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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16条记录   Thermodynamic and Structural Effects of Macrocyclic Constraints in Protein-Ligand Interactions [作者：DELORBE JOHN E; CLEMENTS JOHN H; WHIDDON BENJAMIN B; MARTIN STEPHEN F,期刊：ACS Medicinal Chemistry Letters, 页码：448-452 , 文章类型： Article，,卷期：2010年1-8] The thermodynamic and structural effects of macrocyclization as a tactic for stabilizing the biologically active conformation of Grb2 SH2 binding peptides were investigated using isothermal titration calorimetry and X-ra... Novel Benzofurans with Tc-99m Complexes as Probes for Imaging Cerebral beta-Amyloid Plaques [作者：ONO MASAHIRO; FUCHI YASUFUMI; FUCHIGAMI TAKESHI; KOBASHI NOBUYA; KIMURA HIROYUKI; HARATAKE MAMORU; SAJI HIDEO; NAKAYAMA MORIO,期刊：ACS Medicinal Chemistry Letters, 页码：443-447 , 文章类型： Article，,卷期：2010年1-8] Two novel benzofuran derivatives coupled with Tc-99m complexes were tested as probes for imaging cerebral beta-amyloid plaques using single photon emission tomography. Although both derivatives bound to A beta(1-42) aggr... Ranking Ligand Affinity for the DNA Minor Groove by Experiment and Simulation [作者：WITTAYANARAKUL KITIYAPORN; ANTHONY NAHOUM G; TREESUWAN WITCHA; HANNONGBUA SUPA; ALNISS HASAN; KHALAF ABEDAWN I; SUCKLING COLIN J; PARKINSON JOHN A; MACKAY SIMON P,期刊：ACS Medicinal Chemistry Letters, 页码：376-380 , 文章类型： Article，,卷期：2010年1-8] The structural and thermodynamic basis for the strength and selectivity of the interactions of minor groove binders (MGBs) with DNA is not fully understood. In 2003, we reported the first example of a thiazole-containing... Identification of a New Series of STAT3 Inhibitors by Virtual Screening [作者：MATSUNO KENJI; MASUDA YOSHIAKI; UEHARA YUTAKA; SATO HIROSHI; MUROYA AYUMU; TAKAHASHI OSAMU; YOKOTAGAWA TAKANE; FURUYA TOSHIO; OKAWARA TADASHI; OTSUKA MASAMI; OGO NAOHISA; ASHIZAWA TADASHI; OSHITA CHIE; TAI SACHIKO; ISHII HIDEE; AKIYAMA YASUTO; ASAI AKIRA,期刊：ACS Medicinal Chemistry Letters, 页码：371-375 , 文章类型： Article，,卷期：2010年1-8] The signal transducer and activator of transcription 3 (STAT3) is considered to be an attractive therapeutic target for oncology drug development. We identified a N-[2-(1,3,4-oxadiazolyl)]-4-quinolinecarboxamide derivati... Cytotoxic Profile and Peculiar Reactivity with Biomolecules of a Novel "Rule-Breaker" Iodidoplatinum(II) Complex [作者：MESSORI LUIGI; CASINI ANGELA; GABBIANI CHIARA; MICHELUCCI ELENA; CUBO LETICIA; RIOSLUCI CARLA; PADRON JOSE M; NAVARRORANNINGER CARMEN; QUIROGA ADORACION G,期刊：ACS Medicinal Chemistry Letters, 页码：381-385 , 文章类型： Article，,卷期：2010年1-8] Novel and surprising biological properties were disclosed for the platinum(II) complex cis-diiodidodiisopropylamineplatinum(II). Remarkably this new platinum(II) complex manifests pronounced antiproliferative properties ... Antiproliferative and Differentiating Activities of a Novel Series of Histone Deacetylase Inhibitors [作者：BINASCHI MONICA; BOLDETTI ANDREA; GIANNI MAURIZIO; MAGGI CARLO ALBERTO; GENSINI MARTINA; BIGIONI MARIO; PARLANI MASSIMO; GIOLITTI ALESSANDRO; FRATELLI MADDALENA; VALLI CLAUDIA; TERAO MINEKO; GARATTINI ENRICO,期刊：ACS Medicinal Chemistry Letters, 页码：411-415 , 文章类型： Article，,卷期：2010年1-8] Histone deacetylases are promising molecular targets for the development of antitumor agents. A novel series of histone deacetylase inhibitors of the hydroxamic acid type were synthesized for structure-activity studies. ... From Taxuspine X to Structurally Simplified Taxanes with Remarkable P-Glycoprotein Inhibitory Activity [作者：CASTAGNOLO DANIELE; CONTEMORI LORENZO; MACCARI GIORGIO; AVRAMOVA STANISLAVA I; NERI ANNALISA; SGARAGLI GIANPIETRO; BOTTA MAURIZIO,期刊：ACS Medicinal Chemistry Letters, 页码：416-421 , 文章类型： Article，,卷期：2010年1-8] Three simplified non-natural natural taxanes, related to taxuspine x, were synthetized and assayed as p-glycoprotein (P-gp) inhibitors. One of them (6) proved to be a very efficient P-gp inhibitor with an IC50 = 7.2 x 10... Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor [作者：GARBACCIO ROBERT M; BRNARDIC EDWARD J; FRALEY MARK E; HARTMAN GEORGE D; HUTSON PETE H; OBRIEN JULIE A; MAGLIARO BRIAN C; USLANER JASON M; HUSZAR SARAH L; FILLGROVE KERRY L; SMALL JAMES H; TANG CUYUE; KUO YUHSIN; JACOBSON MARLENE A,期刊：ACS Medicinal Chemistry Letters, 页码：406-410 , 文章类型： Article，,卷期：2010年1-8] Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physicial and pharmacokinetic... Exploring alpha 7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB [作者：GARCIADELGADO NOEMI; BERTRAND SONIA; NGUYEN KONG T; VAN DEURSEN RUUD; BERTRAND DANIEL; REYMOND JEANLOUIS,期刊：ACS Medicinal Chemistry Letters, 页码：422-426 , 文章类型： Article，,卷期：2010年1-8] Virtual analogues (1167860 compounds) of the nicotinic alpha 7-receptor (alpha 7 nAChR) ligands PNU-282,987 and SSR180711 were generated from the chemical universe database GDB-11 by extracting all aliphatic diamine anal... Computational Modeling of Kinase Inhibitor Selectivity [作者：SUBRAMANIAN GOVINDAN; SUD MANISH,期刊：ACS Medicinal Chemistry Letters, 页码：395-399 , 文章类型： Article，,卷期：2010年1-8] An exhaustive computational exercise on a comprehensive set of 15 therapeutic kinase inhibitors was undertaken to indentify as to which compounds hit which kinase off-targets in the human kinome. Although the kinase sele... The Nitric Oxide Prodrug V-PROLI/NO Inhibits Cellular Uptake of Proline [作者：HONG SAM Y; BORCHERT GREGORY L; MACIAG ANNA E; NANDURDIKAR RAHUL S; SAAVEDRA JOSEPH E; KEEFER LARRY K; PHANG JAMES M; CHAKRAPANI HARINATH,期刊：ACS Medicinal Chemistry Letters, 页码：386-389 , 文章类型： Article，,卷期：2010年1-8] V-PYRRO/NO is a well-studied nitric oxide (NO) prodrug that has been shown to protect human liver cells from arsenic, acetaminophen, and other toxic assaults in vivo. Its proline based analogue, V-PROLI/NO, was designed ... Structure-Activity Studies on Antiproliferative Factor (APF) Glycooctapeptide Derivatives [作者：KACZMAREK PIOTR; TOCCI GILLIAN M; KEAY SUSAN K; ADAMS KRISTIE M; ZHANG CHENOU; KOCH KRISTOPHER R; GRKOVIC DAVID; GUO LI; MICHEJDA CHRISTOPHER J; BARCHI JOSEPH J JR,期刊：ACS Medicinal Chemistry Letters, 页码：390-394 , 文章类型： Article，,卷期：2010年1-8] Antiproliferative factor (APF) alsialylated glycopeptide secreted by explanted bladder epithelial cells from interstitial cystitis/painful bladder syndrome (IC/PBS) patients and its unsialylated analogue (as-APF) signifi... Concise Syntheses of the Abyssinones and Discovery of New Inhibitors of Prostate Cancer and MMP-2 Expression [作者：FARMER REBECCA L; BIDDLE MARGARET M; NIBBS ANTOINETTE E; HUANG XIAOKE; BERGAN RAYMOND C; SCHEIDT KARL A,期刊：ACS Medicinal Chemistry Letters, 页码：400-405 , 文章类型： Article，,卷期：2010年1-8] The first asymmetric syntheses of four members of the abyssinone class of natural products (I, II, III, and IV 4'-OMe) via quinine- or quinidine-derived thiourea-catalyzed intramolecular conjugate additions of beta-keto ... Discovery of N-Aryl Piperazines as Selective mGluR(5) Potentiators with Improved In Vivo Utility [作者：ZHOU YA; MANKA JASON T; RODRIGUEZ ALICE L; WEAVER C DAVID; DAYS EMILY L; VINSON PAIGE N; JADHAV SATYAWAN; HERMANN ELIZABETH J; JONES CARRIE K; CONN P JEFFREY; LINDSLEY CRAIG W; STAUFFER SHAUN R,期刊：ACS Medicinal Chemistry Letters, 页码：433-438 , 文章类型： Article，,卷期：2010年1-8] This letter describes the discovery, structure-activity relationship, and in vitro and in vivo pharmacological profile of a novel non-MPEP-derived mGluR(5) positive allosteric modulator (PAM) based upon an N-aryl piperaz... Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery [作者：MEDINA JESUS R; BLACKLEDGE CHARLES W; HEERDING PIRK A; CAMPOBASSO NINO; WARD PARIS; BRIAND JACQUES; WRIGHT LOIS; AXTEN JEFFREY M,期刊：ACS Medicinal Chemistry Letters, 页码：439-442 , 文章类型： Article，,卷期：2010年1-8] Fragment screening of phosphoinositide-dependent kinase-1 (PDK1) in a biochemical kinase assay afforded hits that were characterized and prioritized based on ligand efficiency and binding interactions with PDK1 as determ... DNA Sequence Preference and Adduct Orientation of Pyrrolo[2,1-c][1,4]benzodiazepine Antitumor Agents [作者：RAHMAN KHONDAKER M; VASSOLER HIGIA; JAMES COLIN H; THURSTON DAVID E,期刊：ACS Medicinal Chemistry Letters, 页码：427-432 , 文章类型： Article，,卷期：2010年1-8] The pyrrolobenzodiazepines (PBDs) are covalent DNA minor-groove binding agents with a reported preference for binding to 5'-PU-G-Pu sequences with their A rights oriented toward the 3'-end of the covalently modified DNA ...