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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37条记录   9-[2-(R)-(Phosphonomethoxy)propyl]-2,6-diaminopurine (R)-PMPDAP and its prodrugs: Optimized preparation, including identification of by-products formed, and antiviral evaluation in vitro [作者：KRECMEROVA MARCELA; JANSA PETR; DRACINSKY MARTIN; SAZELOVA PETRA; KASICKA VACLAV; NEYTS JOHAN; AUWERX JOERI; KISS ELEONORA; GORIS NESYA; STEPAN GEORGE; JANEBA ZLATKO,期刊：Bioorganic & Medicinal Chemistry, 页码：1199-1208 , 文章类型： Article，,卷期：2013年21-5] New large-scale synthetic approach to antiretroviral agent 9-[2-(R)-(phosphonomethoxy) propyl]-2,6-diaminopurine, (R)-PMPDAP, was developed. Reaction of (R)-propanediol carbonate with 2,6-diaminopurine afforded exclusive... Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay [作者：STELLA ALESSANDRO; VAN BELLE KRISTIEN; DE JONGHE STEVEN; LOUAT THIERRY; HERMAN JEAN; ROZENSKI JEF; WAER MARK; HERDEWIJN PIET,期刊：Bioorganic & Medicinal Chemistry, 页码：1209-1218 , 文章类型： Article，,卷期：2013年21-5] A series of novel pyrimidine analogues were synthesized and evaluated for immunosuppressive activity in the Mixed Lymphocyte Reaction assay, which is well-known as the in vitro model for in vivo rejection after organ tra... Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema [作者：INOUE TAKAYUKI; MORITA MASATAKA; TOJO TAKASHI; YOSHIHARA KOUSEI; NAGASHIMA AKIRA; MORITOMO AYAKO; OHKUBO MITSURU; MIYAKE HIROSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：1219-1233 , 文章类型： Article，,卷期：2013年21-5] Vascular adhesion protein-1 (VAP-1), an amine oxidase that is also known as a semicarbazide-sensitive amine oxidase (SSAO), is present in particularly high levels in human plasma, and is considered a potential therapeuti... The effect of absolute configuration on activity, subtype selectivity (M3/M2) of 3 alpha-acyloxy-6 beta-acetoxyltropane derivatives as muscarinic M3 receptor antagonists [作者：WANG ZHIPENG; LIU HUIZHONG; ZHU LIANG; HU YOUMIN; CUI YONGYAO; NIU YINYAO; LU YANG; CHEN HONGZHUAN,期刊：Bioorganic & Medicinal Chemistry, 页码：1234-1239 , 文章类型： Article，,卷期：2013年21-5] Both enantiomers of 3 alpha-acyloxy-6 beta-acetoxyltropane derivatives 1-4 were prepared respectively and underwent functional studies and radioreceptor binding assays. 6S Enantiomers showed obvious muscarinic M3, M2 ant... Selection of heptapeptides that bind helix 69 of bacterial 23S ribosomal RNA [作者：KAUR MONINDERPAL; RUPASINGHE CHAMILA N; KLOSI EDVIN; SPALLER MARK R; CHOW CHRISTINE S,期刊：Bioorganic & Medicinal Chemistry, 页码：1240-1247 , 文章类型： Article，,卷期：2013年21-5] Helix 69 of Escherichia coli 23S rRNA has important roles in specific steps of translation, such as subunit association, translocation, and ribosome recycling. An M13 phage library was used to identify peptide ligands wi... Synthesis and mechanistic studies of novel spin-labeled combretastatin derivatives as potential antineoplastic agents [作者：LIU YINGQIAN; LI XIAOJING; ZHAO CHUNYAN; NAN XIANG; TIAN JING; MORRISNATSCHKE SUSAN L; ZHANG ZHIJUN; YANG XIAOMING; YANG LIU; LI LINHAI; ZHOU XINGWEN; LEE KUOHSIUNG,期刊：Bioorganic & Medicinal Chemistry, 页码：1248-1256 , 文章类型： Article，,卷期：2013年21-5] Two series (14a-d and 21a-h) of novel spin-labeled combretastatin derivatives were synthesized and evaluated for cytotoxicity against four tumor cell lines (K562, SGC-7901, Hela and HepG-2). Simultaneously, a representat... Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands [作者：FUKAYA TAKAYUKI; KODO TORU; ISHIYAMA TAKEO; NISHIKAWA HIROYUKI; BABA SATOKO; MASUMOTO SHUJI,期刊：Bioorganic & Medicinal Chemistry, 页码：1257-1267 , 文章类型： Article，,卷期：2013年21-5] The 18 kDa translocator protein (TSPO) was identified as a discrete receptor for diazepam (1). Since TSPO in the central nervous system (CNS) is believed to regulate neurosteroids biosynthesis, selective TSPO ligands are... Retrospective group fusion similarity search based on eROCE evaluation metric [作者：AVRAM SORIN I; CRISAN LUMINITA; BORA ALINA; PACUREANU LILIANA M; AVRAM STEFANA; KURUNCZI LUDOVIC,期刊：Bioorganic & Medicinal Chemistry, 页码：1268-1278 , 文章类型： Article，,卷期：2013年21-5] In this study, a simple evaluation metric, denoted as eROCE was proposed to measure the early enrichment of predictive methods. We demonstrated the superior robustness of eROCE compared to other known metrics throughout ... Nebulosides A-B, novel triterpene saponins from under-ground parts of Gypsophila arrostii Guss. var. nebulosa [作者：ARSLAN IDRIS; CELIK ALI; MELZIG MATTHIAS F,期刊：Bioorganic & Medicinal Chemistry, 页码：1279-1283 , 文章类型： Article，,卷期：2013年21-5] A bioassay-guided phytochemical analysis of the triterpene saponins from under ground parts of Gypsophila arrostii var. nebulosa allowed the isolation of two triterpene saponins; nebuloside A, B based on gypsogenin and q... Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents [作者：NICULESCUDUVAZ DAN; NICULESCUDUVAZ ION; SUIJKERBUIJK BART M J M; MENARD DELPHINE; ZAMBON ALFONSO; DAVIES LAWRENCE; PONS JEANFRANCOIS; WHITTAKER STEVEN; MARAIS RICHARD; SPRINGER CAROLINE J,期刊：Bioorganic & Medicinal Chemistry, 页码：1284-1304 , 文章类型： Article，,卷期：2013年21-5] The RAS-RAF-MEK-ERK pathway is hyperactivated in 30% of human cancers. BRAF is a serine-threonine kinase, belonging to this pathway that is mutated with high frequency in human melanoma and other cancers thus BRAF is an ... Selective inhibition of glycosyltransferases by bivalent imidazolium salts [作者：GAO YIN; VLAHAKIS JASON Z; SZAREK WALTER A; BROCKHAUSEN INKA,期刊：Bioorganic & Medicinal Chemistry, 页码：1305-1311 , 文章类型： Article，,卷期：2013年21-5] Galactosyltransferases (GalTs) extend the glycan chains of mammalian glycoproteins by adding Gal to terminal GlcNAc residues, and thus build the scaffolds for biologically important glycan structures. We have shown that ... N-2-Trimethylacetyl substituted and unsubstituted-N-4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2 ,3-d]pyrimidine-2,4-diamines: Design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents [作者：GANGJEE ALEEM; NAMJOSHI OJAS A; YU JIANMING; IHNAT MICHAEL A; THORPE JESSICA E; BAILEYDOWNS LORA C,期刊：Bioorganic & Medicinal Chemistry, 页码：1312-1323 , 文章类型： Article，,卷期：2013年21-5] Six novel N-4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines and their N-2-trimethylacetyl substituted analogs were synthesized as receptor tyrosine kinase (RTK) inhibitors. A microwav... Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters [作者：COLABUFO NICOLA A; CONTINO MARIALESSANDRA; CANTORE MARIANGELA; CAPPARELLI ELENA; PERRONE MARIA GRAZIA; CASSANO GIUSEPPE; GASPARRE GIUSEPPE; LEOPOLDO MARCELLO; BERARDI FRANCESCO; PERRONE ROBERTO,期刊：Bioorganic & Medicinal Chemistry, 页码：1324-1332 , 文章类型： Article，,卷期：2013年21-5] Substituted naphthalenyl derivatives bearing oxazole, or thiazole or furyl heteronuclei have been carried out as bioisosters of aryl-oxazoles and -thiazoles derivatives previously reported in order to investigate the rol... Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase [作者：LI HUIYING; XUE FENGTIAN; KRAUS JAMES M II; JI HAITAO; LABBY KRISTIN JANSEN; MATAKA JAN; DELKER SILVIA L; MARTASEK PAVEL; ROMAN LINDA J; POULOS THOMAS L; SILVERMAN RICHARD B,期刊：Bioorganic & Medicinal Chemistry, 页码：1333-1343 , 文章类型： Article，,卷期：2013年21-5] Inhibitors of neuronal nitric oxide synthase have been proposed as therapeutics for the treatment of different types of neurological disorders. On the basis of a cis-3,4-pyrrolidine scaffold, a series of trans-cyclopropy... Evaluation of adamantane hydroxamates as botulinum neurotoxin inhibitors: Synthesis, crystallography, modeling, kinetic and cellular based studies [作者：SILHAR PETER; SILVAGGI NICHOLAS R; PELLETT SABINE; CAPKOVA KATERINA; JOHNSON ERIC A; ALLEN KAREN N; JANDA KIM D,期刊：Bioorganic & Medicinal Chemistry, 页码：1344-1348 , 文章类型： Article，,卷期：2013年21-5] Botulinum neurotoxins (BoNTs) are the most lethal biotoxins known to mankind and are responsible for the neuroparalytic disease botulism. Current treatments for botulinum poisoning are all protein based and thus have a l... Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists [作者：PHAM TUANANH N; YANG ZUNHUA; FANG YUANYING; LUO JUN; LEE JONGKOOK; PARK HAEIL,期刊：Bioorganic & Medicinal Chemistry, 页码：1349-1356 , 文章类型： Article，,卷期：2013年21-5] GPR119 agonist has emerged as a promising target for the treatment of type 2 diabetes. A series of novel 2,4-disubstituted quinazoline analogues was prepared and evaluated their agonistic activity against human GPR119. T...