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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44条记录   Engineering pH-Gated Transitions for Selective and Efficient Double-Strand DNA Photocleavage in Hypoxic Tumors [作者：YANG WANGYONG; ROY SAUMYA; PHRATHEP BOONDANIWON; RENGERT ZACH; KENWORTHY RACHAEL; ZORIO DIEGO A R; ALABUGIN IGOR V,期刊：Journal of Medicinal Chemistry, 页码：8501-8516 , 文章类型： Article，,卷期：2011年54-24] We describe a family of hybrid compounds for the most efficient light-activated double-strand (ds) DNA cleavage known to date. This family represents the second generation of "switchable" molecular systems for pH-gated d... 5-Amino-2-aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors. Part 2. The Impact of Bridging Groups at Position C-2 [作者：LEE HSUEHYUN; CHANG JANGYANG; NIEN CHIHYING; KUO CHINGCHUAN; SHIH KUANGHSING; WU CHUNHSEIN; CHANG CHIYEN; LAI WENYANG; LIOU JINGPING,期刊：Journal of Medicinal Chemistry, 页码：8517-8525 , 文章类型： Article，,卷期：2011年54-24] A variety of studies on the modification of combretastatin A-4 triggered our interest in the impact of the linkers between the 3,4,5-trimethoxyphenyl ring and 5-amino-6-methoxyquinoline on biological activity. The replac... A New Class of Antimalarial Dioxanes Obtained through a Simple Two-Step Synthetic Approach: Rational Design and Structure-Activity Relationship Studies [作者：PERSICO MARCO; QUINTAVALLA ARIANNA; RONDINELLI FRANCESCA; TROMBINI CLAUDIO; LOMBARDO MARCO; FATTORUSSO CATERINA; AZZARITO VALERIA; TARAMELLI DONATELLA; PARAPINI SILVIA; CORBETT YOLANDA; CHIANESE GIUSEPPINA; FATTORUSSO ERNESTO; TAGLIALATELASCAFATI ORAZIO,期刊：Journal of Medicinal Chemistry, 页码：8526-8540 , 文章类型： Article，,卷期：2011年54-24] A new series of simple endoperoxides, characterized by a 3-methoxy-1,2-dioxane scaffold, was designed on the basis of a previously developed pharmacophore. Through a simplified and versatile scheme of synthesis, which ut... Benzimidazolones: A New Class of Selective Peroxisome Proliferator-Activated Receptor gamma (PPAR gamma) Modulators [作者：LIU WEIGUO; LAU FIONA; LIU KUN; WOOD HAROLD B; ZHOU GAOCHAO; CHEN YULI; LI YING; AKIYAMA TARO E; CASTRIOTA GINO; EINSTEIN MONICA; WANG CHUALIN; MCCANN MARGARET E; DOEBBER THOMAS W; WU MARGARET; CHANG CHING H; MCNAMARA LESLEY; MCKEEVER BRIAN; MOSLEY RALPH T; BERGER JOEL P; MEINKE PETER T,期刊：Journal of Medicinal Chemistry, 页码：8541-8554 , 文章类型： Article，,卷期：2011年54-24] A series of benzimidazolone carboxylic acids and oxazolidinediones were designed and synthesized in search of selective PPAR gamma modulators (SPPAR gamma Ms) as potential therapeutic agents for the treatment of type II ... Binding of Ibuprofen, Ketorolac, and Diclofenac to COX-1 and COX-2 Studied by Saturation Transfer Difference NMR [作者：VIEGAS ALDINO; MANSO JOAO; CORVO MARTA C; MARQUES M MANUEL B; CABRITA EURICO J,期刊：Journal of Medicinal Chemistry, 页码：8555-8562 , 文章类型： Article，,卷期：2011年54-24] Saturation transfer difference NMR (STD-NMER) spectroscopy has emerged as a powerful screening tool and a straightforward way to study the binding epitopes of active compounds in early stage lead discovery in pharmaceuti... Targeting the Binding Function 3 (BF3) Site of the Human Androgen Receptor through Virtual Screening [作者：LACK NATHAN A; AXERIOCILIES PETER; TAVASSOLI PEYMAN; HAN FRANK Q; CHAN KA HONG; FEAU CLEMENTINE; LEBLANC ERIC; GUNS EMMA TOMLINSON; GUY R KIPLIN; RENNIE PAUL