个性化文献订阅>文章检索

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15条记录   Synthesis and Evaluation of 1,5-Disubstituted Tetrazoles as Rigid Analogues of Combretastatin A-4 with Potent Antiproliferative and Antitumor Activity [作者：ROMAGNOLI ROMEO; BARALDI PIER GIOVANNI; SALVADOR MARIA KIMATRAI; PRETI DELIA; TABRIZI MOJGAN AGHAZADEH; BRANCALE ANDREA; FU XIANHUA; LI JUN; ZHANG SUZHAN; HAMEL ERNEST; BORTOLOZZI ROBERTA; BASSO GIUSEPPE; VIOLA GIAMPIETRO,期刊：Journal of Medicinal Chemistry, 页码：475-488 , 文章类型： Article，,卷期：2012年55-1] Tubulin, the major structural component of microtubules, is a target for the development of anticancer agents. Two series of 1,5-diaryl substituted 1,2,3,4-tetrazoles were concisely synthesized, using a palladium-catalyz... Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious gamma-Secretase Modulators in Vivo [作者：SUN ZHONGYUE; ASBEROM THEODROS; BARA THOMAS; BENNETT CHAD; BURNETT DUANE; CHU INHOU; CLADER JOHN; COHENWILLIAMS MARY; COLE DAVID; CZARNIECKI MICHAEL; DURKIN JAMES; GALLO GIOCONDA; GREENLEE WILLIAM; JOSIEN HUBERT; HUANG XIANHAI; HYDE LYNN; JONES NICHOLAS; KAZAKEVICH IRINA; LI HONGMEI; LIU XIAOXIANG; LEE JULIE; MACCOSS MALCOLM; MANDAL MIHIR B; MCCRACKEN TROY; NOMEIR AMIN; MAZZOLA ROBERT; PALANI ANANDAN; PARKER ERIC M; PISSARNITSKI DMITRI A; QIN JUN; SONG LIXIN; TERRACINA GIUSEPPE; VICAREL MONICA; VOIGT JOHANNES; XU RUO; ZHANG LILI; ZHANG QI; ZHAO ZHIQIANG; ZHU XIAOHONG; ZHU ZHAONING,期刊：Journal of Medicinal Chemistry, 页码：489-502 , 文章类型： Article，,卷期：2012年55-1] Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharma... Niphatenones, Glycerol Ethers from the Sponge Niphates digitalis Block Androgen Receptor Transcriptional Activity in Prostate Cancer Cells: Structure Elucidation, Synthesis, and Biological Activity [作者：MEIMETIS LABROS G; WILLIAMS DAVID E; MAWJI NASRIN R; BANUELOS CARMEN A; LAL AARON A; PARK JACOB J; TIEN AMY H; FERNANDEZ JAVIER GARCIA; DE VOOGD NICOLE J; SADAR MARIANNE D; ANDERSEN RAYMOND J,期刊：Journal of Medicinal Chemistry, 页码：503-514 , 文章类型： Article，,卷期：2012年55-1] Extracts of the marine sponge Niphates digitalis collected in Dominica showed strong activity in a cell-based assay designed to detect antagonists of the androgen receptor (AR) that could act as lead compounds for the de... ADME-Guided Design and Synthesis of Aryloxanyl Pyrazolone Derivatives To Block Mutant Superoxide Dismutase 1 (SOD1) Cytotoxicity and Protein Aggregation: Potential Application for the Treatment of Amyotrophic Lateral Sclerosis [作者：CHEN TIAN; BENMOHAMED RADHIA; KIM JINHO; SMITH KAREN; AMANTE DANIEL; MORIMOTO RICHARD I; KIRSCH DONALD R; FERRANTE ROBERT J; SILVERMAN RICHARD B,期刊：Journal of Medicinal Chemistry, 页码：515-527 , 文章类型： Article，,卷期：2012年55-1] Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure: The arylsulfanyl pyrazolone (ASP) scaffold was one of the active scaffolds identified in a cell-based high throughput s... Diarylpropionitrile (DPN) Enantiomers: Synthesis and Evaluation of Estrogen Receptor beta-Selective Ligands [作者：CARROLL VINCENT M; JEYAKUMAR M; CARLSON KATHRYN E; KATZENELLENBOGEN JOHN A,期刊：Journal of Medicinal Chemistry, 页码：528-537 , 文章类型： Article，,卷期：2012年55-1] Two estrogen receptor (ER) subtypes, ER alpha and ER beta, mediate. the actions of estrogens in diverse reproductive and nonreproductive target tissues. ER subtype-selective ligands, which bind to and activate. these sub... Evaluation of Molecular Modeling of Agonist Binding in Light of the Crystallographic Structure of an Agonist-Bound A(2A) Adenosine Receptor [作者：DEFLORIAN FRANCESCA; KUMAR T SANTHOSH; PHAN KHAI; GAO ZHANGUO; XU FEI; WU HUIXIAN; KATRITCH VSEVOLOD; STEVENS RAYMOND C; JACOBSON KENNETH A,期刊：Journal of Medicinal Chemistry, 页码：538-552 , 文章类型： Article，,卷期：2012年55-1] Molecular modeling of agonist binding to the human A(2A) adenosine receptor (AR) was assessed and extended in light of crystallographic structures. Heterocyclic adenine nitrogens of cocrystallized agonist overlaid corres... Studies toward Novel Peptidomimetic Inhibitors of Thioredoxin-Thioredoxin Reductase System [作者：KLOSSOWSKI SZYMON; MUCHOWICZ ANGELIKA; FIRCZUK MALGORZATA; SWIECH MARTA; REDZEJ ADAM; GOLAB JAKUB; OSTASZEWSKI RYSZARD,期刊：Journal of Medicinal Chemistry, 页码：55-67 , 文章类型： Article，,卷期：2012年55-1] Thioredoxins (Trx) are ubiquitous multifunctional low-molecular weight proteins that together with thioredoxin reductases (TrxR) participate in the maintenance of protein thiol homeostasis in NADPH-dependent reactions. A... Design, Synthesis, and Evaluation of Thiol-Activated Sources of Sulfur Dioxide (SO(2)) as Antimycobacterial Agents [作者：MALWAL SATISH R; SRIRAM DHARMARAJAN; YOGEESWARI PERUMAL; KONKIMALLA V BADIREENATH; CHAKRAPANI HARINATH,期刊：Journal of Medicinal Chemistry, 页码：553-557 , 文章类型： Article，,卷期：2012年55-1] Here, 2,4-dinitrophenylsulfonamides with tunable cysteine-activated SO(2) release profiles with half-lives of SO(2) release varying from 2 to 63 min are reported. N-Benzyl-2,4-dinitrobenzenesulfonamide (6), which is prep... Synthesis of Rocaglamide Hydroxamates and Related Compounds as Eukaryotic Translation Inhibitors: Synthetic and Biological Studies [作者：RODRIGO CHRISTINA M; CENCIC REGINA; ROCHE STEPHANE P; PELLETIER JERRY; PORCO JOHN A JR,期刊：Journal of Medicinal Chemistry, 页码：558-562 , 文章类型： Article，,卷期：2012年55-1] The rocaglates/rocaglamides are a class of natural products known to display potent anticancer activity. One such derivative, silvestrol, has shown activity comparable to taxol in certain settings. Here, we report the sy... Synthesis and SAR of 5-Amino- and 5-(Aminomethyl)benzofuran Histamine H(3) Receptor Antagonists with Improved Potency (vol 48, pg 6482, 2005) [作者：SUN MINGHUA; ZHAO CHEN; GFESSER GREGORY A; THIFFAULT CHRISTINE; MILLER THOMAS R; MARSH KENNAN; WETTER JILL; CURTIS MICHAEL; FAGHIH RAMIN; ESBENSHADE TIMOTHY A; HANCOCK ARTHUR A; COWART