个性化文献订阅>文章检索

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44条记录   Molecular Mechanisms of Acquired Proteasome Inhibitor Resistance [作者：KALE ANDREW J; MOORE BRADLEY S,期刊：Journal of Medicinal Chemistry, 页码：10317-10327 , 文章类型： Article，,卷期：2012年55-23] The development of proteasome inhibitors (Pis) has transformed the treatment of multiple myeloma and mantle cell lymphoma. To date, two PIs have been FDA approved, the boronate peptide bortezomib and, most recently, the ... Effects of Antimalarial Molecules on the Gametocyte Stage of Plasmodium falciparum: The Debate [作者：DECHYCABARET ODILE; BENOITVICAL FRANCOISE,期刊：Journal of Medicinal Chemistry, 页码：10328-10344 , 文章类型： Article，,卷期：2012年55-23] Although the illness malaria is caused by the asexual blood stages, the presence of gametocytes is directly responsible for the infection of the vector Anopheles, thus perpetuating the plasmodial cycle. Fight against mal... A Prospect for Pyrrolidine Iminosugars as Antidiabetic alpha-Glucosidase Inhibitors [作者：TRAPERO ANA; LLEBARIA AMADEU,期刊：Journal of Medicinal Chemistry, 页码：10345-10346 , 文章类型： Editorial Material，,卷期：2012年55-23] alpha-1-C-Butyl-1,4-dideoxy-1,4-imino-L-arabinitol as a Second-Generation Iminosugar-Based Oral alpha-Glucosidase Inhibitor for Improving Postprandial Hyperglycemia [作者：KATO ATSUSHI; HAYASHI ERINA; MIYAUCHI SAORI; ADACHI ISAO; IMAHORI TATSUSHI; NATORI YOSHIHIRO; YOSHIMURA YUICHI; NASH ROBERT J; SHIMAOKA HIDEYUKI; NAKAGOME IZUMI; KOSEKI JUN; HIRONO SHUICHI; TAKAHATA HIROKI,期刊：Journal of Medicinal Chemistry, 页码：10347-10362 , 文章类型： Article，,卷期：2012年55-23] We report on the synthesis and the biological evaluation of a series of alpha-1-C-alkylated 1,4-dideoxy-1,4-imino-L-arabinitol (LAB) derivatives. The asymmetric synthesis of the derivatives was achieved by asymmetric all... Synthesis and Biological Evaluation of Tylophorine-Derived Dibenzoquinolines as Orally Active Agents: Exploration of the Role of Tylophorine E Ring on Biological Activity [作者：LEE YUEZHI; YANG CHENGWEI; HSU HSINGYU; QIU YAQI; YEH TENGKUANG; CHANG HSINYU; CHAO YUSHENG; LEE SHIOWJU,期刊：Journal of Medicinal Chemistry, 页码：10363-10377 , 文章类型： Article，,卷期：2012年55-23] A series of novel tylophorine-derived dibenzoquinolines has been synthesized and their biological activity evaluated. Three assays were conducted: inhibition of cancer cell proliferation, inhibition of TGEV replication f... Redox-active Magnetic Resonance Imaging Contrast Agents: Studies with Thiol-bearing 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetracetic Acid Derivatives [作者：JAGADISH BHUMASAMUDRAM; GUNTLE GERALD P; ZHAO DEZHENG; GOKHALE VIJAY; OZUMERZIFON TARIK J; AHAD ALI M; MASH EUGENE A; RAGHUNAND NATARAJAN,期刊：Journal of Medicinal Chemistry, 页码：10378-10386 , 文章类型： Article，,卷期：2012年55-23] The synthesis and structure-activity relationships of a homologous series of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid gadolinium(III) complexes bearing thiol-terminated alkyl side chains from three to nin... Mimicking the Intramolecular