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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35条记录   Lipo-gamma-AApeptides as a New Class of Potent and Broad-Spectrum Antimicrobial Agents [作者：NIU YOUHONG; PADHEE SHRUTI; WU HAIFAN; BAI GE; QIAO QIAO; HU YAOGANG; HARRINGTON LACEY; BURDA WHITTNEY N; SHAW LINDSEY N; CAO CHUANHAI; CAI JIANFENG,期刊：Journal of Medicinal Chemistry, 页码：4003-4009 , 文章类型： Article，,卷期：2012年55-8] There is increasing demand to develop antimicrobial peptides (AMPs) as next generation antibiotic agents, as they have the potential to circumvent emerging drug resistance against conventional antibiotic treatments. Non-... Computational Design and Discovery of "Minimally Structured" hERG Blockers [作者：CAVALLI ANDREA; BUONFIGLIO ROSA; IANNI CRISTINA; MASETTI MATTEO; CECCARINI LUISA; CAVES RACHEL; CHANG MICHAEL W Y; MITCHESON JOHN S; ROBERTI MARINELLA; RECANATINI MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：4010-4014 , 文章类型： Article，,卷期：2012年55-8] Molecular knowledge of hERG blocking liability can offer the possibility of optimizing lead compounds in a way that eliminates potentially lethal side effects. In this study, we computationally designed, synthesized, and... Effect of Nonenzymatic Glycosylation on the Magnetic Resonance Imaging (MRI) Contrast Agent Binding to Human Serum Albumin [作者：HENOUMONT CELINE; LAURENT SOPHIE; MULLER ROBERT N; ELST LUCE VANDER,期刊：Journal of Medicinal Chemistry, 页码：4015-4019 , 文章类型： Article，,卷期：2012年55-8] Enhanced nonenzymatic glycosylation (NEG) of human serum albumin (HSA) is observed in diabetic patients. This modifies some of the physiological functions of HSA, as the binding of ligands. Some gadolinium complexes, com... Design, Synthesis, and Biological Evaluation of Conformationally Constrained Analogues of Naphthol AS-E as Inhibitors of CREB-Mediated Gene Transcription [作者：JIANG MIN; LI BINGBING X; XIE FUCHUN; DELANEY FRANCES; XIAO XIANGSHU,期刊：Journal of Medicinal Chemistry, 页码：4020-4024 , 文章类型： Article，,卷期：2012年55-8] Cyclic AMP response element binding protein (CREB) is often dysregulated in cancer cells and is an attractive cancer drug target. Previously, we described naphthol AS-E (1) as a small molecule inhibitor of CREB-mediated ... Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12, 13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3, 4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent (vol 55, pg 903, 2012) [作者：HUDKINS ROBERT L; BECKNELL NADINE C; ZULLI ALLISON L; UNDERINER TED L; ANGELES THELMA S; AIMONE LISA D; ALBOM MARK S; CHANG HONG; MIKNYOCZKI SHEILA J; HUNTER KATHRYN; JONESBOLIN SUSAN; ZHAO HUGH; BACON EDWARD R; MALLAMO JOHN P; ATOR MARK A; RUGGERI BRUCE A,期刊：Journal of Medicinal Chemistry, 页码：4025-4025 , 文章类型： Correction，,卷期：2012年55-8] Cellular Quantitative Structure-Activity Relationship (Cell-QSAR): Conceptual Dissection of Receptor Binding and Intracellular Disposition in Antifilarial Activities of Selwood Antimycins [作者：NATESAN SENTHIL; WANG TIANSHENG; LUKACOVA VIERA; BARTUS VLADIMIR; KHANDELWAL