MARLON,期刊：Journal of Medicinal Chemistry, 页码：563-563 , 文章类型： Correction，,卷期：2012年55-1] Tricyclic Series of Heat Shock Protein 90 (Hsp90) Inhibitors Part I: Discovery of Tricyclic Imidazo[4,5-c]pyridines as Potent Inhibitors of the Hsp90 Molecular Chaperone (vol 54, pg 7206, 2011) [作者：VALLEE FRANCOIS; CARREZ CHANTAL; PILORGE FABIENNE; DUPUY ALAIN; PARENT ANNICK; BERTIN LUC; THOMPSON FABIENNE; FERRARI PAUL; FASSY FLORENCE; LAMBERTON ANNABELLE; THOMAS ANNE; ARREBOLA ROSALIA; GUERIF STEPHANE; ROHAUT ALEXANDRE; CERTAL VICTOR; RUXER JEANMARIE; GOUYON THIERRY; DELORME CECILE; JOUANEN ALAIN; DUMAS JACQUES; GREPIN CLAUDINE; COMBEAU CECILE; GOULAOUIC HELENE; DEREU NORBERT; MIKOL VINCENT; MAILLIET PATRICK; MINOUX HERVE,期刊：Journal of Medicinal Chemistry, 页码：564-564 , 文章类型： Correction，,卷期：2012年55-1] Targeting the Binding Function 3 (BF3) Site of the Human Androgen Receptor through Virtual Screening (vol 54, pg 8563, 2011) [作者：LACK NATHAN A; AXERIOCILIES PETER; TAYASSOLI 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：565-565 , 文章类型： Correction，,卷期：2012年55-1] Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors [作者：FLIPO MARION; DESROSES MATTHIEU; LECATGUILLET NATHALIE; VILLEMAGNE BAPTISTE; BLONDIAUX NICOLAS; LEROUX FLORENCE; PIVETEAU CATHERINE; MATHYS VANESSA; FLAMENT MARIEPIERRE; SIEPMANN JUERGEN; VILLERET VINCENT; WOHLKONIG ALEXANDRE; WINTJENS RENE; SOROR SAMEH H; CHRISTOPHE THIERRY; JEON HEE KYOUNG; LOCHT CAMILLE; BRODIN PRISCILLE; DEPREZ BENOIT; BAULARD ALAIN R; WILLAND NICOLAS,期刊：Journal of Medicinal Chemistry, 页码：68-83 , 文章类型： Article，,卷期：2012年55-1] Mycobacterial transcriptional repressor EthR controls the expression of EthA, the bacterial monooxygenase activating ethionamide, and is thus largely responsible for the low sensitivity of the human pathogen Mycobacteriu... Conicasterol E, a Small Heterodimer Partner Sparing Farnesoid X Receptor Modulator Endowed with a Pregnane X Receptor Agonistic Activity, from the Marine Sponge Theonella swinhoei [作者：SEPE VALENTINA; UMMARINO RAFFAELLA; DAURIA MARIA VALERIA; CHINI MARIA GIOVANNA; BIFULCO GIUSEPPE; RENGA BARBARA; DAMORE CLAUDIO; DEBITUS CECILE; FIORUCCI STEFANO; ZAMPELLA ANGELA,期刊：Journal of Medicinal Chemistry, 页码：84-93 , 文章类型： Article，,卷期：2012年55-1] We report the isolation and pharmacological characterization of conicasterol E isolated from the marine sponge Theonella swinhoei. Pharmacological characterization of this steroid in comparison to CDCA, a natural FXR lig... Myelin Imaging Compound (MIC) Enhanced Magnetic Resonance Imaging of Myelination [作者：FRULLANO LUCA; ZHU JUNQING; WANG CHANGNING; WU CHUNYING; MILLER ROBERT H; WANG YANMING,期刊：Journal of Medicinal Chemistry, 页码：94-105 , 文章类型： Article，,卷期：2012年55-1] The vertebrate nervous system is characterized by myelination, a fundamental biological process that protects the axons and facilitates electric pulse transduction. Damage to myelin is considered a major effect of autoin...