S; CHERKASOV ARTEM,期刊：Journal of Medicinal Chemistry, 页码：8563-8573 , 文章类型： Article，,卷期：2011年54-24] The androgen receptor (AR) is the best studied drug target for the treatment of prostate cancer. While there are a number of drugs that target the AR, they all work through the same mechanism of action and are prone to t... Inhibition of Glutathione S-Transferase M1 by New Gabosine Analogues Is Essential for Overcoming Cisplatin Resistance in Lung Cancer Cells [作者：WANG CHIEHONG; WU HO T; CHENG HAU M; YEN TIENJUI; LU IHSUAN; CHANG HUI CHUAN; JAO SHUCHUAN; SHING TONY K M; LI WENSHAN,期刊：Journal of Medicinal Chemistry, 页码：8574-8581 , 文章类型： Article，,卷期：2011年54-24] A new class of human GST inhibitors has been identified via rational design approach; we report their discovery, synthesis, inhibitory activity, and synergetic effect in combination with cisplatin against A549 lung cance... Computationally-Guided Optimization of a Docking Hit to Yield Catechol Diethers as Potent Anti-HIV Agents [作者：BOLLINI MARIELA; DOMAOAL ROBERT A; THAKUR VINAY V; GALLARDOMACIAS RICARDO; SPASOV KRASIMIR A; ANDERSON KAREN S; JORGENSEN WILLIAM L,期刊：Journal of Medicinal Chemistry, 页码：8582-8591 , 文章类型： Article，,卷期：2011年54-24] A 5-mu M docking hit has been optimized to an extraordinarily potent (55 pM) non-nucleoside inhibitor of HIV reverse transcriptase. Use of free energy perturbation (PEP) calculations to predict relative free energies of ... Novel 3,4-Isoxazolediamides as Potent Inhibitors of Chaperone Heat Shock Protein 90 [作者：BARUCHELLO RICCARDO; SIMONI DANIELE; GRISOLIA GIUSEPPINA; BARBATO GIUSEPPINA; MARCHETTI PAOLO; RONDANIN RICCARDO; MANGIOLA STEFANIA; GIANNINI GIUSEPPE; BRUNETTI TIZIANA; ALLOATTI DOMENICO; GALLO GRAZIA; CIACCI ANDREA; VESCI LOREDANA; CASTORINA MASSIMO; MILAZZO FERDINANDO M; CERVONI MARIA L; GUGLIELMI MARIO B; BARBARINO MARCELLA; FODERA ROSANNA; PISANO CLAUDIO; CABRI WALTER,期刊：Journal of Medicinal Chemistry, 页码：8592-8604 , 文章类型： Article，,卷期：2011年54-24] A structural investigation on the isoxazole scaffold led to the discovery of 3,4-isoxazolediamide compounds endowed with potent Hsp90 inhibitory properties. We have found that compounds possessing a nitrogen atom directl... NHC Gold Halide Complexes Derived from 4,5-Diarylimidazoles: Synthesis, Structural Analysis, and Pharmacological Investigations as Potential Antitumor Agents [作者：LIU WUKUN; BENSDORF KERSTIN; PROETTO MARIA; ABRAM ULRICH; HAGENBACH ADELHEID; GUST RONALD,期刊：Journal of Medicinal Chemistry, 页码：8605-8615 , 文章类型： Article，,卷期：2011年54-24] A series of novel neutral NHC gold halide complexes derived from 4,5-diarylimidazoles were synthesized, characterized, and analyzed for biological effects. High growth inhibitory effects in MCF-7 and MDA-MB 231 breast ca... Identification of Benzoxazin-3-one Derivatives as Novel, Potent, and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists [作者：HASUI TOMOAKI; MATSUNAGA NOBUYUKI; ORA TAIICHI; OHYABU NORIO; NISHIGAKI NOBUHIRO; IMURA YOSHIMI; IGATA YUMIKO; MATSUI HIDEKI; MOTOYAJI TAKASHI; TANAKA TOSHIMASA; HABUKA NORIYUKI; SOGABE SATOSHI; ONO MIDORI; SIEDEM CHRISTOPHER S; TANG TONY P; GAUTHIER CASSANDRA; DE MEESE LISA A; BOYD STEVEN A; FUKUMOTO SHOJI,期刊：Journal of Medicinal Chemistry, 页码：8616-8631 , 文章类型： Article，,卷期：2011年54-24] Mineralocorticoid receptor (MR) blockade has come into focus as a promising approach for the treatment of cardiovascular diseases