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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   Concise Syntheses of the Abyssinones and Discovery of New Inhibitors of Prostate Cancer and MMP-2 Expression (vol 1, pg 400, 2010) [作者：FARMER REBECCA L; BIDDLE MARGARET M; NIBBS ANTOINETTE E; HUANG XIAOKE; XU LI; BERGAN RAYMOND C; SCHEIDT KARL A,期刊：ACS Medicinal Chemistry Letters, 页码：257-257 , 文章类型： Correction，,卷期：2011年2-3] Novel, Broad Spectrum Anticancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System [作者：KONDASKAR ATUL; KONDASKAR SHILPI; KUMAR RAJ; FISHBEIN JAMES C; MUVARAK NIDAL; LAPIDUS RENA G; SADOWSKA MARIOLA; EDELMAN MARTIN J; BOL GUUS M; VESUNA FARHAD; RAMAN VENU; HOSMANE RAMACHANDRA S,期刊：ACS Medicinal Chemistry Letters, 页码：252-256 , 文章类型： Article，,卷期：2011年2-3] Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4',5'-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promi... Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D-2 Receptors [作者：SROMEK ANNA W; SI YUGUI; ZHANG TANGZHI; GEORGE SUSAN R; SEEMAN PHILIP; NEUMEYER JOHN L,期刊：ACS Medicinal Chemistry Letters, 页码：189-194 , 文章类型： Article，,卷期：2011年2-3] The 2-fluoroalkoxy-substituted catechol-aporphines 6, 8a-f and 11-mono-hydroxyaporphines 11a-e were synthesized and found to have high in vitro affinity and selectivity for the dopamine D-2 receptors. The catechol aporph... Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1 [作者：DENG XIANMING; YANG QINGKAI; KWIATKOWSKI NICHOLAS; SIM TAEBO; MCDERMOTT ULTAN; SETTLEMAN JEFFREY E; LEE JIINGDWAN; GRAY NATHANAEL S,期刊：ACS Medicinal Chemistry Letters, 页码：195-200 , 文章类型： Article，,卷期：2011年2-3] Kinome-wide selectivity profiling of a collection of 2-amino-pyrido[2,3-d]pyrimidines followed by cellular structure activity relationship-guided optimization resulted in the identification of moderately potent and selec... Inhibitory Effect of Silver Nanoparticles on Trypanothione Reductase Activity and Leishmania infantum Proliferation [作者：BAIOCCO PAOLA; ILARI ANDREA; CECI PIERPAOLO; ORSINI STEFANIA; GRAMICCIA MARINA; DI MUCCIO TRENTINA; COLOTTI GIANNI,期刊：ACS Medicinal Chemistry Letters, 页码：230-233 , 文章类型： Article，,卷期：2011年2-3] In Leishmania the glutathione/glutathione reductase eukaryotic redox system is replaced by the unique trypanothione/trypanothione reductase (TR) system. In vitro, silver is a more effective TR inhibitor than antimony, th... Extracting SAR Information from a Large Collection of Anti-Malarial Screening Hits by NSG-SPT Analysis [作者：WAWER MATHIAS; BAJORATH JUERGEN,期刊：ACS Medicinal Chemistry Letters, 页码：201-206 , 文章类型： Article，,卷期：2011年2-3] We combine two graphical SAR analysis methods, Network-like Similarity Graphs (NSGs) and Similarity-Potency Trees (SPTs), to search for SAR information in a large and heterogeneous compound data set containing more than ... Structure Guided Development of Potent Reversibly Binding Penicillin Binding Protein Inhibitors [作者：WOON ESTHER C Y; ZERVOSEN ASTRID; SAUVAGE ERIC; SIMMONS KATIE J; ZIVEC MATEJ; INGLIS STEVEN R; FISHWICK COLIN W G; GOBEC STANISLAV; CHARLIER PAULETTE; LUXEN ANDRE; SCHOFIELD CHRISTOPHER J,期刊：ACS Medicinal Chemistry Letters, 页码：219-223 , 文章类型： Article，,卷期：2011年2-3] Following from the evaluation of different types of electrophiles, combined modeling and crystallographic analyses are used to generate potent boronic acid based inhibitors of a penicillin binding protein. The results su... Inhibitors of HCV NS5A: From Iminothiazolidinones to Symmetrical Stilbenes [作者：ROMINE JEFFREY L; ST LAURENT DENIS R; LEET JOHN E; MARTIN SCOTT W; SERRANOWU MICHAEL H; YANG FUKANG; GAO MIN; OBOYLE DONALD R II; LEMM JULIE A; SUN JINHUA; NOWER PETER T; HUANG XIAOHUA STELLA; DESHPANDE MILIND S; MEANWELL NICHOLAS A; SNYDER LAWRENCE B,期刊：ACS Medicinal Chemistry Letters, 页码：224-229 , 文章类型： Article，,卷期：2011年2-3] The iminothiazolidinone BMS-858 (2) was identified as a specific inhibitor of HCV replication in a genotype 1b replicon assay via a high-throughput screening campaign. A more potent analogue, BMS-824 (18), was used in re... Discovery of a Potent and Short-Acting Oral Calcilytic with a Pulsatile Secretion of Parathyroid Hormone [作者：SHINAGAWA YUKO; INOUE TERUHIKO; KATSUSHIMA TAKEO; KIGUCHI TOSHIHIRO; IKENOGAMI TAKU; OGAWA NAOKI; FUKUDA KENJI; HIRATA KAZUYUKI; HARADA KAZUHITO; TAKAGI MASAKI; NAKAGAWA TAKASHI; KIMURA SHUICHI; MATSUO YUSHI; MAEKAWA MARIKO; HAYASHI MILDO; SOEJIMA YUKI; TAKAHASHI MITSURU; SHINDO MASANORI; HASHIMOTO HIROMASA,期刊：ACS Medicinal Chemistry Letters, 页码：238-242 , 文章类型： Article，,卷期：2011年2-3] Short-acting oral calcilytics, calcium-sensing receptor (CaSR) antagonists, have been considered as alternatives for parathyroid hormone (PTH), an injectable bone anabolic drug used in the treatment of osteoporosis. Prev... Hybrid Dual Aromatase-Steroid Sulfatase Inhibitors with Exquisite Picomolar Inhibitory Activity [作者：WOO L W LAWRENCE; BUBERT CHRISTIAN; PUROHIT ATUL; POTTER BARRY V L,期刊：ACS Medicinal Chemistry Letters, 页码：243-247 , 文章类型： Article，,卷期：2011年2-3] Single agents against multiple drug targets are highly topical. Hormone-dependent breast cancer (HDBC) may be more effectively treated by dual inhibition of aromatase and steroid sulfatase (STS), and several dual aromata... In Vitro and In Vivo Osteogenic Activity of Largazole [作者：LEE SUUI; KWAK HAN BOK; PI SUNGHEE; YOU HYUNGKEUN; BYEON SEONG RIM; YING YONGCHENG; LUESCH HENDRIK; HONG JIYONG; KIM SEONG HWAN,期刊：ACS Medicinal Chemistry Letters, 页码：248-251 , 文章类型： Article，,卷期：2011年2-3] Due to their capability of modifying chromatin structure and thereby regulating gene transcription, histone deacetylases (HDACs) have been reported to play important roles in osteogenesis and considered a promising poten... Synthesis and Antibacterial Activity of a Novel Class of 15-Membered Macrolide Antibiotics, "11a-Azalides" [作者：SUGIMOTO TOMOHIRO; TANIKAWA TETSUYA,期刊：ACS Medicinal Chemistry Letters, 页码：234-237 , 文章类型： Article，,卷期：2011年2-3] An efficient method for the reconstruction of the 9-dihydroerythromycin A macrolactone skeleton has been established. The key steps are oxidative cleavage at the 11,12-position and reconstruction after insertion of an ap... Discovery of MK-1220: A Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure [作者：RUDD MICHAEL T; MCCAULEY JOHN A; BUTCHER JOHN W; ROMANO JOSEPH J; MCINTYRE CHARLES J; NGUYEN KEVIN T; GILBERT KEVIN F; BUSH KIMBERLY J; HOLLOWAY M KATHARINE; SWESTOCK JOHN; WAN BANGLIN; CARROLL STEVEN S; DIMUZIO JILLIAN M; GRAHAM DONALD J; LUDMERER STEVEN W; STAHLHUT MARK W; FANDOZZI CHRISTINE M; TRAINOR NICOLE; OLSEN DAVID B; VACCA JOSEPH P; LIVERTON NIGEL J,期刊：ACS Medicinal Chemistry Letters, 页码：207-212 , 文章类型： Article，,卷期：2011年2-3] The discovery of MK-1220 is reported along with the development of a series of HCV NS3/4A protease inhibitors containing a P2 to P4 macrocyclic constraint with improved preclinical pharmacokinetics. Optimization of the P... Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A(2B) Adenosine Receptor Antagonist [作者：EASTWOOD PAUL; ESTEVE CRISTINA; GONZALEZ JACOB; FONQUERNA SILVIA; AIGUADE JOSEP; CARRANCO INES; DOMENECH TERESA; APARICI MONICA; MIRALPEIX MONTSERRAT; ALBERTI JOAN; CORDOBA MONICA; FERNANDEZ RAQUEL; PONT MERCE; GODESSART NURIA; PRATS NEUS; ISABEL LOZA MARIA; ISABEL CADAVID MARIA; NUEDA ARSENIO; VIDAL BERNAT,期刊：ACS Medicinal Chemistry Letters, 页码：213-218 , 文章类型： Article，,卷期：2011年2-3] The structure activity relationships for a series of pyrazine-based A(2B) adenosine receptor antagonists are described. From this work, LAS101057 (17), a potent, selective, and orally efficacious A(2B) receptor antagonis...