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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42条记录   Colloid Formation by Drugs in Simulated Intestinal Fluid [作者：DOAK ALLISON K; WILLE HOLGER; PRUSINER STANLEY B; SHOICHET BRIAN K,期刊：Journal of Medicinal Chemistry, 页码：4259-4265 , 文章类型： Article，,卷期：2010年53-10] Many organic molecules form colloidal aggregates in aqueous solution at micromolar concentrations. These aggregates promiscuously inhibit soluble proteins and are a major source of false positives in high-throughput scre... 2-Aminoimidazole Amino Acids as Inhibitors of the Binuclear Manganese Metalloenzyme Human Arginase I [作者：ILIES MONICA; DI COSTANZO LUIGI; NORTH MICHELLE L; SCOTT JEREMY A; CHRISTIANSON DAVID W,期刊：Journal of Medicinal Chemistry, 页码：4266-4276 , 文章类型： Article，,卷期：2010年53-10] Arginase, a key metalloenzyme of the urea cycle that converts L-arginine into L-ornithine and urea, is presently considered a pharmaceutical target for the management of diseases associated with aberrant L-arginine homeo... Modulation of Cellular Adhesion by Glycoengineering [作者：DAFIK LAILA; DALARCAO MARC; KUMAR KRISHNA,期刊：Journal of Medicinal Chemistry, 页码：4277-4284 , 文章类型： Article，,卷期：2010年53-10] Aberrant glycosylation of lipid and protein molecules on cellular surfaces is responsible for many of the pathophysiological events in tumor progression and metastasis. Sialic acids in particular, are over-expressed on t... Entropic Contribution to the Linking Coefficient in Fragment Based Drug Design: A Case Study [作者：BORSI VALENTINA; CALDERONE VITO; FRAGAI MARCO; LUCHINAT CLAUDIO; SARTI NIKO,期刊：Journal of Medicinal Chemistry, 页码：4285-4289 , 文章类型： Article，,卷期：2010年53-10] For several drug leads obtained by tethering weak binding ligands, the dissociation constant is smaller than the product of those of the individual fragments by a factor named the linking coefficient, E. This favorable c... Synthesis and Evaluation of 17 alpha-Arylestradiols as Ligands for Estrogen Receptor alpha and beta [作者：SEDLAK DAVID; NOVAK PETR; KOTORA MARTIN; BARTUNEK PETR,期刊：Journal of Medicinal Chemistry, 页码：4290-4294 , 文章类型： Article，,卷期：2010年53-10] To identify novel estrogen receptor ligands a series of substituted 17 alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17 alpha-ethynylestradiol with various 1,7-diynes in the p... Crystal Structures of HIV-1 Reverse Transcriptase with Etravirine (TMC125) and Rilpivirine (TMC278): Implications for Drug Design [作者：LANSDON ERIC B; BRENDZA KATHERINE M; HUNG MAGDELEINE; WANG RUTH; MUKUND SUSMITH; JIN DEBI; BIRKUS GABRIEL; KUTTY NILIMA; LIU XIAOHONG,期刊：Journal of Medicinal Chemistry, 页码：4295-4299 , 文章类型： Article，,卷期：2010年53-10] Diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitors (NNRTIs) have inherent flexibility, helping to maintain activity against a wide range of resistance mutations. Crystal structures were determined wi... Stereochemical Requirements for the Mineralocorticoid Receptor Antagonist Activity of Dihydropyridines [作者：ARHANCET GRACIELA B; WOODARD SCOTT S; DIETZ JESSICA D; GARLAND DANNY J; WAGNER GRACE M; IYANAR KALIAPPAN; COLLINS JOE T; BLINN JAMES R; NUMANN RANDAL E; HU XIAO; HUANG HORNGCHIH,期刊：Journal of Medicinal Chemistry, 页码：4300-4304 , 文章类型： Article，,卷期：2010年53-10] A number of known 1,4-dihydropyridine CCBs were identified as having comparable potency to the steroidal MR antagonist eplerenone. Chiral resolution of mebudipine revealed that MR and CCB activity reside in opposite enan... Leech-Derived Thrombin Inhibitors: From Structures to Mechanisms to Clinical Applications [作者：ANGELES CORRALRODRIGUEZ MARIA; MACEDORIBEIRO SANDRA; BARBOSA PEREIRA PEDRO JOSE; FUENTESPRIOR PABLO,期刊：Journal of Medicinal Chemistry, 页码：3847-3861 , 文章类型： Article，,卷期：2010年53-10] Molecular Shape and Medicinal Chemistry: A Perspective [作者：NICHOLLS ANTHONY; MCGAUGHEY GEORGIA B; SHERIDAN ROBERT P; GOOD ANDREW C; WARREN GREGORY; MATHIEU MAGALI; MUCHMORE STEVEN W; BROWN SCOTT P; GRANT J ANDREW; HAIGH JAMES A; NEVINS NEYSA; JAIN AJAY N; KELLEY BRIAN,期刊：Journal of Medicinal Chemistry, 页码：3862-3886 , 文章类型： Article，,卷期：2010年53-10] Second Generation Analogues of the Cancer Drug