Hydrogen Bond: Synthesis, Biological Evaluation, and Molecular Modeling of Benzoxazines and Quinazolines as Potential Antimalarial Agents [作者：GEMMA SANDRA; CAMODECA CATERINA; BRINDISI MARGHERITA; BROGI SIMONE; KUKREJA GAGAN; KUNJIR SANIL; GABELLIERI EMANUELE; LUCANTONI LEONARDO; HABLUETZEL ANNETTE; TARAMELLI DONATELLA; BASILICO NICOLETTA; GUALDANI ROBERTA; TADINIBUONINSEGNI FRANCESCO; BARTOLOMMEI GIANLUCA; MONCELLI MARIA ROSA; MARTIN ROWENA E; SUMMERS ROBERT L; LAMPONI STEFANIA; SAVINI LUISA; FIORINI ISABELLA; VALOTI MASSIMO; NOVELLINO ETTORE; CAMPIANI GIUSEPPE; BUTINI STEFANIA,期刊：Journal of Medicinal Chemistry, 页码：10387-10404 , 文章类型： Article，,卷期：2012年55-23] The intramolecular hydrogen bond formed between a protonated amine and a neighboring H-bond acceptor group in the side chain of amodiaquine and isoquine is thought to play an important role in their antimalarial activiti... HIV-1 X4 Activities of Polycationic "Viologen" Based Dendrimers by Interaction with the Chemokine Receptor CXCR4: Study of Structure-Activity Relationship [作者：ASAFTEI SIMONA; HUSKENS DANA; SCHOLS DOMINIQUE,期刊：Journal of Medicinal Chemistry, 页码：10405-10413 , 文章类型： Article，,卷期：2012年55-23] A series of "viologen" based dendrimers with polycationic scaffold carrying 10, 18, 26, 42, and 90 charges per molecule were used to determine the structure-activity relationship (SAP.) with regard to HIV-1 inhibitory ac... Rational Design of Highly Selective Spleen Tyrosine Kinase Inhibitors [作者：LUCAS MATTHEW C; GOLDSTEIN DAVID M; HERMANN JOHANNES C; KUGLSTATTER ANDREAS; LIU WENJIAN; LUK KIN CHUN; PADILLA FERNANDO; SLADE MICHELLE; VILLASENOR ARMANDO G; WANNER JUTTA; XIE WENWEI; ZHANG XIAOHU; LIAO CHENG,期刊：Journal of Medicinal Chemistry, 页码：10414-10423 , 文章类型： Article，,卷期：2012年55-23] A novel approach to design selective spleen tyrosine kinase (Syk) inhibitors is described. Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of autoimmune diseases such as... Synthesis of New 7-Oxycoumarin Derivatives As Potent and Selective Monoamine Oxidase A Inhibitors [作者：ABDELHAFEZ OMAIMA M; AMIN KAMELIA M; ALI HAMED I; ABDALLA MOHAMED M; BATRAN RASHA Z,期刊：Journal of Medicinal Chemistry, 页码：10424-10436 , 文章类型： Article，,卷期：2012年55-23] New series of 4-methyl and 3,4-dimethy1-7-oxycoumarin derivatives (oxadiazoles, thiadiazoles, triazoles, and thiazolidinones) were designed, synthesized, and evaluated for their monoamine oxidase (MAO) A and B inhibiting... Designed Glucopeptides Mimetics of Myelin Protein Epitopes As Synthetic Probes for the Detection of Autoantibodies, Biomarkers of Multiple Sclerosis [作者：PANDEY SHASHANK; ALCARO MARIA C; SCRIMA MARIO; PERONI ELISA; PAOLINI ILARIA; DI MARINO SARA; BARBETTI FRANCESCA; CAROTENUTO ALFONSO; NOVELLINO ETTORE; PAPINI ANNA MARIA; DURSI ANNA MARIA; ROVERO PAOLO,期刊：Journal of Medicinal Chemistry, 页码：10437-10447 , 文章类型： Article，,卷期：2012年55-23] We previously reported that CSF114(Glc) detects diagnostic autoantibodies in multiple sclerosis sera. We report herein a bioinformatic analysis of myelin proteins and