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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57条记录   Imidazoquines as Antimalarial and Antipneumocystis Agents [作者：VALE NUNO; PRUDENCIO MIGUEL; MARQUES CATARINA A; COLLINS MARGARET S; GUT JIRI; NOGUEIRA FATIMA; MATOS JOANA; ROSENTHAL PHILIP J; CUSHION MELANIE T; DO ROSARIO VIRGILIO E; MOTA MARIA M; MOREIRA RUI; GOMES PAULA,期刊：Journal of Medicinal Chemistry, 页码：7800-7807 , 文章类型： Article，,卷期：2009年52-23] Peptidomimetic imidazolidin-4-one derivatives of primaquine (imidazoquines) recently displayed in vitro activity against blood schizonts of a chloroquine-resistant strain of Plasmodium falciparum. Preliminary studies wit... Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N '-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor [作者：CHAO QI; SPRANKLE KELLY G; GROTZFELD ROBERT M; LAI ANDILIY G; CARTER TODD A; VELASCO ANNE MARIE; GUNAWARDANE RUWANTHI N; CRAMER MERRYL D; GARDNER MICHAEL F; JAMES JOYCE; ZARRINKAR PATRICK P; PATEL HITESH K; BHAGWAT SHRIPAD S,期刊：Journal of Medicinal Chemistry, 页码：7808-7816 , 文章类型： Article，,卷期：2009年52-23] Treatment of AM L patients with small molecule inhibitors of FLT3 kinase has been explored as a viable therapy. However, these agents arc found to be less than optimal for the treatment of AM L because of lack of suffici... Exploring the Importance of Piperazine N-Atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) [作者：BERARDI FRANCESCO; ABATE CARMEN; FERORELLI SAVINA; URICCHIO VINCENZO; COLABUFO NICOLA A; NISO MAURO; PERRONE ROBERTO,期刊：Journal of Medicinal Chemistry, 页码：7817-7828 , 文章类型： Article，,卷期：2009年52-23] sigma(2)-Agonist 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]p iperazine (7, PB 28), which proved to revert doxorubicin resistance in breast cancer cells, was taken as a template to prepare new ... Carborane Derivatives Loaded into Liposomes as Efficient Delivery Systems for Boron Neutron Capture Therapy [作者：ALTIERI S; BALZI M; BORTOLUSSI S; BRUSCHI P; CIANI L; CLERICI A M; FARAONI P; FERRARI C; GADAN M A; PANZA L; PIETRANGELI D; RICCIARDI G; RISTORI S,期刊：Journal of Medicinal Chemistry, 页码：7829-7835 , 文章类型： Article，,卷期：2009年52-23] Boron neutron capture therapy (BNCT) is an anticancer therapy based oil the incorporation of 1013 in tumors, followed by neutron irradiation. Recently, the synthesis and delivery of new boronated compounds have been reco... Discovery of Potent and Selective Histone Deacetylase Inhibitors via Focused Combinatorial Libraries of Cyclic alpha(3)beta-Tetrapeptides [作者：OLSEN CHRISTIAN A; GHADIRI M REZA,期刊：Journal of Medicinal Chemistry, 页码：7836-7846 , 文章类型： Article，,卷期：2009年52-23] Historic deacetylase (HDAC) inhibitors are powerful tools in understanding epigenetic regulation and have proven especially promising for the treatment of various cancers, but the discovery of potent, isoform-selective H... Discovery of a 2,4-Disubstituted Pyrrolo[1,2-f][1,2,4]triazine Inhibitor (BMS-754807) of Insulin-like Growth Factor Receptor (IGF-1R) Kinase in Clinical Development [作者：WITTMAN MARK D; CARBONI JOAN M; YANG ZHENG; LEE FRANCIS Y; ANTMAN MELISSA; ATTAR RICARDO; BALIMANE PRAVEEN; CHANG CHIEHYING; CHEN CLIFF; DISCENZA LORELL; FRENNESSON DAVID; GOTTARDIS MARCO M; GREER ANN; HURLBURT WARREN; JOHNSON WALTER; LANGLEY DAVID R; LI AIXIN; LI JIANQING; LIU PEIYING; MASTALERZ HAROLD; MATHUR ARVIND; MENARD KRISTA; PATEL KARISHMA; SACK JOHN; SANG XIAOPENG; SAULNIER MARK; SMITH DANIEL; STEFANSKI KEVIN; TRAINOR GEORGE; VELAPARTHI UPENDER; ZHANG GUIFEN; ZIMMERMANN KURT; VYAS DOLATRAI M,期刊：Journal of Medicinal Chemistry, 页码：7360-7363 , 文章类型： Article，,卷期：2009年52-23] This report describes the biological activity, characterization, and SAR leading to 9d (BMS-754807) a small molecule IGF-1R kinase inhibitor in clinical development. Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model [作者：YUE EDDY W; DOUTY BRENT; WAYLAND BRIAN; BOWER MICHAEL; LIU XIANGDONG; LEFFET LYNN; WANG QIAN; BOWMAN KEVIN J; HANSBURY MICHAEL J; LIU CHANGNIAN; WEI MIN; LI YANLONG; WYNN RICHARD; BURN TIMOTHY C; KOBLISH HOLLY K; FRIDMAN JORDAN S; METCALF BRIAN; SCHERLE PEGGY A; COMBS ANDREW P,期刊：Journal of Medicinal Chemistry, 页码：7364-7367 , 文章类型： Article，,卷期：2009年52-23] A hydroxyamidine chemotype has been discovered as a key pharmacophore in novel inhibitors of indoleamine 2,3-dioxygenase (I DO). Optimization led to the identification of 5l, which is a potent (HeLa IC50 = 19 nM) competi... Mechanistic Insight into the Inhibition of Matrix Metalloproteinases by Platinum Substrates [作者：ARNESANO FABIO; BOCCARELLI ANGELA; CORNACCHIA DANIELE; NUSHI