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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14条记录   Assessment of Partially Deoxygenated Deoxynojirimycin Derivatives as Glucosylceramide Synthase Inhibitors [作者：VAN DEN BERG RICHARD J B H N; WENNEKES TOM; GHISAIDOOBE AMAR; DONKERKOOPMAN WILMA E; STRIJLAND ANNEKE; BOOT ROLF G; VAN DER MAREL GIJSBERT A; AERTS JOHANNES M F G; OVERKLEEFT HERMAN S,期刊：ACS Medicinal Chemistry Letters, 页码：519-522 , 文章类型： Article，,卷期：2011年2-7] Glucosylceramide synthase (GCS) is an approved drug target for the treatment of Gaucher disease and is considered as a valid target for combating other human pathologies, including type 2 diabetes. The clinical drug N-bu... Chemical Transformations That Yield Compounds with Distinct Activity Profiles [作者：HU YE; BAJORATH JUERGEN,期刊：ACS Medicinal Chemistry Letters, 页码：523-527 , 文章类型： Article，,卷期：2011年2-7] We have systematically searched for chemical changes that generate compounds with distinct biological activity profiles. For this purpose, activity profiles were generated for similar to 42000 compounds active against hu... Targeting Anthracycline-Resistant Tumor Cells with Synthetic Aloe-Emodin Glycosides [作者：BREINERGOLDSTEIN ELINOR; EVRON ZOHARIA; FRENKEL MICHAEL; COHEN KEREN; MEIRON KEREN NIR; PEER DAN; ROICHMAN YAEL; FLESCHER ELIEZER; FRIDMANT MICHA,期刊：ACS Medicinal Chemistry Letters, 页码：528-531 , 文章类型： Article，,卷期：2011年2-7] The cytotoxic activity of aloe-emodin (AE), a natural anthranoid that readily permeates anthracycline-resistant tumor cells, was improved by the attachment of an amino-sugar unit to its anthraquinone core. The new class ... Structure-Activity Relationship Studies of HIV-1 Integrase Oligonucleotide Inhibitors [作者：AGAPKINA JULIA; ZATSEPIN TIMOFEI; KNYAZHANSKAYA EKATERINA; MOUSCADET JEANFRANCOIS; GOTTIKH MARINA,期刊：ACS Medicinal Chemistry Letters, 页码：532-537 , 文章类型： Article，,卷期：2011年2-7] Integration of human immunodeficiency virus type 1 DNA into an infected cell genome is one of the key steps of the viral replication cycle. Therefore, viral enzyme integrase, which realizes the integration, represents an... Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site [作者：MARYANOFF BRUCE E; ONEILL JOHN C; MCCOMSEY DAVID F; YABUT STEPHEN C; LUCI DIANE K; JORDAN ALFONZO D JR; MASUCCI JOHN A; JONES WILLIAM J; ABAD MARTA C; GIBBS ALAN C; PETROUNIA IOANNA,期刊：ACS Medicinal Chemistry Letters, 页码：538-543 , 文章类型： Article，,卷期：2011年2-7] Attenuation of fructose metabolism by the inhibition of ketohexokinase (KHK; fructokinase) should reduce body weight, free fatty acids, and triglycerides, thereby offering a novel approach to treat diabetes and obesity i... Screening for GPCR Ligands Using Surface Plasmon Resonance [作者：NAVRATILOVA IVA; BESNARD JEREMY; HOPKINS ANDREW L,期刊：ACS Medicinal Chemistry Letters, 页码：549-554 , 文章类型： Article，,卷期：2011年2-7] G-protein coupled receptors (GPCRs) are a class of drug targets of primary importance. However, receptor assays are based on measurement of either ligand displacement or downstream functional responses, rather than direc... A Platform for the Detection of Trypanosomes via Selective Small Molecule Recognition [作者：BEAULIEU ELLEN D; OLSON LORI L; TANGA MARY J,期刊：ACS Medicinal Chemistry Letters, 页码：555-558 , 文章类型： Article，,卷期：2011年2-7] Trypanothione (TSH(2)), a metabolite unique to trypanosomal parasites, was evaluated as a potential biomarker for trypanosomal infection using fluorescence as the means of detection. Fluoroescein arsenical helix binder (... The 3-Deoxy Analogue of alpha-GalCer: Disclosing the Role of the 4-Hydroxyl Group for CD1d-Mediated NKT Cell Activation [作者：BAEK DONG JAE; SEO JEONGHWAN; LIM