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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24条记录   Synthesis, Structure-Activity Relationship, and Mode-of-Action Studies of Antimalarial Reversed Chloroquine Compounds [作者：BURGESS STEVEN J; KELLY JANE X; SHOMLOO SHAWHEEN; WITTLIN SERGIO; BRUN RETO; LIEBMANN KATHERINE; PEYTON DAVID H,期刊：Journal of Medicinal Chemistry, 页码：6477-6489 , 文章类型： Article，,卷期：2010年53-17] We have previously shown that a "reversed chloroquine (RCQ)" molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum (Burgess, S. J.; Se... Novel Carbamates as Orally Active Acetylcholinesterase Inhibitors Found to Improve Scopolamine-Induced Cognition Impairment: Pharmacophore-Based Virtual Screening, Synthesis, and Pharmacology [作者：CHAUDHAERY SHAILENDRA S; ROY KULDEEP K; SHAKYA NEERAJ; SAXENA GUNJAN; SAMMI SHREESH RAJ; NAZIR AAMIR; NATH CHANDISHWAR; SAXENA ANIL K,期刊：Journal of Medicinal Chemistry, 页码：6490-6505 , 文章类型： Article，,卷期：2010年53-17] A systematic virtual screening (VS) experiment, consisting of the development of 3D-pharmacophore, screening of virtual library, synthesis, and pharmacology, is reported. The predictive pharmacophore model (correlation =... Design, Synthesis, and in Vitro Pharmacology of New Radiolabeled gamma-Hydroxybutyric Acid Analogues Including Photolabile Analogues with Irreversible Binding to the High-Affinity gamma-Hydroxybutyric Acid Binding Sites [作者：SABBATINI PAOLA; WELLENDORPH PETRINE; HOG SIGNE; PEDERSEN MARTIN H F; BRAUNEROSBORNE HANS; MARTINY LARS; FROLUND BENTE; CLAUSEN RASMUS P,期刊：Journal of Medicinal Chemistry, 页码：6506-6510 , 文章类型： Article，,卷期：2010年53-17] gamma-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, the complete molecular mechanisms of action remain unexplained. To facilitate the isol... alpha,beta-Unsaturated N-Acylpyrrole Peptidyl Derivatives: New Proteasome Inhibitors [作者：BALDISSEROTTO ANNA; FERRETTI VALERIA; DESTRO FEDERICA; FRANCESCHINI CHRISTIAN; MARASTONI MAURO; GAVIOLI RICCARDO; TOMATIS ROBERTO,期刊：Journal of Medicinal Chemistry, 页码：6511-6515 , 文章类型： Article，,卷期：2010年53-17] Because of the encouraging results obtained using vinyl ester derivatives, we synthesized and tested a novel series of peptide-based proteasome inhibitors bearing a new pharmacophore unit at the C-terminal. N-Acylpyrrole... Synthesis, Stereochemical Separation, and Biological Evaluation of Selective Inhibitors of Human MAO-B: 1-(4-Arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines [作者：CHIMENTI FRANCO; SECCI DANIELA; BOLASCO ADRIANA; CHIMENTI PAOLA; GRANESE ARIANNA; CARRADORI SIMONE; YANEZ MATILDE; ORALLO FRANCISCO; SANNA M LUISA; GALLINELLA BRUNO; CIRILLI ROBERTO,期刊：Journal of Medicinal Chemistry, 页码：6516-6520 , 文章类型： Article，,卷期：2010年53-17] Novel 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazine derivatives have been investigated for their ability to inhibit selectively the activity of the human B isoform of monoamine oxidase. These compounds were... Factor Xa Inhibitors: Next-Generation Antithrombotic Agents [作者：PINTO DONALD J P; SMALLHEER JOANNE M; CHENEY DANIEL L; KNABB ROBERT M; WEXLER RUTH R,期刊：Journal of Medicinal Chemistry, 页码：6243-6274 , 文章类型： Article，,卷期：2010年53-17] Synthesis and Biological Effects of Hydrogen Sulfide (H2S): Development of H2S-Releasing Drugs as Pharmaceuticals [作者：CALIENDO GIUSEPPE; CIRINO GIUSEPPE; SANTAGADA VINCENZO; WALLACE JOHN L,期刊：Journal of Medicinal Chemistry, 页码：6275-6286 , 文章类型： Article，,卷期：2010年53-17] Identification and Development of Novel Inhibitors of Toxoplasma gondii Enoyl Reductase [作者：TIPPARAJU SURESH K; MUENCH STEPHEN P; MUI ERNEST J; RUZHEINIKOV SERGEY N; LU JEFFREY Z; HUTSON SAMUEL L; KIRISITS MICHAEL J; PRIGGE SEAN T; ROBERTS CRAIG W; HENRIQUEZ FIONA L; KOZIKOWSKI ALAN P; RICE DAVID W; MCLEOD RIMA L,期刊：Journal of Medicinal Chemistry, 页码：6287-6300 , 文章类型： Article，,卷期：2010年53-17] Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by toxicities and hypersensitivity. Because improved medicines are needed urgently, rational approaches were used to ident... Synthesis, in Vitro Activity, and Three-Dimensional Quantitative Structure-Activity Relationship of Novel Hydrazine Inhibitors of Human Vascular Adhesion Protein-1 [作者：NURMINEN ELISA M; PIHLAVISTO MARJO; LAZAR LASZLO; SZAKONYI ZSOLT; PENTIKAINEN ULLA; FULOP FERENC; PENTIKAINEN OLLI T,期刊：Journal of Medicinal Chemistry, 页码：6301-6315 , 