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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   Discovery of Potent Dual PPAR alpha Agonists/CB1 Ligands [作者：PEREZFERNANDEZ RUTH; FRESNO NIEVES; MACIASGONZALEZ MANUEL; ELGUERO JOSE; DECARA JUAN; GIRON ROCIO; RODRIGUEZALVAREZ ANA; ISABEL MARTIN MARIA; RODRIGUEZ DE FONSECA FERNANDO; GOYA PILAR,期刊：ACS Medicinal Chemistry Letters, 页码：793-797 , 文章类型： Article，,卷期：2011年2-11] This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisorne proliferator-activated receptors (PPAR). These compounds were obtained from fusing the pha... Host-Directed Inhibitors of Myxoviruses: Synthesis and in Vitro Biochemical Evaluation [作者：SUN AIMING; NDUNGU J MAINA; KRUMM STEFANIE A; YOON JEONGJOONG; THEPCHATRI PAHK; NATCHUS MICHAEL; PLEMPER RICHARD K; SNYDER JAMES P,期刊：ACS Medicinal Chemistry Letters, 页码：798-803 , 文章类型： Article，,卷期：2011年2-11] Drugs targeted to viral proteins are highly vulnerable to the development of viral resistance. One little explored approach to the treatment of viral diseases is the development of agents that target host factors require... Mannitol Bis-phosphate Based Inhibitors of Fructose 1,6-Bisphosphate Aldolases [作者：MABIALABASSILOUA CHARLESGABIN; ARTHUSCARTIER GUILLAUME; HANNAERT VERONIQUE; THERISOD HELENE; SYGUSCH JURGEN; THERISOD MICHEL,期刊：ACS Medicinal Chemistry Letters, 页码：804-808 , 文章类型： Article，,卷期：2011年2-11] Several 5-O-alkyl- and 5-C-alkyl-mannitol bis-phosphates were synthesized and comparatively assayed as inhibitors of fructose bis-phosphate aldolases (Fbas) from rabbit muscle (taken as surrogate model of the human enzym... Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity [作者：LIU KEVIN KC; ZHU JINJIANG; SMITH GRAHAM L; YIN MINJEAN; BAILEY SIMON; CHEN JEFFREY H; HU QIYUE; HUANG QINHUA; LI CHUNZE; LI QING J; MARX MATTHEW A; PADERES GENEVIEVE; RICHARDSON PAUL F; SACH NEAL W; WALLS MARLENA; WELLS PETER A; ZOU AIHUA,期刊：ACS Medicinal Chemistry Letters, 页码：809-813 , 文章类型： Article，,卷期：2011年2-11] Highly selective PI3K inhibitors with subnanomolar PI3K alpha potency and greater than 7000-fold selectivity against mTOR kinase were discovered through structure-based drug design (SBDD). These tetra-substituted thiophe... A Manganese-Porphyrin Complex Decomposes H(2)O(2), Inhibits Apoptosis, and Acts as a Radiation Mitigator in Vivo [作者：STOYANOVSKY DETCHO A; HUANG ZHENTAI; JIANG JIANFEI; BELIKOVA NATALIA A; TYURIN VLADIMIR; EPPERLY MICHAEL W; GREENBERGER JOEL S; BAYIR HUELYA; KAGAN VALERIAN E,期刊：ACS Medicinal Chemistry Letters, 页码：814-817 , 文章类型： Article，,卷期：2011年2-11] Ionizing radiation triggers mitochondria] overproduction of H(2)O(2) with concomitant induction of intrinsic apoptosis, whereby clearance of H(2)O(2) upon overexpression of mitochondrial catalase increases radioresistanc... CoA Adducts of 4-Oxo-4-phenylbut-2-enoates: Inhibitors of MenB from the M. tuberculosis Menaquinone Biosynthesis Pathway [作者：LI XIAOKAI; LIU NINA; ZHANG HUANING; KNUDSON SUSAN E; LI HUEIJIUN; LAI CHENGTSUNG; SIMMERLING CARLOS; SLAYDEN RICHARD A; TONGE PETER J,期刊：ACS Medicinal Chemistry Letters, 页码：818-823 , 文章类型： Article，,卷期：2011年2-11] A high-throughput screen led to the discovery of 2-amino-4-oxo-4-phenylbutanoate inhibitors of the 1,4-dihydroxy-2-naphthoyl-CoA synthase (MenB) from the menaquinone biosynthesis pathway in Mycobacterium tuberculosis. Ho... Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes [作者：LI AIWEN; YUAN CHESTER C; CHOW DAVID; CHEN MICHELLE; EMERY MAURICE G; HALE CLARENCE; ZHANG XIPING; SUBRAMANIAN RAJU; ST JEAN DAVID J JR; KOMOROWSKI RENEE; VENIANT MURIELLE; WANG MINGHAN; FOTSCH CHRISTOPHER,期刊：ACS Medicinal Chemistry Letters, 页码：824-827 , 文章类型： Article，,卷期：2011年2-11] All eight of the major active metabolites of (S)-2-(1S,2S,4R)-bicyclo [2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221, compound 1), an inhibitor of 11 beta-hydroxysteroid dehydrogenase type 1 that... Type 1 Phototherapeutic Agents, Part I: Preparation and Cancer Cell Viability Studies of Novel Photolabile Sulfenamides [作者：KARWA AMOLKUMAR S; POREDDY AMRUTA R; ASMELASH BETHEL; LIN TIENSUNG; DORSHOW RICHARD B; RAJAGOPALAN RAGHAVAN,期刊：ACS Medicinal Chemistry Letters, 页码：828-833 , 文章类型： Article，,卷期：2011年2-11] Novel type 1 phototherapeutic agents based on compounds containing S-N bonds (sulfenamides) were synthesized, assessed for free radical generation, and evaluated in vitro for cell death efficacy in four cancer cell lines... Homology Model and Docking-Based Virtual Screening for Ligands of the sigma(1) Receptor [作者：LAURINI ERIK; DAL COL VALENTINA; MAMOLO MARIA GRAZIA; ZAMPIERI DANIELE; POSOCCO PAOLA; FERMEGLIA MAURIZIO; VIO LUCIANO; PRICL SABRINA,期刊：ACS Medicinal Chemistry Letters, 页码：834-839 , 文章类型： Article，,卷期：2011年2-11] This study presents for the first time the 3D model of the sigma(1) receptor protein as obtained from homology modeling techniques, shows the applicability of this structure to docking-based virtual screening, defines a ... Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS) [作者：RUEDA LOURDES; CASTELLOTE ISABEL; CASTROPICHEL JULIA; CHAPARRO MARIA J; CARLOS DE LA ROSA JUAN; GARCIAPEREZ ADOLFO; GORDO MARIOLA; BELEN JIMENEZDIAZ MARIA; KESSLER ALBANE; MACDONALD SIMON J F; SANTOS MARTINEZ MARIA; SANZ LAURA M; JAVIER GAMO FRANCISCO; FERNANDEZ ESTHER,期刊：ACS Medicinal Chemistry Letters, 页码：840-844 , 文章类型： Article，,卷期：2011年2-11] Rapid triaging of three series of related hits selected from the Tres Cantos Anti-Malarial Set (TCAMS) are described. A triazolopyrimidine series was deprioritized due to delayed inhibition of parasite growth. A lactic a... Synthesis of C-Pseudonucleosides Bearing Thiazolidin-4-one as a Novel Potential Immunostimulating Agent [作者：CHEN HUA; YIN QINGMEI; LI CHUNXIAO; WANG ENKAI; GAO FANG; ZHANG XIAOBO; YIN ZHI; WEI SINAN; LI XIAOLIU; MENG MING; ZHANG PINGZHU; LI NA; ZHANG JINCHAO,期刊：ACS Medicinal Chemistry Letters, 页码：845-848 , 文章类型： Article，,卷期：2011年2-11] Several novel C-pseudonucleosides bearing thiazolidin-4-one were synthesized by one-pot three-component condensation using unprotected sugar aldehyde at room temperature, and their effects on T cells, B cells, the cytoki... Nitazoxanide Disrupts Membrane Potential and Intrabacterial pH Homeostasis of Mycobacterium tuberculosis [作者：DE CARYALHO LUIZ PEDRO S; DARBY CRYSTAL M; RHEE KYU Y; NATHAN CARL,期刊：ACS Medicinal Chemistry Letters, 页码：849-854 , 文章类型： Article，,卷期：2011年2-11] Nitazoxanide (Alinia), a nitro-thiazolyl antiparasitic drug, kills diverse microorganisms by unknown mechanisms. Here we identified two actions of nitazoxanide against Mycobacterium tuberculosis (Mtb): disruption of Mtb'... Discovery of Novel alpha 4 beta 2 Neuronal Nicotinic Receptor Modulators through Structure-Based Virtual Screening [作者：MAHASENAN KIRAN V; PAVLOVICZ RYAN E; HENDERSON BRANDON J; GONZALEZCESTARI TATIANA F; YI BITNA; MCKAY DENNIS B; LI CHENGLONG,期刊：ACS Medicinal Chemistry Letters, 页码：855-860 , 文章类型： Article，,卷期：2011年2-11] We performed a hierarchical structure-based virtual screening utilizing a comparative model of the human alpha 4 beta 2 neuronal nicotinic acetylcholine receptor (nAChR) extracellular domain. Compounds were selected for ... Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity [作者：CHEN QIYIN; LIU YANXIA; LUESCH HENDRIK,期刊：ACS Medicinal Chemistry Letters, 页码：861-865 , 文章类型： Article，,卷期：2011年2-11] Apratoxins are cytotoxic marine natural products that prevent cotranslational translocation early in the secretory pathway. We showed that apratoxins downregulate receptors and growth factor ligands, giving a one-two pun... Identification of a Potent and Selective Cannabinoid CB, Receptor Antagonist from Auxarthron reticulatum [作者：ELSEBAI MAHMOUD FAHMI; REMPEL VIKTOR; SCHNAKENBURG GREGOR; KEHRAUS STEFAN; MUELLER CHRISTA E; KOENIG GABRIELE M,期刊：ACS Medicinal Chemistry Letters, 页码：866-869 , 文章类型： Article，,卷期：2011年2-11] The fungus Auxarthron reticulatum derived from the marine sponge Ircinia variabilis produced the diketopiperazine alkaloid amauromine (1) and the quinolinone methyl-penicinoline (2). Compound 2 is identical to the report... Inhibition of DNA Synthesis by a Platinum-Acridine Hybrid Agent Leads to Potent Cell Kill in Nonsmall Cell Lung Cancer [作者：SMYRE CHRISTOPHER L; SALUTA GILDA; KUTE TIMOTHY E; KUCERA GREGORY L; BIERBACH ULRICH,期刊：ACS Medicinal Chemistry Letters, 页码：870-874 , 文章类型： Article，,卷期：2011年2-11] The platinum acridine anticancer agent [PtCl(en)(LH)] (NO(3))2 (1) [en = ethane-1,2-diamine, LH = N-(2-(acridin-9-ylamino)ethyl)-N-methylpropionimidamide, acridinium cation] and the clinical drug cisplatin were studied i...