CHAEMIN; KIM JAE HYUN; CHUNG DOO HYUN; CHO WONJEA; KANG CHANGYUIL; KIM SANGHEE,期刊：ACS Medicinal Chemistry Letters, 页码：544-548 , 文章类型： Article，,卷期：2011年2-7] KRN7000, or alpha-GalCer, is a potent agonist for natural killer T (NKT) cells. The 3-hydroxyl group of its phytosphingosine moiety is important for activating NKT cells, whereas its 4-hydroxyl group is perceived to be l... Target Flexibility in RNA-Ligand Docking Modeled by Elastic Potential Grids [作者：KRUEGER DENNIS M; BERGS JOHANNES; KAZEMI SINA; GOHLKE HOLGER,期刊：ACS Medicinal Chemistry Letters, 页码：489-493 , 文章类型： Article，,卷期：2011年2-7] The highly flexible nature of RNA provides a formidable challenge for structure-based drug design approaches that target RNA. We introduce an approach for modeling target conformational changes in RNA-ligand docking base... Nitric Oxide Donor Doxorubicins Accumulate into Doxorubicin-Resistant Human Colon Cancer Cells Inducing Cytotoxicity [作者：CHEGAEV KONSTANTIN; RIGANTI CHIARA; LAZZARATO LORETTA; ROLANDO BARBARA; GUGLIELMO STEFANO; CAMPIA IVANA; FRUTTERO ROBERTA; BOSIA AMALIA; GASCO ALBERTO,期刊：ACS Medicinal Chemistry Letters, 页码：494-497 , 文章类型： Article，,卷期：2011年2-7] Products 4 and 5, obtained by conjugation of doxorubicin with nitric oxide (NO) donor nitrooxy and phenylsulfonyl furoxan moieties, respectively, accumulate in doxorubicin-resistant human colon cancer cells (HT29-dx), in... Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as beta-Amyloid PET Ligands and Identification of MK-3328 [作者：HARRISON SCOTT T; MULHEARN JAMES; WOLKENBERG SCOTT E; MILLER PATRICIA J; OMALLEY STACEY S; ZENG ZHIZHEN; WILLIAMS DAVID L JR; HOSTETLER ERIC D; SANABRIABOHORQUEZ SANDRA; GAMMAGE LINDA; FAN HONG; SUR CYRILLE; CULBERSON J CHRISTOPHER; HARGREAVES RICHARD J; COOK JACQUELYNN J; HARTMAN GEORGE D; BARROW JAMES C,期刊：ACS Medicinal Chemistry Letters, 页码：498-502 , 文章类型： Article，,卷期：2011年2-7] 5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential (18)F containing beta-amyloid PET ligands. In competition binding assays using human AD brain homogenates, compounds 14b, 16b, and 17b... Novel Alkynylphosphonate Analogue of Calcitriol with Potent Antiproliferative Effects in Cancer Cells and Lack of Calcemic Activity [作者：SALOMON DEBORA G; GRIOLI SILVINA M; BUSCHIAZZO MAXIMILIANO; MASCARO EVANGELINA; VITALE CRISTIAN; RADIVOY GABRIEL; PEREZ MANUEL; FALL YAGAMARE; MESRI ENRIQUE A; CURINO ALEJANDRO C; FACCHINETTI MARIA M,期刊：ACS Medicinal Chemistry Letters, 页码：503-508 , 文章类型： Article，,卷期：2011年2-7] Here, we describe the design and synthesis of diethyl [(5Z,7E)-(1S,3R)-1,3-dihydroxy-9,10-secochola-5,7,10(19)-trien-23-in-24- yl] phosphonate (compound 10), which combines the low calcemic properties of phosphonates wit... N-Methylated sst(2) Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation [作者：CHATTERJEE JAYANTA; LAUFER BURKHARDT; BECK JOHANNES G; HELYES ZSUZSANNA; PINTER ERIKA; SZOLCSANYI JANOS; HORVATH ANIKO; MANDL JOZSEF; REUBI JEAN C; KERI GYOERGY; KESSLER HORST,期刊：ACS Medicinal Chemistry Letters, 页码：509-514 , 文章类型： Article，,卷期：2011年2-7] A focused multiply N-methylated library of a cyclic hexapeptidic somatostatin analogue: MK678 cyclo(-MeAYwKVF-) was generated, which resulted in the unexpected observation of an efficacious tetra-N-methylated analogue, c... Benzodiazepinone Derivatives as CRTH2 Antagonists [作者：LIU JIWEN JIM; CHENG ALAN C; TANG H LUCY; MEDINA JULIO C,期刊：ACS Medicinal Chemistry Letters, 页码：515-518 , 文章类型： Article，,卷期：2011年2-7] Multiple CRTH2 antagonists are currently evaluated in human clinical trials for asthma and chronic obstructive pulmonary disease (COPD). During our lead optimization for CRTH2 antagonists, an observation of an intramolec...