Clinical Candidate Tipifarnib for Anti-Chagas Disease Drug Discovery [作者：KRAUS JAMES M; TATIPAKA HARI BABU; MCGUFFIN SARAH A; CHENNAMANENI NAVEEN KUMAR; KARIMI MANDANA; ARIF JENIFER; VERLINDE CHRISTOPHE L M J; BUCKNER FREDERICK S; GELB MICHAEL H,期刊：Journal of Medicinal Chemistry, 页码：3887-3898 , 文章类型： Article，,卷期：2010年53-10] We previously reported that the cancer drug clinical candidate tipifarnib kills the causative agent of Chagas disease, Trypanosoma cruzi, by blocking ergosterol biosynthesis at the level of inhibition of lanosterol 14 al... Vaccinia Virus Virulence Factor N1L is a Novel Promising Target for Antiviral Therapeutic Intervention [作者：CHELTSOV ANTON V; AOYAGI MIKA; ALESHIN ALEXANDER; YU ERIC CHIWANG; GILLILAND TAYLOR; ZHAI DAYONG; BOBKOV ANDREY A; REED JOHN C; LIDDINGTON ROBERT C; ABAGYAN RUBEN,期刊：Journal of Medicinal Chemistry, 页码：3899-3906 , 文章类型： Article，,卷期：2010年53-10] The 14 kDa homodimeric N1L protein is a potent vaccinia and variola (smallpox) virulence factor. It is not essential for viral replication, but it causes a strong attenuation of viral production in culture when deleted. ... Conserved High Activity Binding Peptides are Involved in Adhesion of Two Detergent-Resistant Membrane-Associated Merozoite Proteins to Red Blood Cells during Invasion [作者：ZULEIMA OBANDOMARTINEZ ANA; CURTIDOR HERNANDO; AREVALOPINZON GABRIELA; VANEGAS MAGNOLIA; VIZCAINO CAROLINA; ALFONSO PATARROYO MANUEL; ELKIN PATARROYO MANUEL,期刊：Journal of Medicinal Chemistry, 页码：3907-3918 , 文章类型： Article，,卷期：2010年53-10] Detergent resistant membranes (DRMs) of Plasmodium falciparum merozoites contain a large number of glycosylphosphatidylinositol (GPI)-anchored proteins that have been implicated in interactions between merozoites and red... Peptide Nucleic Acids Conjugated to Short Basic Peptides Show Improved Pharmacokinetics and Antisense Activity in Adipose Tissue [作者：WANCEWICZ EDWARD V; MAIER MARTIN A; SIWKOWSKI ANDREW M; ALBERTSHOFER KLAUS; WINGER THEODORE M; BERDEJA ANDRES; GAUS HANS; VICKERS TIMOTHY A; BENNETT C FRANK; MONIA BRETT P; GRIFFEY RICHARD H; NULF CHRISTOPHER J; HU JIAXIN; COREY DAVID R; SWAYZE ERIC E; KINBERGER GARTH A,期刊：Journal of Medicinal Chemistry, 页码：3919-3926 , 文章类型： Article，,卷期：2010年53-10] A peptide nucleic acid (PNA) targeting a splice junction of the amine PTEN primary transcript was covalently conjugated to various basic peptides. When systemically administered to healthy mice, the conjugates displayed ... Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties [作者：HAYDON DAVID J; BENNETT JAMES M; BROWN DAVID; COLLINS IAN; GALBRAITH GRETA; LANCETT PAUL; MACDONALD REBECCA; STOKES NEIL R; CHAUHAN PRAMOD K; SUTARIYA JIGNESH K; NAYAL NARENDRA; SRIVASTAVA ANIL; BEANLAND JOY; HALL ROBIN; HENSTOCK VINCENT; NOULA CATERINA; ROCKLEY CHRIS; CZAPLEWSKI LLOYD,期刊：Journal of Medicinal Chemistry, 页码：3927-3936 , 文章类型： Article，,卷期：2010年53-10] 3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the st... Novel Ferrocenic Steroidal Drug Derivatives and Their Bioactivities [作者：MANOSROI JIRADEJ; RUEANTO KANJANA; BOONPISUTTINANT KORAWINWICH; MANOSROI WORAPAKA; BIOT CHRISTOPHE; AKAZAWA HIROYUKI; AKIHISA TOSHIHIRO; ISSARANGPORN WITCHAPONG; MANOSROI ARANYA,期刊：Journal of Medicinal Chemistry, 页码：3937-3943 , 文章类型： Article，,卷期：2010年53-10] Seven novel ferrocenic derivatives, compounds 1-7, were synthesized from steroidal drugs by Aldol condensation reaction. The derivatives were purified by chromatography, and their structures were determined on the basis ... Synthesis of DOTA-Conjugated Multimeric [Tyr(3)]Octreotide Peptides via a Combination of Cu(I)-Catalyzed "Click" Cycloaddition and Thio Acid/Sulfonyl Azide "Sulfo-Click" Amidation and Their in Vivo Evaluation [作者：YIM CHENGBIN; DIJKGRAAF INGRID; MERKX REMCO; VERSLUIS CEES; EEK ANNEMARIE; MULDER GWENN E; RIJKERS DIRK T S; BOERMAN OTTO C; LISKAMP ROB M J,期刊：Journal of Medicinal Chemistry, 页码：3944-3953 , 文章类型： Article，,卷期：2010年53-10] Herein, we describe the design, synthesis, and biological evaluation of a series of DOTA-conjugated monomeric, dimeric, and tetrameric [Tyr(3)]octreotide-based analogues as a tool for tumor imaging and/or radionuclide th...