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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26条记录   Carnitine Palmitoyltransferase (CPT) Modulators: A Medicinal Chemistry Perspective on 35 Years of Research [作者：CECCARELLI SIMONA M; CHOMIENNE ODILE; GUBLER MARCEL; ARDUINI ARDUINO,期刊：Journal of Medicinal Chemistry, 页码：3109-3152 , 文章类型： Editorial Material，,卷期：2011年54-9] Synthesis and Biological Evaluation of 4-Arylcoumarin Analogues of Combretastatins. Part 2 [作者：COMBES SEBASTIEN; BARBIER PASCALE; DOUILLARD SOAZIG; MCLEERFLORIN ANNE; BOURGARELREY VERONIQUE; PIERSON JEANTHOMAS; FEDOROV ALEXEY YU; FINET JEANPIERRE; BOUTONNAT JEAN; PEYROT VINCENT,期刊：Journal of Medicinal Chemistry, 页码：3153-3162 , 文章类型： Article，,卷期：2011年54-9] A series of A-ring variously methoxylated 4-(3-hydroxy-4-methoxyphenyl)coumarins related to combretastatin A-4 was prepared by cross-coupling reactions. Cytotoxicity studies indicated a potent activity against HBL100 cel... Pharmacophore Modeling and Virtual Screening for Novel Acidic Inhibitors of Microsomal Prostaglandin E-2 Synthase-1 (mPGES-1) [作者：WALTENBERGER BIRGIT; WIECHMANN KATJA; BAUER JULIA; MARKT PATRICK; NOHA STEFAN M; WOLBER GERHARD; ROLLINGER JUDITH M; WERZ OLIVER; SCHUSTER DANIELA; STUPPNER HERMANN,期刊：Journal of Medicinal Chemistry, 页码：3163-3174 , 文章类型： Article，,卷期：2011年54-9] Microsomal prostaglandin E-2 synthase-1 (mPGES-1) catalyzes prostaglandin E-2 formation and is considered as a potential anti-inflammatory pharmacological target. To identify novel chemical scaffolds active on this enzym... Synthesis of Tetrahydronaphthalene Lignan Esters by Intramolecular Cyclization of Ethyl p-Azidophenyl-2-phenylalkanoates and Evaluation of the Growth Inhibition of Human Tumor Cell Lines [作者：PINTO ORLANDO; SARDINHA JOAO; VAZ PEDRO D; PIEDADE FATIMA; CALHORDA MARIA J; ABRAMOVITCH RUDOLPH; NAZARETH NAIR; PINTO MADALENA; NASCIMENTO MARIA S J; RAUTER AMELIA P,期刊：Journal of Medicinal Chemistry, 页码：3175-3187 , 文章类型： Article，,卷期：2011年54-9] Intramolecular cyclization via nitrenium ion of 2-phenylpentanoic/2-phenylbutanoic acid esters with a terminal p-azidophenyl group gives direct access to tetrahydronaphthalene lignan esters. The p-azidophenyl-substituted... Impact of the Nature of the Substituent at the 3-Position of 4H-1,2,4-Benzothiadiazine 1,1-Dioxides on Their Opening Activity toward ATP-Sensitive Potassium Channels [作者：PIROTTE BERNARD; DE TULLIO PASCAL; BOVERIE STEPHANE; MICHAUX CATHERINE; LEBRUN PHILIPPE,期刊：Journal of Medicinal Chemistry, 页码：3188-3199 , 文章类型： Article，,卷期：2011年54-9] The synthesis of diversely substituted 3-isopropoxy-, 3-isopropylsulfanyl-, 3-isopropylsulfinyl-, and 3-isobutyl-4H-1,2,4-benzothiadiazine 1,1-dioxides is described. Their activity on pancreatic beta-cells (inhibitory ef... Synthesis and Biological Evaluation of 2,4,5-Substituted Pyrimidines as a New Class of Tubulin Polymerization Inhibitors [作者：XIE FUCHUN; ZHAO HONGBING; LI DEWEN; CHEN HONG; QUAN HAITIAN; SHI XIAOJING; LOU LIGUANG; HU YOUHONG,期刊：Journal of Medicinal Chemistry, 页码：3200-3205 , 文章类型： Article，,卷期：2011年54-9] Members of a series of 2,4,5-substituted pyrimidine derivatives were synthesized, and their interactions with tubulin and their antiproliferative activities against the human hepatocellular carcinoma cells of liver (BEL-... Discovery of 1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A Novel Multimodal Compound for the Treatment of Major Depressive Disorder [作者：BANGANDERSEN BENNY; RUHLAND THOMAS; JORGENSEN MORTEN; SMITH GARRICK; FREDERIKSEN KRISTEN; JENSEN KLAUS GJERVIG; ZHONG HUAILING; NIELSEN SOREN MOLLER; HOGG SANDRA; MORK ARNE; STENSBOL TINE BRYAN,期刊：Journal of Medicinal Chemistry, 页码：3206-3221 , 文章类型： Article，,卷期：2011年54-9] The synthesis and structure-activity relationship of a novel series of compounds with combined effects on 5-HT3A and 5-HT1A receptors and on the serotonin (5-HT) transporter (SERT) are described. Compound 5m (Lu AA21004)... Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds [作者：BEGHYN TERENCE B; CHARTON JULIE; LEROUX FLORENCE; LACONDE GUILLAUME; BOURIN ARNAUD; COS PAUL; MAES LOUIS; DEPREZ BENOIT,期刊：Journal of Medicinal Chemistry, 页码：3222-3240 , 文章类型： Article，,卷期：2011年54-9] The dominant strategy for discovery of new antimalarial drugs relies on cell-free assays on specific biochemical pathways of Plasmodium falciparum . However, it appears that screening directly on the parasite is a more r... Discovery of 2-Arylbenzoxazoles as Upregulators of Utrophin Production for the Treatment of Duchenne Muscular Dystrophy [作者：CHANCELLOR DANIEL R; DAVIES KAY E; DE MOOR OLIVIER; DORGAN COLIN R; JOHNSON PETER D; LAMBERT ADAM G; LAWRENCE DANIEL; LECCI CRISTINA; MAILLOL CAROLE; MIDDLETON PENNY J; NUGENT GARY; POIGNANT SEVERINE D; POTTER ALLYSON C; PRICE PAUL D; PYE RICHARD J; STORER RICHARD; TINSLEY JONATHON M; VAN WELL RENATE; VICKERS RICHARD; VILE JULIA; WILKES FRASER J; WILSON FRANCIS X; WREN STEPHEN P; WYNNE GRAHAM M,期刊：Journal of Medicinal Chemistry, 页码：3241-3250 , 文章类型： Article，,卷期：2011年54-9] A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold conside... Novel Nitric Oxide-Releasing Derivatives of Farnesylthiosalicylic Acid: Synthesis and Evaluation of Antihepatocellular Carcinoma Activity [作者：LING YONG; YE XIAOLEI; ZHANG ZHENZHEN; ZHANG YIHUA; LAI YISHENG; JI HUI; PENG SIXUN; TIAN JIDE,期刊：Journal of Medicinal Chemistry, 页码：3251-3259 , 文章类型： Article，,卷期：2011年54-9] Novel furoxan-based nitric oxide (NO) releasing derivatives (8a-p) of farnesylthiosalicylic acid (FTS) were synthesized. Compound 8l displayed the strongest inhibition on the proliferation of human hepatocellular carcino... Identification of Inhibitors that Block Vaccinia Virus Infection by Targeting the DNA Synthesis Processivity Factor D4 [作者：NUTH MANUNYA; HUANG LIJUAN; SAW YIH LING; SCHORMANN NORBERT; CHATTOPADHYAY DEBASISH; RICCIARDI ROBERT P,期刊：Journal of Medicinal Chemistry, 页码：3260-3267 , 文章类型： Article，,卷期：2011年54-9] Smallpox was globally eradicated 30 years ago by vaccination. The recent threat of bioterrorism demands the development of improved vaccines and novel therapeutics to effectively preclude a reemergence of smallpox. One n... Exploration of the Activity of 7-Pyrrolidino-8-methoxyisothiazoloquinolones against Methicillin-Resistant Staphylococcus aureus (MRSA) [作者：KIM HA YOUNG; WILES JASON A; WANG QIUPING; PAIS GODWIN C G; LUCIEN EDLAINE; HASHIMOTO AKIHIRO; NELSON DAVID M; THANASSI JANE A; PODOS STEVEN D; DESHPANDE MILIND; PUCCI MICHAEL J; BRADBURY BARTON J,期刊：Journal of Medicinal Chemistry, 页码：3268-3282 , 文章类型： Article，,卷期：2011年54-9] A series of 7-(3'-substituted)pyrrolidino-8-methoxyisothiazoloquinolone (ITQ) analogues were prepared, and their antibacterial potency against methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Sta... Chiral Sulfoxides as Metabolites of 2-Thioimidazole-Based p38 alpha Mitogen-Activated Protein Kinase Inhibitors: Enantioselective Synthesis and Biological Evaluation [作者：BUEHLER STEFANIE; GOETTERT MARCIA; SCHOLLMEYER DIETER; ALBRECHT WOLFGANG; LAUFER STEFAN A,期刊：Journal of Medicinal Chemistry, 页码：3283-3297 , 文章类型： Article，,卷期：2011年54-9] A number of pharmaceutically important drugs contain asymmetric sulfinyl moieties, so the biological evaluation of chiral sulfoxides as human drug metabolites is important for the development of safe and effective pharma... Synthesis and Biological Activity of 22-Deoxo-23-oxa Analogues of Saponin OSW-1 [作者：MAJ JADWIGA; MORZYCKI JACEK W; RAROVA LUCIE; OKLESTKOVA JANA; STRNAD MIROSLAV; WOJTKIELEWICZ AGNIESZKA,期刊：Journal of Medicinal Chemistry, 页码：3298-3305 , 文章类型： Article，,卷期：2011年54-9] Analogues of the potent cytotoxic saponin OSW-1 were prepared from the readily available steroidal 16 beta,17 alpha,22-triol. The new 22-deoxo-23-oxa analogues of OSW-1 were screened against eight cancer cell lines and n... Potent Bivalent Smac Mimetics: Effect of the Linker on Binding to Inhibitor of Apoptosis Proteins (IAPs) and Anticancer Activity [作者：SUN HAIYING; LIU LIU; LU JIANFENG; BAI LONGCHUAN; LI XIAOQIN; NIKOLOVSKACOLESKA ZANETA; MCEACHERN DONNA; YANG CHAOYIE; QIU SU; YI HAN; SUN DUXIN; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：3306-3318 , 文章类型： Article，,卷期：2011年54-9] We have synthesized and evaluated a series of nonpeptidic, bivalent Smac mimetics as antagonists of the inhibitor of apoptosis proteins and new anticancer agents. All these bivalent Smac mimetics bind to full-length XIAP... Amidine-Oximes: Reactivators for Organophosphate Exposure [作者：KALISIAK JAROSLAW; RALPH ERIK C; ZHANG JUN; CASHMAN JOHN R,期刊：Journal of Medicinal Chemistry, 页码：3319-3330 , 文章类型： Article，,卷期：2011年54-9] A new class of amidine-oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) were designed, synthesized, and tested. These compounds represent a novel group of oximes with enhanced capabilities of cr...