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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63条记录   Thiophene Bioisosteres of Spirocyclic sigma Receptor Ligands: Relationships between Substitution Pattern and sigma Receptor Affinity [作者：OBERDORF CHRISTOPH; SCHEPMANN DIRK; MIGUEL VELA JOSE; BUSCHMANN HELMUT; HOLENZ JOERG; WUENSCH BERNHARD,期刊：Journal of Medicinal Chemistry, 页码：5350-5360 , 文章类型： Article，,卷期：2012年55-11] On the basis of the 6',7'-dihydrospiro-[piperidine-4,4'-thieno[3,2-c]pyran] framework, a series of more than 30 sigma ligands with versatile substituents in 1-, 2'-, and 6'-position has been synthesized and pharmacologic... Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation [作者：SCOTT JAMES S; BIRCH ALAN M; BROCKLEHURST KATY J; BROO ANDERS; BROWN HAYLEY S; BUTLIN ROGER J; CLARKE DAVID S; DAVIDSSON OJVIND; ERTAN ANNE; GOLDBERG KRISTIN; GROOMBRIDGE SAM D; HUDSON JULIAN A; LABER DAVID; LEACH ANDREW G; MACFAUL PHILIP A; MCKERRECHER DARREN; PICKUP ADRIAN; SCHOFIELD PAUL; SVENSSON PER H; SOERME PERNILLA; TEAGUE JOANNE,期刊：Journal of Medicinal Chemistry, 页码：5361-5379 , 文章类型： Article，,卷期：2012年55-11] G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward discovering agonists of GPR119, we here... Water-Soluble Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as Human A(3) Adenosine Receptor Antagonists [作者：BARALDI PIER GIOVANNI; SAPONARO GIULIA; ROMAGNOLI ROMEO; TABRIZI MOJGAN AGHAZADEH; BARALDI STEFANIA; MOORMAN ALLAN R; COSCONATI SANDRO; DI MARO SALVATORE; MARINELLI LUCIANA; GESSI STEFANIA; MERIGHI STEFANIA; VARANI KATIA; BOREA PIER ANDREA; PRETI DELIA,期刊：Journal of Medicinal Chemistry, 页码：5380-5390 , 文章类型： Article，,卷期：2012年55-11] A relevant problem of the pyrazolo[4,3-e]-[1,2,4]triazolo[1,5-c]pyrimidine nucleus, an attractive scaffold for the preparation of adenosine receptor antagonists, is the low water solubility. We originally functionalized ... Design, Synthesis, and Pharmacological Characterization of Indol-3-ylacetamides, Indol-3-yloxoacetamides, and Indol-3-ylcarboxamides: Potent and Selective CB2 Cannabinoid Receptor Inverse Agonists [作者：PASQUINI SERENA; MUGNAINI CLAUDIA; LIGRESTI ALESSIA; TAFI ANDREA; BROGI SIMONE; FALCIANI CHIARA; PEDANI VALENTINA; PESCO NICOLO; GUIDA FRANCESCA; LUONGO LIVIO; VARANI KATIA; BOREA PIER ANDREA; MAIONE SABATINO; DI MARZO VINCENZO; CORELLI FEDERICO,期刊：Journal of Medicinal Chemistry, 页码：5391-5402 , 文章类型： Article，,卷期：2012年55-11] In our search for new cannabinoid receptor modulators, we describe herein the design and synthesis of three sets of indole-based ligands characterized by an acetamide, oxalylamide, or carboxamide chain, respectively. Mos... Structure-Activity Relationship Study of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro -4H- chromene-3-carbonitrile (UCPH-101) and Absolute Configurational Assignment Using Infrared and Vibrational Circular Dichroism Spectroscopy in Combination with ab Initio Hartree-Fock Calculations [作者：HUYNH TRI H V; SHIM IRENE; BOHR HENRIK; ABRAHAMSEN BJARKE; NIELSEN BIRGITTE; JENSEN ANDERS A; BUNCH LENNART,期刊：Journal of Medicinal Chemistry, 页码：5403-5412 , 文章类型： Article，,卷期：2012年55-11] The excitatory amino acid transporters (EAATs) play essential roles in regulating the synaptic concentration of the neurotransmitter glutamate in the mammalian central nervous system. To date, five subtypes have been ide... Antitumor Agents. 293. Nontoxic Dimethyl-4,4 '-dimethoxy-5,6,5 ',6 '-dimethylenedioxybiphenyl-2,2 '-dicarboxylate (DDB) Analogues Chennosensitlize Multidrug-Resistant Cancer Cells to Clinical Anticancer Drugs [作者：HUNG HSINYI; OHKOSHI EMIKA; GOTO MASUO; BASTOW KENNETH F; NAKAGAWAGOTO KYOKO; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：5413-5424 , 文章类型： Article，,卷期：2012年55-11] Novel dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybipheny1-2,2'-dicarboxylate (DDB) analogues were designed and synthesized to improve their chemo-sensitizing action on KBvin (vincristine-resistant nasopharyngeal c... Characterization and Solubilization of Pyrrole-Imidazole Polyamide Aggregates [作者：HARGROVE AMANDA E; RASKATOV JEVGENIJ A; MEIER JORDAN L; MONTGOMERY DAVID C; DERVAN PETER B,期刊：Journal of Medicinal Chemistry, 页码：5425-5432 , 文章类型： Article，,卷期：2012年55-11] To optimize the biological activity of pyrrole imidazole polyamide DNA-binding molecules, we characterized the aggregation propensity of these compounds through dynamic light scattering and fractional solubility analysis... Discovery and Optimization of a Series of 2-Aryl-4-Amino-5-(3 ',4 ',5 '-trimethoxybenzoyl)Thiazoles as Novel Anticancer Agents [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; PORCU ELENA; BASSO GIUSEPPE; VIOLA GIAMPIETRO,期刊：Journal of Medicinal Chemistry, 页码：5433-5445 , 文章类型： Article，,卷期：2012年55-11] A new series of tubulin polymerization inhibitors based on the 2-aryl/heteroaryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole scaffold was synthesized and evaluated for growth inhibition activity on a panel of cancer c... A Zinc(II) Phthalocyanine Conjugated with an Oxaliplatin Derivative for Dual Chemo- and Photodynamic Therapy [作者：LAU JANET T F; LO PUICHI; FONG WINGPING; NG DENNIS K P,期刊：Journal of Medicinal Chemistry, 页码：5446-5454 , 文章类型： Article，,卷期：2012年55-11] A novel zinc(II) phthalocyanine substituted with an oxaliplatin derivative via a triethylene glycol linker has been synthesized. The two components work in a cooperative manner in the antitumor action. The conjugate show... Structure-Activity Relationship and Mode of Action of N-(6-Ferrocenyl-2-naphthoyl) Dipeptide Ethyl Esters: Novel Organometallic Anticancer Compounds [作者：MOONEY AINE; TIEDT RACHEL; MAGHOUB THAMIR; ODONOVAN NORMA; CROWN JOHN; WHITE BLANAID; KENNY PETER T M,期刊：Journal of Medicinal Chemistry, 页码：5455-5466 , 文章类型： Article，,卷期：2012年55-11] In this article, we report the findings of a comprehensive structure-activity relationship study of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters, in which novel analogues were designed, synthesized, and evaluated ... Discovery of a Novel Series of Potent and Orally Bioavailable Phosphoinositide 3-Kinase gamma Inhibitors [作者：LEAHY JAMES W; BUHR CHRIS A; JOHNSON HENRY W B; KIM BYUNG GYU; BAIK TAEGON; CANNOY JONAH; FORSYTH TIMOTHY P; JEONG JOON WON; LEE MATTHEW S; MA SUNGHOON; NOSON KEVIN; WANG LONGCHENG; WILLIAMS MATTHEW; NUSS JOHN M; BROOKS ERIC; FOSTER PAUL; GOON LEANNE; HEALD NATHAN; HOLST CHARLES; JAEGER CHRISTOPHER; LAM SCOTT; LOUGHEED JULIE; LAM NGUYEN; PLONOWSKI ARTHUR; SONG JOANNE; STOUT THOMAS; WU XIANG; YAKES MICHAEL F; YU PEIWEN; ZHANG WENTAO; LAMB PETER; RAEBER OLIVIA,期刊：Journal of Medicinal Chemistry, 页码：5467-5482 , 文章类型： Article，,卷期：2012年55-11] The phosphoinositide 3-kinases (PI3Ks) have been linked to an extraordinarily diversified group of cellular functions making these enzymes compelling targets for the treatment of disease. A large body of evidence has lin... Discovery of Highly Potent Human Deoxyuridine Triphosphatase Inhibitors Based on the Conformation Restriction Strategy [作者：MIYAHARA SEIJI; MIYAKOSHI HITOSHI; YOKOGAWA TATSUSHI; CHONG KHOON TEE; TAGUCHI JUNKO; MUTO TOSHIHARU; ENDOH KANJI; YANO WAKAKO; WAKASA TAKESHI; UENO HIROYUKI; TAKAO YAYOI; AKIO FUJIOKA; HASHIMOTO AKIHIRO; ITOU KENJIROU; YAMAMURA KEISUKE; NOMURA MAKOTO; NAGASAWA HIDEKO; SHUTO SATOSHI; FUKUOKA MASAYOSHI,期刊：Journal of Medicinal Chemistry, 页码：5483-5496 , 文章类型： Article，,卷期：2012年55-11] Human deoxyuridine triphosphatase (dUTPase) inhibition is a promising approach to enhance the efficacy of thymidylate synthase (TS) inhibitor based chemotherapy. In this study, we describe the discovery of a novel class ... 6-(Methylamino)hexane-1,2,3,4,5-pentanol 4-(((1S,2S)-1-Hydroxy-2,3-dihydro-1H,1 ' H-[2,2-biinden]-2-yl)methyl)benzoate (PH46A): A Novel Small Molecule With Efficacy In Murine Models Of Colitis [作者：FRANKISH NEIL; SHERIDAN HELEN,期刊：Journal of Medicinal Chemistry, 页码：5497-5505 , 文章类型： Article，,卷期：2012年55-11] The indane skeleton is found naturally and in several therapeutic molecules in medicinal chemistry. During our work on the anti-inflammatory activity of naturally occurring and synthetic indanes, we have synthesized a no... Metallocene-Based Inhibitors of Cancer-Associated Carbonic Anhydrase Enzymes IX and XII [作者：SALMON ADAM J; WILIAMS MICHAEL L; WU QUOC K; MORIZZI JULIA; GREGG DANIEL; CHARMAN SUSAN A; VULLO DANIELA; SUPURAN CLAUDIU T; POULSEN SALLYANN,期刊：Journal of Medicinal Chemistry, 页码：5506-5517 , 文章类型： Article，,卷期：2012年55-11] In this study, 20 metallocene-based compounds comprising extensive structural diversity were synthesized and evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. These compounds proved moderate to good CA inhibit... Gold(I) Carbene Complexes Causing Thioredoxin 1 and Thioredoxin 2 Oxidation as Potential Anticancer Agents [作者：SCHUH ESTHER; PFLUEGER CAROLIN; CITTA ANNA; FOLDA ALESSANDRA; RIGOBELLO MARIA PIA; BINDOLI ALBERTO; CASINI ANGELA; MOHR FABIAN,期刊：Journal of Medicinal Chemistry, 页码：5518-5528 , 文章类型： Article，,卷期：2012年55-11] Gold(I) complexes with 1,3-substituted imidazole-2-ylidene and benzimidazole-2-ylidene ligands of the type NHC-Au-L (NHC = N-heterocyclic carbene L = Cl or 2-mercapto-pyrimidine) have been synthesized and structurally ch... Protein-Protein Interactions: Inhibition of Mammalian Carbonic Anhydrases I-XV by the Murine Inhibitor of Carbonic Anhydrase and Other Members of the Transferrin Family [作者：DURDAGI SERDAR; VULLO DANIELA; PAN PEIWEN; KAHKONEN NIKLAS; MAATTA JUHA A; HYTONEN VESA P; SCOZZAFAVA ANDREA; PARKKILA SEPPO; SUPURAN CLAUDIU T,期刊：Journal of Medicinal Chemistry, 页码：5529-5535 , 文章类型： Article，,卷期：2012年55-11] The marine inhibitor of carbonic anhydrase (mICA), a member of the transferrin (TF) superfamily of proteins, together with human holo- and apoTF and lactoferrin (LF) were assessed as inhibitors of all catalytically activ...