogues of Pyrimidine Nucleosides as a New Class of Potent Inhibitors of Mycobacterium tuberculosis [作者：SHAKYA NEERAJ; SRIVASTAV NAVEEN C; DESROCHES NANCY; AGRAWAL BABITA; KUNIMOTO DENNIS Y; KUMAR RAKESH,期刊：Journal of Medicinal Chemistry, 页码：4130-4140 , 文章类型： Article，,卷期：2010年53-10] Tuberculosis (TB) is a major health problem worldwide. We herein report a new class of pyrimidine nucleosides as potent inhibitors of Mycobacterium tuberculosis (M. tuberculosis). Various 2'- or 3'-halogeno derivatives o...