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38条记录   L-Aminoacyl-triazine Derivatives Are Isoform-Selective PI3K beta Inhibitors That Target Nonconserved Asp862 of PI3K beta [作者：PINSON JOANNE; ZHENG ZHAOHUA; MILLER MICHELLE S; CHALMERS DAVID K; JENNINGS IAN G; THOMPSON PHILIP E,期刊：ACS Medicinal Chemistry Letters, 页码：206-210 , 文章类型： Article，,卷期：2013年4-2] A series of aminoacyl-triazine derivatives based upon the pan-PI3K inhibitor ZSTK474 were identified as potent and isoform-selective inhibitors of PI3K beta. The compounds showed selectivity based upon stereochemistry wi... Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195 [作者：TONG YUNSONG; STEWART KENT D; FLORJANCIC ALAN S; HARLAN JOHN E; MERTA PHILIP J; PRZYTULINSKA MAGDALENA; SONI NIRUPAMA; SWINGER KERREN K; ZHU HAIZHONG; JOHNSON ERIC F; SHOEMAKER ALEXANDER R; PENNING THOMAS D,期刊：ACS Medicinal Chemistry Letters, 页码：211-215 , 文章类型： Article，,卷期：2013年4-2] To investigate the role played by the unique pre-DFG residue Val 195 of Cdc7 kinase on the potency of azaindole-chloropyridines (1), a series of novel analogues with various chloro replacements were synthesized and evalu... Gadolinium Complex of I-125/I-127-RGD-DOTA Conjugate as a Tumor-Targeting SPECT/MR Bimodal Imaging Probe [作者：PARK JIAE; KIM JUNG YOUNG; LEE YONG JIN; LEE WONHO; LIM SANG MOO; KIM TAEJEONG; YOO JEONGSOO; CHANG YONGMIN; KIM KYEONG MIN,期刊：ACS Medicinal Chemistry Letters, 页码：216-219 , 文章类型： Article，,卷期：2013年4-2] The work describes the synthesis and in vivo application of [Gd(L)(H2O)]center dot xH(2)O, where L is a (I-125/I-127-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (I-125/I-127-RGD)-DOTA... Novel Hybrid-Type Antimicrobial Agents Targeting the Switch Region of Bacterial RNA Polymerase [作者：YAKUSHIJI FUMIKA; MIYAMOTO YUKO; KUNOH YUKI; OKAMOTO REIKO; NAKAMINAMI HIDEMASA; YAMAZAKI YURI; NOGUCHI NORIHISA; HAYASHI YOSHIO,期刊：ACS Medicinal Chemistry Letters, 页码：220-224 , 文章类型： Article，,卷期：2013年4-2] The bacterial RNA polymerase (RNAP) is an ideal target for the development of antimicrobial agents against drug-resistant bacteria. Especially, the switch region within RNAP has been considered as an attractive binding s... A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases [作者：STADERINI MATTEO; AULIC SUZANA; BARTOLINI MANUELA; HOANG NGOC AI TRAN; GONZALEZRUIZ VICTOR; PEREZ DANIEL I; CABEZAS NIEVES; MARTINEZ ANA; ANTONIA MARTIN M; ANDRISANO VINCENZA; LEGNAME GIUSEPPE; CARLOS MENENDEZ J; BOLOGNESI MARIA LAURA,期刊：ACS Medicinal Chemistry Letters, 页码：225-229 , 文章类型： Article，,卷期：2013年4-2] (E)-6-Methyl-4'-amino-2-styrylquinoline (3) is a small molecule with the proper features to potentially diagnose, deliver therapy and monitor response to therapy in protein misfolding diseases. These features include com... [3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase beta Inhibitors [作者：YU HONGYI; MOORE MICHAEL L; ERHARD KARL; HARDWICKE MARY ANN; LIN HONG; LUENGO JUAN I; MCSURDYFREED JEANELLE; PLANT RAMONA; QU JUNYA; RAHA KAUSHIK; ROMINGER CYNTHIA M; SCHABER MICHAEL D; SPENGLER MICHAEL D; RIVERO RALPH A,期刊：ACS Medicinal Chemistry Letters, 页码：230-234 , 文章类型： Article，,卷期：2013年4-2] A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3K beta. The template afforded the opportunity to develop novel SAR for both the hinge-bind... Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with an Indole-Containing Cap Group [作者：ZHANG YINGJIE; YANG PENGHUI; CHOU C JAMES; LIU CHUNXI; WANG XUEJIAN; XU WENFANG,期刊：ACS Medicinal Chemistry Letters, 页码：235-238 , 文章类型： Article，,卷期：2013年4-2] A novel series of histone deacetylase inhibitors combining N-hydroxycinnamamide bioactive fragment and indole bioactive fragment was designed and synthesized. Several compounds (17c, 17g, 17h, 17j, and 17k) exhibited com... Inhibition of Ebola Virus Infection: Identification of Niemann-Pick C1 as the Target by Optimization of a Chemical Probe [作者：LEE KYUNGAE; REN TAO; COTE MARCELINE; GHOLAMREZA BERAHMAN; MISASI JOHN; BRUCHEZ ANNA; CUNNINGHAM JAMES,期刊：ACS Medicinal Chemistry Letters, 页码：239-243 , 文章类型： Article，,卷期：2013年4-2] A high-throughput screen identified adamantane dipeptide 1 as an inhibitor of Ebola virus (EboV) infection. Hit-to-lead optimization to determine