AKASH; SUBRAMANIAM RAJESH; BALAZ STEFAN,期刊：Journal of Medicinal Chemistry, 页码：3699-3712 , 文章类型： Article，,卷期：2012年55-8] We present the cellular quantitative structure-activity relationship (cell-QSAR) concept that adapts ligand-based and receptor-based 3D-QSAR methods for use with cell-level activities. The unknown intracellular drug disp... Synthesis, Characterization, and in Vitro Studies of Bis[1,3-diethyl-4,5-diarylimidazol-2-ylidene]gold(I/III) Complexes [作者：LIU WUKUN; BENSDORF KERSTIN; PROETTO MARIA; HAGENBACH ADELHEID; ABRAM ULRICH; GUST RONALD,期刊：Journal of Medicinal Chemistry, 页码：3713-3724 , 文章类型： Article，,卷期：2012年55-8] Cationic bis[1,3-diethyl-4,5-diarylimidazol-2-ylidene]gold(I) complexes with 4-OCH3 or 4-F substituents in the aromatic rings and Br- (3a,b) or BF4- (7a,b) counterions were synthesized, characterized, and investigated fo... Phthalocyanine-Peptide Conjugates for Epidermal Growth Factor Receptor Targeting [作者：ONGARORA BENSON G; FONTENOT KRYSTAL R; HU XIAOKE; SEHGAL INDER; SATYANARAYANAJOIS SEETHARAMA D; VICENTE DM GRACA H,期刊：Journal of Medicinal Chemistry, 页码：3725-3738 , 文章类型： Article，,卷期：2012年55-8] Four phthalocyanine (Pc)-peptide conjugates designed to target the epidermal growth factor receptor (EGFR) were synthesized and evaluated in vitro using four cell lines: human carcinoma A431 and HEp2, human colorectal HT... Discovery of Selective Menaquinone Biosynthesis Inhibitors against Mycobacterium tuberculosis [作者：DEBNATH JOY; SIRICILLA SHAJILA; WAN BAJOIE; CRICK DEAN C; LENAERTS ANNE J; FRANZBLAU SCOTT G; KUROSU MICHIO,期刊：Journal of Medicinal Chemistry, 页码：3739-3755 , 文章类型： Article，,卷期：2012年55-8] Aurachin RE (1) is a strong antibiotic that was recently found to possess 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA) and bacterial electron transport inhibitory activities. Aurachin RE is the only molecule in a ... Searching for New Chemotherapies for Tropical Diseases: Ruthenium-Clotrimazole Complexes Display High in Vitro Activity against Leishmania major and Trypanosoma cruzi and Low Toxicity toward Normal Mammalian Cells [作者：MARTINEZ ALBERTO; CARREON TERESIA; INIGUEZ EVA; ANZELLOTTI ATILIO; SANCHEZ ANTONIO; TYAN MARINA; SATTLER AARON; HERRERA LINDA; MALDONADO ROSA A; SANCHEZDELGADO ROBERTO A,期刊：Journal of Medicinal Chemistry, 页码：3867-3877 , 文章类型： Article，,卷期：2012年55-8] Eight new ruthenium complexes of clotrimazole (CTZ) with high antiparasitic activity have been synthesized, cis,fac-[(RuCl2)-Cl-II(DMSO)(3)(CTZ)] (1), cis,cis,trans-[(RuCl2)-Cl-II(DMSO)(2)(CTZ)(2)] (2), Na[(RuCl4)-Cl-III... Synthesis, Binding Affinity, and Functional in Vitro Activity of 3-Benzylaminomorphinan and 3-Benzylaminomorphine Ligands at Opioid Receptors [作者：NEUMEYER JOHN L; ZHANG BIN; ZHANG TANGZHI; SROMEK ANNA W; KNAPP BRIAN I; COHEN DANA J; BIDLACK JEAN M,期刊：Journal of Medicinal Chemistry, 页码：3878-3890 , 文章类型： Article，,卷期：2012年55-8] A series of 3-benzylamino-3-desoxymorphinan (I) and 3-benzylamino-3-desoxymorphine (II) derivatives were synthesized and evaluated for their binding affinities, and functional activity data are presented at MOR, KOR, and... Synthesis, Structure-Activity Relationship Studies, and X-ray Crystallographic Analysis of Arylsulfonamides as Potent Carbonic Anhydrase Inhibitors [作者：GITTO ROSARIA; DAMIANO FRANCESCA M; MADER PAVEL; DE LUCA LAURA; FERRO STEFANIA; SUPURAN CLAUDIU T; VULLO DANIELA; BRYNDA JIRI; REZACOVA PAVLINA; CHIMIRRI ALBA,期刊：Journal of Medicinal Chemistry, 页码：3891-3899 , 文章类型： Article，,卷期：2012年55-8] A series of arylsulfonamides has been synthesized and investigated for the inhibition of some selected human carbonic anhydrase isoforms. The studied compounds showed significant inhibitory effects in the nanomolar range... Synthesis and Biological Activity of Potent HIV-1 Protease Inhibitors Based on Phe-Pro Dihydroxyethylene Isosteres [作者：BENEDETTI FABIO; BERTI FEDERICO; BUDAL SARA; CAMPANER PIETRO; DINON FRANCESCA; TOSSI ALESSANDRO; ARGIROVA RADKA; GENOVA PETIA; ATANASSOV VASIL; HINKOV ANTON,期刊：Journal of Medicinal Chemistry, 页码：3900-3910 , 文章类型： Article，,卷期：2012年55-8] Peptidomimetic inhibitors of HIV-1 PR are still a key resource in the fight against AIDS. Here we describe the synthesis and biological activity of HIV-1 PR inhibitors based on four novel dihydroxyethylene isosteres of t... Design, Synthesis, and Structure-Activity Correlations of Novel Dibenzo[b,d]furan, Dibenzo[b,d]thiophene, and N-Methylcarbazole Clubbed 1,2,3-Triazoles as Potent Inhibitors of Mycobacterium tuberculosis [作者：PATPI SANTHOSH REDDY; PULIPATI LOKESH; YOGEESWARI PERUMAL; SRIRAM DHARMARAJAN; JAIN NISHANT; SRIDHAR BALASUBRAMANIAN; MURTHY RAMALINGA; DEVI ANJANA T; KALIVENDI SHASI VARDHAN; KANTEVARI SRINIVAS,期刊：Journal of Medicinal Chemistry, 页码：3911-3922 , 文章类型： Article，,卷期：2012年55-8] A molecular hybridization approach is an emerging structural modification tool to design new molecules with improved pharmacophoric properties. In this study, 1,2,3-triazole-based Mycobacterium tuberculosis inhibitors an... Rationally Designing Safer Anilines: The Challenging Case of 4-Aminobiphenyls [作者：BIRCH ALAN M; GROOMBRIDGE SAM; LAW ROBERT; LEACH ANDREW G; MEE CHRISTINE D; SCHRAMM CAROLIN,期刊：Journal of Medicinal Chemistry, 页码：3923-3933 , 文章类型： Article，,卷期：2012年55-8] We describe how we have been able to design 4-aminobiphenyls that are nonmutagenic (inactive in the Ames test). No such 4-aminobiphenyls were known to us, but insights provided by quantum mechanical calculations have per... Dabigatran and Dabigatran Ethyl Ester: Potent Inhibitors of Ribosyldihydronicotinamide Dehydrogenase (NQO2) [作者：MICHAELIS SIMON; MARAIS ANETT; SCHREY ANNA K; GRAEBNER OLIVIA Y; SCHAUDT CORNELIA; SEFKOW MICHAEL; KROLL FRIEDRICH; DREGER MATHIAS; GLINSKI MIRKO; KOESTER HUBERT; METTERNICH RAINER; FISCHER JENNY J,期刊：Journal of Medicinal Chemistry, 页码：3934-3944 , 文章类型： Article，,卷期：2012年55-8] Recent studies have revealed that compounds believed to be highly selective frequently address multiple target proteins. We investigated the protein interaction profile of the widely prescribed thrombin inhibitor dabigat...