such as hypertension and congestive heart failure. In order to identify a novel class of n... Phosphorodiamidates as a Promising New Phosphate Prodrug Motif for Antiviral Drug Discovery: Application to Anti-HCV Agents [作者：MCGUIGAN CHRISTOPHER; MADELA KAROLINA; ALJARAH MOHAMED; BOURDIN CLAIRE; ARRICA MARIA; BARRETT EMMA; JONES SARAH; KOLYKHALOV ALEXANDER; BLEIMAN BLAIR; BRYANT K DAWN; GANGULY BABITA; GOROVITS ELENA; HENSON GEOFFREY; HUNLEY DAMOUND; HUTCHINS JEFF; MUHAMMAD JERRY; OBIKHOD ALEKSANDR; PATTI JOSEPH; WALTERS C ROBIN; WANG JIN; VERNACHIO JOHN; RAMAMURTY CHANGALVALA V S; BATTINA SRINIVAS K; CHAMBERLAIN STANLEY,期刊：Journal of Medicinal Chemistry, 页码：8632-8645 , 文章类型： Article，,卷期：2011年54-24] We herein report phosphorodiamidates as a significant new phosphate prodrug motif. Sixty-seven phosphorodiamidates are reported of two 6-O-alkyl 2'-C-methyl guanosines, with significant variation in the diamidate structu... Comparative in Vitro Evaluation of N-Heterocyclic Carbene Gold(I) Complexes of the Benzimidazolylidene Type [作者：RUBBIANI RICCARDO; CAN SUZAN; KITANOVIC IGOR; ALBORZINIA HAMED; STEFANOPOULOU MARIA; KOKOSCHKA MALTE; MOENCHGESANG SUSANN; SHELDRICK WILLIAM S; WOELFL STEFAN; OTT INGO,期刊：Journal of Medicinal Chemistry, 页码：8646-8657 , 文章类型： Article，,卷期：2011年54-24] Gold(I) complexes with a 1,3-diethylbenzimidazol-2-ylidene N-heterocyclic carbene (NHC) ligand of the type NHC-Au-L (L = -Cl, -NHC, or -PPh(3)) were comparatively evaluated as thioredoxin reductase (TrxR) inhibitors and ... Retooling Manganese(III) Porphyrin-Based Peroxynitrite Decomposition Catalysts for Selectivity and Oral Activity: A Potential New Strategy for Treating Chronic Pain [作者：RAUSARIA SMITA; GHAFFARI MAHSA M E; KAMADULSKI ANDREW; RODGERS KENNY; BRYANT LEESA; CHEN ZHOUMOU; DOYLE TIM; SHAW MICHAEL J; SALVEMINI DANIELA; NEUMANN WILLIAM L,期刊：Journal of Medicinal Chemistry, 页码：8658-8669 , 文章类型： Article，,卷期：2011年54-24] Redox-active metalloporphyrins represent the most well-characterized class of catalysts capable of attenuating oxidative stress in vivo through the direct interception and decomposition of superoxide and peroxynitrite. W... Thiazolides as Novel Antiviral Agents. 2. Inhibition of Hepatitis C Virus Replication [作者：STACHULSKI ANDREW V; PIDATHALA CHANDRAKALA; ROW ELEANOR C; SHARMA RAMAN; BERRY NEIL G; LAWRENSON ALEXANDRE S; MOORES SHELLEY L; IQBAL MAZHAR; BENTLEY JOANNE; ALLMAN SARAH A; EDWARDS GEOFFREY; HELM ALISON; HELLIER JENNIFER; KORBA BRENT E; SEMPLE J EDWARD; ROSSIGNOL JEANFRANCOIS,期刊：Journal of Medicinal Chemistry, 页码：8670-8680 , 文章类型： Article，,卷期：2011年54-24] We report the activities of a number of thiazolides [2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis C virus (HCV) genotypes IA and IB, using replicon assays. The structure activity relationships (SARs) of thiaz... Structure-Activity Relationship Studies of Sulfonylpiperazine Analogues as Novel Negative Allosteric Modulators of Human Neuronal Nicotinic Receptors [作者：HENDERSON BRANDON J; CARPER DANIEL J; GONZALEZCESTARI TATIANA F; YI BITNA; MAHASENAN KIRAN; PAVLOVICZ RYAN E; DALEFIELD MARTIN L; COLEMAN ROBERT S; LI CHENGLONG; MCKAY DENNIS B,期刊：Journal of Medicinal Chemistry, 页码：8681-8692 , 文章类型： Article，,卷期：2011年54-24] Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer's disease, Parkinson's disease, epilepsy, and various forms of addiction. To understand the role of nicotinic ...