CSF114(Glc), which led to the identification of five ... Copper-Dependent Cytotoxicity of 8-Hydroxyquinoline Derivatives Correlates with Their Hydrophobicity and Does Not Require Caspase Activation [作者：TARDITO SAVERIO; BARILLI AMELIA; BASSANETTI IRENE; TEGONI MATTEO; BUSSOLATI OVIDIO; FRANCHIGAZZOLA RENATA; MUCCHINO CLAUDIO; MARCHIO LUCIANO,期刊：Journal of Medicinal Chemistry, 页码：10448-10459 , 文章类型： Article，,卷期：2012年55-23] This study reports the structure-activity relationship of a series of 8-hydroxoquinoline derivatives (8-HQs) and focuses on the cytotoxic activity of 5-Cl-7-I-8-HQ (clioquinol, CQ) copper complex (Cu(CQ)). 8-HQs alone ca... Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine-Glycine-Aspartate (RGD) Peptidomimetic-Paclitaxel Conjugates Targeting lntegrin alpha(v)beta(3) [作者：COLOMBO RAFFAELE; MINGOZZI MICHELE; BELVISI LAURA; AROSIO DANIELA; PIARULLI UMBERTO; CARENINI NIVES; PEREGO PAOLA; ZAFFARONI NADIA; DE CESARE MICHELANDREA; CASTIGLIONI VITTORIA; SCANZIANI EUGENIO; GENNARI CESARE,期刊：Journal of Medicinal Chemistry, 页码：10460-10474 , 文章类型： Article，,卷期：2012年55-23] A small library of integrin ligand paclitaxel conjugates 10-13 was synthesized with the aim of using the tumor-homing cyclo[DKP-RGD] peptidomimetics for site-directed delivery of the cytotoxic drug. All the paclitaxel-RG... Design, Synthesis, and Antidiabetic Activity of 4-Phenoxynicotinamide and 4-Phenoxypyrimidine-5-carboxamide Derivatives as Potent and Orally Efficacious TGR5 Agonists [作者：DUAN HONGLIANG; NING MENGMENG; CHEN XIAOYAN; ZOU QINGAN; ZHANG LIMING; FENG YING; ZHANG LINA; LENG YING; SHEN JIANHUA,期刊：Journal of Medicinal Chemistry, 页码：10475-10489 , 文章类型： Article，,卷期：2012年55-23] 4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (... Conjugation of Quinones with Natural Polyamines: Toward an Expanded Antitrypanosomatid Profile [作者：LIZZI FEDERICA; VERONESI GIACOMO; BELLUTI FEDERICA; BERGAMINI CHRISTIAN; LOPEZSANCHEZ ALMUDENA; KAISER MARCEL; BRUN RETO; KRAUTHSIEGEL R LUISE; HALL DENNIS G; RIVAS LUIS; BOLOGNESI MARIA LAURA,期刊：Journal of Medicinal Chemistry, 页码：10490-10500 , 文章类型： Article，,卷期：2012年55-23] A combinatorial library of quinone-polyamine conjugates designed to optimize the antitrypanosomatid profile of hit compounds 1 and 2 has been prepared by a solid-phase approach. The conjugates were evaluated against the ... The Multi-Leu Peptide Inhibitor Discriminates Between PACE4 and Furin And Exhibits Antiproliferative Effects On Prostate Cancer Cells [作者：LEVESQUE CHRISTINE; FUGERE MARTIN; KWIATKOWSKA ANNA; COUTURE FREDERIC; DESJARDINS ROXANE; ROUTHIER SOPHIE; MOUSSETTE PHILIPPE; PRAHL ADAM; LAMMEK BERNARD; APPEL JON R; HOUGHTEN RICHARD A; DANJOU FRANCOIS; DORY YVES L; NEUGEBAUER WITOLD; DAY ROBERT,期刊：Journal of Medicinal Chemistry, 页码：10501-10511 , 文章类型： Article，,卷期：2012年55-23] The proprotein convertases (PCs) play an important role in protein precursor activation through processing at paired basic residues. However, significant substrate cleavage redundancy has been reported between PCs. The q...