文章类型： Article，,卷期：2010年53-17] Vascular adhesion protein-1 (VAP-1) belongs to the semicarbazide-sensitive amine oxidases (SSAOs) that convert amines into aldehydes. SSAOs are distinct from the mammalian monoamine oxidases (MAOs), but their substrate s... Toward Development of Targeted Nonsteroidal Antiandrogen-1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic Acid-Gadolinium Complex for Prostate Cancer Diagnostics [作者：MAROM HANIT; MILLER KEREN; BECHORBAR YOSSI; TSARFATY GALIA; SATCHIFAINARO RONIT; GOZIN MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：6316-6325 , 文章类型： Article，,卷期：2010年53-17] Androgen receptors are present in most advanced prostate cancer specimens, having a critical role in development of this type of cancer. For correct prognosis of patient conditions and treatment monitoring, noninvasive i... Peptidyl alpha-Ketoamides with Nucleobases, Methylpiperazine, and Dimethylaminoalkyl Substituents as Calpain Inhibitors [作者：OVAT ASLI; LI ZHAO ZHAO; HAMPTON CHRISTINA Y; ASRESS SENESHAW A; FERNANDEZ FACUNDO M; GLASS JONATHAN D; POWERS JAMES C,期刊：Journal of Medicinal Chemistry, 页码：6326-6336 , 文章类型： Article，,卷期：2010年53-17] A series of peptidyl alpha-ketoamides with the general structure Cbz-L-Leu-D,L-AA-CONH-R were synthesized and evaluated as inhibitors for the cystcine proteases calpain I, calpain II, and cathepsin B. Nucleobases, methyl... Identification of CKD-516: A Potent Tubulin Polymerization Inhibitor with Marked Antitumor Activity against Murine and Human Solid Tumors [作者：LEE JAEKWANG; KIM SOO JIN; CHOI HOJIN; KIM YOUNG HOON; LIM IN TACK; YANG HYUNMO; LEE CHANG SIK; KANG HEE RYONG; AHN SOON KIL; MOON SEUNG KEE; KIM DALHYUN; LEE SUNGSOOK; CHOI NAM SONG; LEE KYUNG JOO,期刊：Journal of Medicinal Chemistry, 页码：6337-6354 , 文章类型： Article，,卷期：2010年53-17] Tubulin polymerization inhibitors had emerged as one of promising anticancer therapeutics because of their dual mechanism of action, i.e. apoptosis by cell-cycle arrest and VDA, vascular disrupting agent. VDAs are believ... Discovery of Canagliflozin, a Novel C-Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus [作者：NOMURA SUMIHIRO; SAKAMAKI SHIGEKI; HONGU MITSUYA; KAWANISHI EIJI; KOGA YUICHI; SAKAMOTO TOSHIAKI; YAMAMOTO YASUO; UETA KIICHIRO; KIMATA HIROTAKA; NAKAYAMA KEIKO; TSUDATSUKIMOTO MINORU,期刊：Journal of Medicinal Chemistry, 页码：6355-6360 , 文章类型： Article，,卷期：2010年53-17] We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2 (SGLT2) than the O-glucoside, 2 (T-1095). A novel thiophene derivat... Nonpeptidic and Potent Small-Molecule Inhibitors of cIAP-1/2 and XIAP Proteins [作者：SUN HAIYING; LU JIANFENG; LIU LIU; YI HAN; QIU SU; YANG CHAOYIE; DESCHAMPS JEFFREY R; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：6361-6367 , 文章类型： Article，,卷期：2010年53-17] A series of compounds were designed and synthesized as antagonists of cIAP-1/2 and XIAP based upon our previously identified lead compound SM-122 (1). The most potent of these (7) binds to XIAP, cIAP-1, and cIAP-2 protei... Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor [作者：CEE VICTOR J; SCHENKEL LAURIE B; HODOUS BRIAN L; DEAK HOLLY L; NGUYEN HANH N; OLIVIERI PHILIP R; ROMERO KARINA; BAK ANNETTE; BE XUHAI; BELLON STEVE; BUSH TAMMY L; CHENG ALAN C; CHUNG GRACE; COATS STEVE; EDEN PATRICK M; HANESTAD KELLY; GALLANT PAUL L; GU YAN; HUANG XIN; KENDALL RICHARD L; LIN MINHWA JASMINE; MORRISON MICHAEL J; PATEL VINOD F; RADINSKY ROBERT; ROSE PAUL E; ROSS SANDRA; SUN JIRONG; TANG JIN; ZHAO HUILIN; PAYTON MARC; GEUNSMEYER STEPHANIE D,期刊：Journal of Medicinal Chemistry, 页码：6368-6377 , 文章类型： Article，,卷期：2010年53-17] The discovery of aurora kinases as essential regulators of cell division has led to intense interest in identifying small molecule aurora kinase inhibitors for the potential treatment of cancer. A high-throughput screeni... Synthesis and Characterization of Nitroimidazole Derivatives for Ga-68-Labeling and Testing in Tumor Xenografted Mice [作者：HOIGEBAZAR LATHIKA; JEONG JAE MIN; CHOI SOO YOUNG; CHOI JAE YEON; SHETTY DINESH; LEE YUNSANG; LEE DONG SOO; CHUNG JUNEKEY; LEE MYUNG CHUL; CHUNG YOUNG KEUN,期刊：Journal of Medicinal Chemistry, 页码：6378-6385 , 文章类型： Article，,卷期：2010年53-17] Radiolabeled nitroimidazole (NI) derivatives have been used for imaging hypoxic tissues. We synthesized NI derivatives conjugated with bifunctional chelating agents such as 1,4,7-triazacyclononane-1,4,7-triacetic acid (N...