the structure-activity relationship (SAR) identified the more potent EboV ... Discovery of Novel N-Substituted Oxindoles as Selective M-1 and M-4 Muscarinic Acetylcholine Receptors Partial Agonists [作者：SUMIYOSHI TAKAAKI; ENOMOTO TAKESHI; TAKAI KENTARO; TAKAHASHI YOKO; KONISHI YASUKO; URUNO YOSHIHARU; TOJO KENGO; SUWA ATSUSHI; MATSUDA HARUMI; NAKAKO TOMOKAZU; SAKAI MUTSUKO; KITAMURA ATSUSHI; UEMATSU YASUAKI; KIYOSHI AKIHIKO,期刊：ACS Medicinal Chemistry Letters, 页码：244-248 , 文章类型： Article，,卷期：2013年4-2] Activation of the M-1 and M-4 muscarinic acetylcholine receptors is thought to play an important role in improving the symptoms of schizophrenia. However, discovery of selective agonists for these receptors has been a ch... Interrogation of the Active Sites of Protein Arginine Deiminases (PAD1,-2, and-4) Using Designer Probes [作者：BELLO ANGELICA M; WASIEWSKI EWA; WEI LIANHU; MOSCARELLO MARIO A; KOTRA LAKSHMI P,期刊：ACS Medicinal Chemistry Letters, 页码：249-253 , 文章类型： Article，,卷期：2013年4-2] Protein arginine deiminases (PADs) are involved in a number of cellular pathways, and they catalyze the transformation of peptidyl arginine residue into a citrulline as part of post-translational modifications. To unders... Synthesis of Novel Analogs of Cabergoline: Improving Cardiovascular Safety by Removing 5-HT2B Receptor Agonism [作者：DOSA PETER I; WARD TIM; WALTERS MICHAEL A; KIM SUCK WON,期刊：ACS Medicinal Chemistry Letters, 页码：254-258 , 文章类型： Article，,卷期：2013年4-2] The dopamine agonist cabergoline has been used to treat prolactinomas, Parkinson's disease, Cushing's disease, and sexual dysfunction. However, its clinical use was severely curtailed when it was found that patients taki... Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors [作者：LIU JINJUN; HIGGINS BRIAN; JU GRACE; KOLINSKY KENNETH; LUK KINCHUN; PACKMAN KATHRYN; PIZZOLATO GIACOMO; REN YI; THAKKAR KSHITIJ; TOVAR CHRISTIAN; ZHANG ZHUMING; WOYKULICH PETER M,期刊：ACS Medicinal Chemistry Letters, 页码：259-263 , 文章类型： Article，,卷期：2013年4-2] A new series of 7,8-disubstituted pyrazolobenzodiazepines based on the lead compound 1 have been synthesized and evaluated for their effects on mitosis and angiogenesis. Described herein is the design, synthesis, SAR, an... Synthesis and Antimycobacterial Activity of 2,1 '-Dihydropyridomycins [作者：HORLACHER OLIVER P; HARTKOORN RUBEN C; COLE STEWART T; ALTMANN KARLHEINZ,期刊：ACS Medicinal Chemistry Letters, 页码：264-268 , 文章类型： Article，,卷期：2013年4-2] Dihydropyridomycins 2 and 3, which lack the characteristic enol ester moiety of the potent antimycobacterial natural product pyridomycin (1), have been prepared from L-Thr, R- and S-hydroxy isovaleric acid, and 3-pyridin... Bodilisant-A Novel Fluorescent, Highly Affine Histamine H-3 Receptor Ligand [作者：TOMASCH MIRIAM; SCHWED J STEPHAN; PAULKE ALEXANDER; STARK HOLGER,期刊：ACS Medicinal Chemistry Letters, 页码：269-273 , 文章类型： Article，,卷期：2013年4-2] A piperidine-based lead structure for the human histamine H-3 receptor (hH(3)R) was coupled with the BODIPY fluorophore and resulted in a strong green fluorescent (quantum yield, 0.92) hH(3)R ligand with affinity in the ... Probing the Binding Site of Abl Tyrosine Kinase Using in Situ Click Chemistry [作者：PERUZZOTTI CRISTINA; BORRELLI STELLA; VENTURA MICOL; PANTANO REBECCA; FUMAGALLI GAIA; CHRISTODOULOU MICHAEL S; MONTICELLI DAMIANO; LUZZANI MARCELLO; FALLACARA ANNA LUCIA; TINTORI CRISTINA; BOTTA MAURIZIO; PASSARELLA DANIELE,期刊：ACS Medicinal Chemistry Letters, 页码：274-277 , 文章类型： Article，,卷期：2013年4-2] Modern combinatorial chemistry is used to discover compounds with desired function by an alternative strategy, in which the biological target is directly involved in the choice of ligands assembled from a pool of smaller... Antimalarial and Structural Studies of Pyridine-Containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase [作者：XUE JIAN; DIAO JIASHENG; CAI GUOBIN; DENG LISHENG; ZHENG BAISONG; YAO YUAN; SONG YONGCHENG,期刊：ACS Medicinal Chemistry Letters, 页码：278-282 , 文章类型： Article，,卷期：2013年4-2] 1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) in the nonmevalonate isoprene biosynthesis pathway is a target for developing antimalarial drugs. Fosmidomycin, a potent DXR inhibitor, showed safety as well as effic...