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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49条记录   Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors [作者：MENG WEI; BRIGANCE ROBERT P; CHAO HANNGUANG J; FURA ABERRA; HARRITY THOMAS; MARCINKEVICIENE JOVITA; OCONNOR STEPHEN P; TAMURA JAMES K; XIE DIANLIN; ZHANG YAQUN; KLEI HERBERT E; KISH KEVIN; WEIGELT CAROLYN A; TURDI HUJI; WANG AIYING; ZAHLER ROBERT; KIRBY MARK S; HAMANN LAWRENCE G,期刊：Journal of Medicinal Chemistry, 页码：5620-5628 , 文章类型： Article，,卷期：2010年53-15] Continued structure activity relationship (SA R) exploration within our previously disclosed azolopyrimidine containing dipeptidyl peptidase-4 (DPP4) inhibitors led us to focus on an imidazolopyrimidine series in particu... Design, Synthesis, Enzyme-Inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors [作者：HAMADA SHOHEI; SUZUKI TAKAYOSHI; MINO KOSHIKI; KOSEK KOICHI; OEHME FELIX; FLAMME INGO; OZASA HIROKI; ITOH YUKIHIRO; OGASAWARA DAISUKE; KOMAARASHI HARUKA; KATO AIKO; TSUMOTO HIROKI; NAKAGAWA HIDEHIKO; HASEGAWA MAKOTO; SASAKI RYUZO; MIZUKAMI TAMIO; MIYATA NAOKI,期刊：Journal of Medicinal Chemistry, 页码：5629-5638 , 文章类型： Article，,卷期：2010年53-15] Selective inhibitors of Jumonji domain-containing protein (JMJD) histone demethylases are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs. On the basis of the crys... Novel Hinge Binder Improves Activity and Pharmacokinetic Properties of BRAF Inhibitors [作者：ZAMBON ALFONSO; MENARD DELPHINE; SUIJKERBUIJK BART M J M; NICULESCUDUVAZ ION; WHITTAKER STEVEN; NICULESCUDUVAZ DAN; NOURRY ARNAUD; DAVIES LAWRENCE; MANNE HELEN A; LOPES FILIPA; PREECE NATASHA; HEDLEY DOUGLAS; OGILVIE LESLEY M; KIRK RUTH; MARAIS RICHARD; SPRINGER CAROLINE J,期刊：Journal of Medicinal Chemistry, 页码：5639-5655 , 文章类型： Article，,卷期：2010年53-15] Mutated BRAF serine/threonine kinase is implicated in several types of cancer, with particularly high frequency in melanoma and colorectal carcinoma. We recently reported on the development of BRAF inhibitors based on a ... Heteroadamantyl Cannabinoids [作者：DIXON DARRYL D; SETHUMADHAVAN DIVAKARAMENON; BENNECHE TORE; BANAAG APRIL R; TIUS MARCUS A; THAKUR GANESH A; BOWMAN ANNA; WOOD JODIANNE T; MAKRIYANNIS ALEXANDROS,期刊：Journal of Medicinal Chemistry, 页码：5656-5666 , 文章类型： Article，,卷期：2010年53-15] The aliphatic side chain plays a pivotal role in determining the cannabinergic potency of tricyclic classical cannabinoids. We have synthesized a series of analogues in which the C3 position is substituted either directl... m-Azipropofol (AziPm) a Photoactive Analogue of the Intravenous General Anesthetic Propofol [作者：HALL MICHAEL A; XI JIN; LOR CHONG; DAI SHUIPING; PEARCE ROBERT; DAILEY WILLIAM P; ECKENHOFF RODERIC G,期刊：Journal of Medicinal Chemistry, 页码：5667-5675 , 文章类型： Article，,卷期：2010年53-15] Propofol is the most commonly used sedative-hypnotic drug for noxious procedures, yet the molecular targets underlying either its beneficial or toxic effects remain uncertain. In order to determine targets and thereby me... Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron and Fluorastrol [作者：KAAN HUNG YI KRISTAL; ULAGANATHAN VENKATASUBRAMANIAN; RATH OLIVER; PROKOPCOVA HANA; DALLINGER DORIS; KAPPE C OLIVER; KOZIELSKI FRANK,期刊：Journal of Medicinal Chemistry, 页码：5676-5683 , 文章类型： Article，,卷期：2010年53-15] Human kinesin Eg5, which plays an essential role in mitosis by establishing the bipolar spindle, has proven to be an interesting drug target for the development of cancer chemotherapeutics. Here, we report the crystal st... Crystal Structure-Based Selective Targeting of the Pyridoxal 5 '-Phosphate Dependent Enzyme Kynurenine Aminotransferase II for Cognitive Enhancement [作者：ROSSI FRANCA; VALENTINA CASAZZA; GARAVAGLIA SILVIA; SATHYASAIKUMAR KORRAPATI V; SCHWARCZ ROBERT; KOJIMA SHINICHI; OKUWAKI KEISUKE; ONO SHINICHIRO; KAJII YASUSHI; RIZZI MENICO,期刊：Journal of Medicinal Chemistry, 页码：5684-5689 , 文章类型： Article，,卷期：2010年53-15] Fluctuations in the brain levels of the neuromodulator kynurenic acid may control cognitive processes and play a causative role in several catastrophic brain diseases. Elimination of the pyridoxal 5'-phosphate dependent ... Design and Synthesis of C-2 Substituted Thiazolo and Dihydrothiazolo Ring-Fused 2-Pyridones: Pilicides with Increased Antivirulence Activity [作者：CHORELL ERIK; PINKNER JEROME S; PHAN GILLES; EDVINSSON SOFIE; BUELENS FLORIS; REMAUT HAN; WAKSMAN GABRIEL; HULTGREN SCOTT J; ALMQVIST FREDRIK,期刊：Journal of Medicinal Chemistry, 页码：5690-5695 , 文章类型： Article，,卷期：2010年53-15] Pilicides block pili formation by binding to pilus chaperones and blocking their function in the chaperone/usher pathway in E. coli. Various C-2 substituents were introduced on the pilicide scaffold by design and synthet... Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine(2A) Receptor Antagonists for the Treatment of Insomnia [作者：XIONG YIFENG; ULLMAN BRETT; CHOI JINSUN KAROLINE; CHERRIER MARTIN; STRAHPLEYNET SONJA; DECAIRE MARC; DOSA PETER I; FEICHTINGER KONRAD; TEEGARDEN BRADLEY R; FRAZER JOHN M; YOON WOO H; SHAN YUN; WHELAN KEVIN; HAUSER ERIN K; GROTTICK ANDREW J; SEMPLE GRAEME; ALSHAMMA HUSSIEN,期刊：Journal of Medicinal Chemistry, 页码：5696-5706 , 文章类型： Article，,卷期：2010年53-15] Recent developments in sleep research suggest that antagonism of the serotonin 5-HT2A receptor may improve sleep maintenance insomnia. We herein report the discovery of a series of potent and selective serotonin 5-HT2A r... Scaffold Hopping Using Two-Dimensional Fingerprints: True Potential, Black Magic, or a Hopeless Endeavor? Guidelines for Virtual Screening [作者：VOGT MARTIN; STUMPFE DAGMAR; GEPPERT HANNA; BAJORATH JUERGEN,期刊：Journal of Medicinal Chemistry, 页码：5707-5715 , 文章类型： Article，,卷期：2010年53-15] The scaffold hopping potential of popular 2D fingerprints has been thoroughly investigated. We have found that these types of fingerprints have at least limited scaffold hopping ability including early enrichment of smal... The Structure-Activity Relationship of the 3-Oxy Site in the Anticonvulsant (R)-N-Benzyl 2-Acetamido-3-methoxypropionamide [作者：MORIEUX PIERRE; SALOME CHRISTOPHE; PARK KI DUK; STABLES JAMES P; KOHN HAROLD,期刊：Journal of Medicinal Chemistry, 页码：5716-5726 , 文章类型： Article，,卷期：2010年53-15] Lacosamide ((R)-N-benzyl 2-acetamido-3-methoxypropionamide, (R)-1) is a low molecular weight anticonvulsant recently introduced in the United States and Europe for adjuvant treatment of partial-onset seizures in adults. ... Tetrahydroisoquinoline Derivatives As Highly Selective and Potent Rho Kinase Inhibitors [作者：FANG XINGANG; YIN YAN; CHEN YEN TING; YAO LEI; WANG BO; CAMERON MICHAEL D; LIN LI; KHAN SUSAN; RUIZ CLAUDIA; SCHROETER THOMAS; GRANT WAYNE; WEISER AMIEE; POCAS JENNIFER; PACHORI ALOK; SCHUERER STEPHAN; LOGRASSO PHILIP; FENG YANGBO,期刊：Journal of Medicinal Chemistry, 页码：5727-5737 , 文章类型： Article，,卷期：2010年53-15] Rho kinase (ROCK) is a promising drug target for the treatment of many diseases including hypertension, multiple sclerosis, cancer, and glaucoma. The structure-activity relationships (SAR) around a series of tetrahydrois... Synthesis and Biological Characterization of Novel Charge-Deficient Spermine Analogues [作者：WEISELL JANNE; HYVONEN MERVI T; HAKKINEN MERJA R; GRIGORENKO NIKOLAY A; PIETILA MARKO; LAMPINEN ANITA; KOCHETKOV SERGEY N; ALHONEN LEENA; VEPSALAINEN JOUKO; KEINANEN TUOMO A; KHOMUTOV ALEX R,期刊：Journal of Medicinal Chemistry, 页码：5738-5748 , 文章类型： Article，,卷期：2010年53-15] Biogenic polyamines, spermidine and spermine, are positively charged at physiological pH. They are present in all cells and essential for their growth and viability. Here we synthesized three novel derivatives of the iso... Replacement of Imidazolyl by Pyridyl in Biphenylmethylenes Results in Selective CYP17 and Dual CYP17/CYP11B1 Inhibitors for the Treatment of Prostate Cancer [作者：HU QINGZHONG; JAGUSCH CARSTEN; HILLE ULRIKE E; HAUPENTHAL JOERG; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：5749-5758 , 文章类型： Article，,卷期：2010年53-15] Androgens are well-known to stimulate prostate cancer (PC) growth. Thus, blockade of androgen production in testes and adrenals by CYP17 inhibition is a promising strategy for the treatment of PC. Moreover, many PC patie... Novel Thiosemicarbazones of the ApT and DpT Series and Their Copper Complexes: Identification of Pronounced Redox Activity and Characterization of Their Antitumor Activity [作者：JANSSON PATRIC J; SHARPE PHILIP C; BERNHARDT PAUL V; RICHARDSON DES R,期刊：Journal of Medicinal Chemistry, 页码：5759-5769 , 文章类型： Article，,卷期：2010年53-15] The novel chelators 2-acetylpyridine-4,4-dimethyl-3-thiosemicarbazone (HAp44mT) and di-2-pyridyl-ketone-4,4-dimethyl-3-thiosemicarbazone (HDp44mT) have been examined to elucidate the structure activity relationships nece... Synthesis and Structure-Activity Relationships of N-(2-Oxo-3-oxetanyl)amides as N-Acylethanolamine-hydrolyzing Acid Amidase Inhibitors [作者：SOLORZANO CARLOS; ANTONIETTI FRANCESCA; DURANTI ANDREA; TONTINI ANDREA; RIVARA SILVIA; LODOLA ALESSIO; VACONDIO FEDERICA; TARZIA GIORGIO; PIOMELLI DANIELE; MOR MARCO,期刊：Journal of Medicinal Chemistry, 页码：5770-5781 , 文章类型： Article，,卷期：2010年53-15] The fatty acid ethanolamides (FAEs) are a family of bioactive lipid mediators that include the endogenous agonist of peroxisome proliferator-activated receptor-alpha, palmitoylethanolamide (PEA). FAEs are hydrolyzed intr...