FIORENTIN; SASANELLI ROSSELLA; COLUCCIA MAURO; NATILE GIOVANNI,期刊：Journal of Medicinal Chemistry, 页码：7847-7855 , 文章类型： Article，,卷期：2009年52-23] Platinum compounds are among the most used DNA-damaging anticancer drugs, however they can also be tailored to target biological substrates different from DNA, for instance enzymes involved in cancer progression. We rece... Identification of Lead Compounds As Antagonists of Protein Bcl-x(L) with a Diversity-Oriented Multidisciplinary Approach [作者：DI MICCO SIMONE; VITALE ROMINA; PELLECCHIA MAURIZIO; REGA MICHELE F; RIVA RENATA; BASSO ANDREA; BIFULCO GIUSEPPE,期刊：Journal of Medicinal Chemistry, 页码：7856-7867 , 文章类型： Article，,卷期：2009年52-23] We report on the use of a diversity oriented synthesis (DOS) approach that resulted in the generation of a set of libraries of compounds presenting novel structural cores. These chemical cores have been employed to desig... High Lipophilicity of meta Mn(III) N-Alkylpyridylporphyrin-Based Superoxide Dismutase Mimics Compensates for Their Lower Antioxidant Potency and Makes Them as Effective as Ortho Analogues in Protecting Superoxide Dismutase-Deficient Escherichia coli [作者：KOS IVAN; BENOV LUDMIL; SPASOJEVIC IVAN; REBOUCAS JULIO S; BATINICHABERLE INES,期刊：Journal of Medicinal Chemistry, 页码：7868-7872 , 文章类型： Article，,卷期：2009年52-23] Lipophilicity/bioavailibility of Mn(III) N-alkylpyridylporphyrin-based superoxide dismutase (SOD) mimics has a major impact oil their in vivo ability to suppress oxidative stress. Meta isomers are less potent SOD mimics ... Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors [作者：SONG GAOPENG; YANG SEN; ZHANG WEI; CAO YINGLI; WANG PENG; DING NING; ZHANG ZAIHONG; GUO YING; LI YINGXIA,期刊：Journal of Medicinal Chemistry, 页码：7368-7371 , 文章类型： Article，,卷期：2009年52-23] The occurrence of highly pathogenic avian influenza virus H5N1 highlights the urgent need for new classes of antiviral drugs. Inhibition of H5N1 entry into cells may be an effective strategy. We report the first three sm... Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors [作者：SINHA BHASWATI; CAO ZHENGYU; MURRAY THOMAS F; ALDRICH JANE V,期刊：Journal of Medicinal Chemistry, 页码：7372-7375 , 文章类型： Article，,卷期：2009年52-23] A series of potent electrophilic affinity labels (IC50 = 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the mu opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogues... Synthesis of New Linear Guanidines and Macrocyclic Amidinourea Derivatives Endowed with High Antifungal Activity against Candida spp. and Aspergillus spp. [作者：MANETTI FABRIZIO; CASTAGNOLO DANIELE; RAFFI FRANCESCO; ZIZZARI ALESSANDRA T; RAJAMAKI SUVI; DAREZZO SILVIA; VISCA PAOLO; CONA ALESSANDRA; FRACASSO MARIA ENRICA; DORIA DENISE; POSTERARO BRUNELLA; SANGUINETTI MAURIZIO; FADDA GIOVANNI; BOTTA MAURIZIO,期刊：Journal of Medicinal Chemistry, 页码：7376-7379 , 文章类型： Article，,卷期：2009年52-23] New linear and Cyclic guanidines were synthesized and tested in vitro for their antifungal activity toward clinically relevant strains of Candida species, in comparison to fluconazole. Macrocyclic Compounds showed a mini... Modifications at the C-Terminus To Improve Pyrrole-Imidazole Polyamide Activity in Cell Culture [作者：JACOBS CLAIRE S; DERVAN PETER B,期刊：Journal of Medicinal Chemistry, 页码：7380-7388 , 文章类型： Article，,卷期：2009年52-23] Pyrrole-imidazole (Py-Im) hairpin Polyamides are a class of small molecule DNA minor groove binding compounds that have been shown to modulate endogenous gene expression in cell culture. Gene regulation by polyamides req... Univalent and Bivalent Ligands of Butorphan: Characteristics of the Linking Chain Determine the Affinity and Potency of Such Opioid Ligands [作者：DECKER MICHAEL; FULTON BRIAN S; ZHANG BIN; KNAPP BRIAN I; BIDLACK JEAN M; NEUMEYER JOHN L,期刊：Journal of Medicinal Chemistry, 页码：7389-7396 , 文章类型： Article，,卷期：2009年52-23] Bivalent morphinan compounds containing ester linkers were synthesized and their binding affinities at the mu, delta, and kappa opioid receptors determined. Addition of methyl groups adjacent to the hydrolytically labile... Design, Synthesis, and Biological Evaluation of Substituted Naphthalene Imides and Diimides as Anticancer Agent [作者：TUMIATTI VINCENZO; MILELLI ANDREA; MINARINI ANNA; MICCO MARIALUISA; CAMPANI ANNA GASPERI; RONCUZZI LAURA; BAIOCCHI DANIELA; MARINELLO JESSICA; CAPRANICO GIOVANNI; ZINI MADDALENA; STEFANELLI CLAUDIO; MELCHIORRE CARLO,期刊：Journal of Medicinal Chemistry, 页码：7873-7877 , 文章类型： Article，,卷期：2009年52-23] Naphthalimmide (NI) and 1,4,5,8-naphthalenetetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI ...