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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33条记录   Gd Complexes of DO3A-(Biphenyl-2,2 '-bisamides) Conjugates as MRI Blood-Pool Contrast Agents [作者：JUNG KIHYE; KIM HEEKYUNG; PARK JIAE; NAM KI SOO; LEE GANG HO; CHANG YONGMIN; KIM TAEJEONG,期刊：ACS Medicinal Chemistry Letters, 页码：1003-1007 , 文章类型： Article，,卷期：2012年3-12] We report the synthesis of DO3A derivatives of 2,2'-diaminobiphenyl (1a,b) and their Gd complexes of the type [Gd(1)(H2O)]center dot xH(2)O (2a,b) for use as new MRI blood-pool contrast agents (BPCAs) that provide strong... Small Molecule Ligands for Active Targeting of TrkC-Expressing Tumor Cells [作者：KO EUNHWA; KAMKAEW ANYANEE; BURGESS KEVIN,期刊：ACS Medicinal Chemistry Letters, 页码：1008-1012 , 文章类型： Article，,卷期：2012年3-12] A small molecule motif was used in "active targeting" to deliver cytotoxic substances into tumor cells that express the TrkC receptor. Underlying this study was the hypothesis that internalization of targeted conjugates ... Desmethyl Macrolides: Synthesis and Evaluation of 4,8-Didesmethyl Telithromycin [作者：WAGH BHARAT; PAUL TAPAS; GLASSFORD IAN; DEBROSSE CHARLES; KLEPACKI DOROTA; SMALL MEAGAN C; MACKERELL ALEXANDER D JR; ANDRADE RODRIGO B,期刊：ACS Medicinal Chemistry Letters, 页码：1013-1018 , 文章类型： Article，,卷期：2012年3-12] There is an urgent need for novel sources of antibiotics to address the incessant and inevitable onset of bacterial resistance. To this end, we have initiated a structure-based drug design program that features a desmeth... Strain-Promoted Catalyst-Free Click Chemistry for Rapid Construction of Cu-64-Labeled PET Imaging Probes [作者：CHEN KAI; WANG XINLU; LIN WEIYU; SHEN CLIFTON KF; YAP LIPENG; HUGHES LINDSEY D; CONTI PETER S,期刊：ACS Medicinal Chemistry Letters, 页码：1019-1023 , 文章类型： Article，,卷期：2012年3-12] A rapid, efficient, and catalyst-free click chemistry method for the construction of Cu-64-labeled PET imaging probes was reported based on the strain-promoted aza-dibenzocyclooctyne ligation. This new method was exempli... SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease [作者：WITYAK JOHN; PRIME MICHAEL E; BROOKFIELD FREDERICK A; COURTNEY STEPHEN M; ERFAN SAYEH; JOHNSEN SIW; JOHNSON PETER D; LI MARIE; MARSTON RICHARD W; REED LAURA; VAIDYA DARSHAN; SCHAERTL SABINE; PEDRETDUNN ANNA; BECONI MARIA; MACDONALD DOUGLAS; MUNOZSANJUAN IGNACIO; DOMINGUEZ CELIA,期刊：ACS Medicinal Chemistry Letters, 页码：1024-1028 , 文章类型： Article，,卷期：2012年3-12] We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and bet... 1,4-Naphthoquinone Cations as Antiplasmodial Agents: Hydroxy-, Acyloxy-, and Alkoxy-Substituted Analogues [作者：LU XIAO; ALTHARAWI ALI; GUT JIRI; ROSENTHAL PHILIP J; LONG TIMOTHY E,期刊：ACS Medicinal Chemistry Letters, 页码：1029-1033 , 文章类型： Article，,卷期：2012年3-12] Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite grow... A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells [作者：WEIWER MICHEL; SPOONAMORE JAMES; WEI JINGQIANG; GUICHARD BORIS; ROSS NATHAN T; MASSON KRISTINA; SILKWORTH WHITNEY; DANDAPANI SIVARAMAN; PALMER MICHELLE; SCHERER CHRISTINA A; STERN ANDREW M; SCHREIBER STUART L; MUNOZ BENITO,期刊：ACS Medicinal Chemistry Letters, 页码：1034-1038 , 文章类型： Article，,卷期：2012年3-12] The KRAS oncogene is found in up to 30% of all human tumors. In 2009, RNAi experiments revealed that lowering mRNA levels of a transcript encoding the serine/threonine kinase STK33 was selectively toxic to KRAS-dependent... Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate [作者：ZHANG XUQING; HOU CUIFEN; HUFNAGEL HEATHER; SINGER MONICA; OPAS EVAN; MCKENNEY SANDRA; JOHNSON DANA; SUI ZHIHUA,期刊：ACS Medicinal Chemistry Letters, 页码：1039-1044 , 文章类型： Article，,卷期：2012年3-12] We have discovered a novel series of 4-azetidiny1-1-aryl-cyclohexanes as CCR2 antagonists. Divergent SAR studies on hCCR2 and hERG activities led to the discovery of compound 8d, which displayed good hCCR2 binding affini... A New Approach to Explore the Binding Space of Polysaccharide-Based Ligands: Selectin Antagonists [作者：CALOSSO MICKAEL; CHARPENTIER DANIEL; VAILLANCOURT MARC; BENCHEQROUN MOHAMMED; STPIERRE GABRIELLE; WILKES BRIAN C; GUINDON YVAN,期刊：ACS Medicinal Chemistry Letters, 页码：1045-1049 , 文章类型： Article，,卷期：2012年3-12] The discovery of molecules that interfere with the binding of a ligand to a receptor remains a topic of great interest in medicinal chemistry. Herein, we report that a monosaccharide unit of a polysaccharide ligand can b... Inhibitors of the NAD(+)-Dependent Protein Desuccinylase and Demalonylase Sirt5 [作者：MAURER BENJAMIN; RUMPF TOBIAS; SCHARFE MICHAEL; STOLFA DIANA A; SCHMITT MARTIN L; HE WENJUAN; VERDIN ERIC; SIPPL WOLFGANG; JUNG MANFRED,期刊：ACS Medicinal Chemistry Letters, 页码：1050-1053 , 文章类型： Article，,卷期：2012年3-12] NAD(+)-dependent histone deacetylases (sirtuins) play important roles in epigenetic regulation but also through nonhistone substrates for other key cellular events and have been linked to the pathogenesis of cancer, neur... From alpha 4 beta 2 Nicotinic Ligands to the Discovery of sigma 1 Receptor Ligands: Pharmacophore Analysis and Rational Design [作者：YU LIFANG; ZHANG HANKUN; GUNOSEWOYO HENDRA; KOZIKOWSKI ALAN P,期刊：ACS Medicinal Chemistry Letters, 页码：1054-1058 , 文章类型： Article，,卷期：2012年3-12] Comparative analyses of the pharmacophoric elements required for sigma 1 and nicotinic ligands led to the identification of a potent and selective sigma 1 ligand (15). Compound 15 displayed high selectivity for the sigma... Structure-Based Design of Potent and Selective CK1 gamma Inhibitors [作者：HUANG HONGBING; ACQUAVIVA LISA; BERRY VIRGINIA; BREGMAN HOWARD; CHAKKA NAGASREE; OCONNOR ANNE; DIMAURO ERIN F; DOVEY JENNIFER; EPSTEIN OLEG; GRUBINSKA BARBARA; GOLDSTEIN JON; GUNAYDIN HAKAN; HUA ZIHAO; HUANG XIN; HUANG LIYUE; HUMAN JASON; LONG ALEX; NEWCOMB JOHN; PATEL VINOD F; SAFFRAN DOUG; SERAFINO RANDY; SCHNEIDER STEVE; STRATHDEE CRAIG; TANG JIN; TURCI SUSAN; WHITE RYAN; YU VIOLETA; ZHAO HUILIN; WILSON CINDY; MARTIN MATTHEW W,期刊：ACS Medicinal Chemistry Letters, 页码：1059-1064 , 文章类型： Article，,卷期：2012年3-12] Aberrant activation of the Wnt pathway is believed to drive the development and growth of some cancers. The central role of CK1 gamma in Wnt signal transduction makes it an attractive target for the treatment of Wnt-path... Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds [作者：TORRES EVA; FERNANDEZ ROSER; MIQUET STEPHANIE; FONTBARDIA MERCE; VANDERLINDEN EVELIEN; NAESENS LIEVE; VAZQUEZ SANTIAGO,期刊：ACS Medicinal Chemistry Letters, 页码：1065-1069 , 文章类型： Article，,卷期：2012年3-12] The synthesis of several 2,2-dialkyladamantyl-1-amines through the combination of a Ritter reaction with a Wagner-Meerwein rearrangement from noradamantane alcohols is reported. Several of the novel amines displayed low ... Identification of Amides as Carboxylic Acid Surrogates for Quinolizidinone-Based M-1 Positive Allosteric Modulators [作者：KUDUK SCOTT D; CHANG RONALD K; GRESHOCK THOMAS J; RAY WILLIAM J; MA LEI; WITTMANN MARION; SEAGER MATTHEW A; KOEPLINGER KENNETH A; THOMPSON CHARLES D; HARTMAN GEORGE D; BILODEAU MARK T,期刊：ACS Medicinal Chemistry Letters, 页码：1070-1074 , 文章类型： Article，,卷期：2012年3-12] Selective activation of the M-1 muscarinic receptor via positive allosteric modulation represents an approach to treat the cognitive decline in patients with Alzheimer's disease. A series of amides were examined as a rep... Synthesis and Antiproliferative Activities of Ottelione A Analogues [作者：CHANG TSAIYUAN; TU YUNPENG; WEI WINYIN; CHEN HSIANG YU; CHEN CHIHSHANG; LEE YINGSHUAN E; HUANG JIANNJYH; SHA CHINKANG,期刊：ACS Medicinal Chemistry Letters, 页码：1075-1080 , 文章类型： Article，,卷期：2012年3-12] Through the syntheses of its C-1 desvinyl, C-7 methylene, C-7 exocyclic ethylidene, and various C-3 phenylmethyl analogues, the structure activity relationship of antimitotic ottelione A (4) against tubulin and various c... D-Amino Acid-Based Protein Arginine Deiminase Inhibitors: Synthesis, Pharmacokinetics, and in Cellulo Efficacy [作者：BICKER KEVIN L; ANGUISH LYNNE; CHUMANEVICH ALEXANDER A; CAMERON MICHAEL D; CUI XIANGLI; WITALISON ERIN; SUBRAMANIAN VENKATARAMAN; ZHANG XUESEN; CHUMANEVICH ALENA P; HOFSETH LORNE J; COONROD SCOTT A; THOMPSON PAUL R,期刊：ACS Medicinal Chemistry Letters, 页码：1081-1085 , 文章类型： Article，,卷期：2012年3-12] The protein arginine deiminases (PADs) are known to play a crucial role in the onset and progression of multiple inflammatory diseases, including rheumatoid arthritis, inflammatory bowel disease, and cancer. However, it ...