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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75条记录   Antiviral effect of ribonuclease conjugated oligodeoxynucleotides targeting the IRES RNA of the hepatitis C virus [作者：Gamble, C; Trotard, M; Le Seyec, J; Abreu-Guerniou, V; Nicolas, G; Berree, F; Carboni, B; Felden, B; Gillet, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3581-3585 , 文章类型： Article，,卷期：2009年19-13] Hepatitis C virus (HCV) translation initiation is mediated by a highly structured and conserved RNA, termed the Internal Ribosome Entry Site (IRES), located at the 5'-end of its single stranded RNA genome. It is a key ta... The discovery of the potent aurora inhibitor MK-0457 (VX-680) [作者：Bebbington, D; Binch, H; Charrier, JD; Everitt, S; Fraysse, D; Golec, J; Kay, D; Knegtel, R; Mak, C; Mazzei, F; Miller, A; Mortimore, M; O'Donnell, M; Patel, S; Pierard, F; Pinder, J; Pollard, J; Ramaya, S; Robinson, D; Rutherford, A; Studley, J; Westcott, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3586-3592 , 文章类型： Article，,卷期：2009年19-13] The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR is described. Replacement of the initial quinazoline core with a pyrimidine scaffold and modi. cation of substituents led to ... Discovery of novel lipophilic inhibitors of OXA-10 enzyme (class D beta-lactamase) by screening amino analogs and homologs of citrate and isocitrate [作者：Beck, J; Vercheval, L; Bebrone, C; Herteg-Fernea, A; Lassaux, P; Marchand-Brynaert, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3593-3597 , 文章类型： Article，,卷期：2009年19-13] Aminocitrate (and homolog) derivatives have been prepared by bis-alkylation of glycinate Schiff bases with bromoacetates (and ethyl acrylate), followed by N-acylation and esters (partial or complete) deprotection. Aminoi... Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening [作者：Robert, K; Timea, P; Kirabo, A; Sayyah, J; Figueroa, NC; List, AF; Sokol, L; Zuckerman, KS; Gali, M; Bisht, KS; Sayeski, PP; Keseru, GM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3598-3601 , 文章类型： Article，,卷期：2009年19-13] Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematologic malignancies. A somatic mutation of JAK2 (Val617Phe) was previously shown to occur in 98% of patients with ... Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs) [作者：Bailey, N; Bamford, MJ; Brissy, D; Brookfield, J; Demont, E; Elliott, R; Garton, N; Farre-Gutierrez, I; Hayhow, T; Hutley, G; Naylor, A; Panchal, TA; Seow, HX; Spalding, D; Takle, AK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3602-3606 , 文章类型： Article，,卷期：2009年19-13] Acid pump antagonists (APAs) such as the imidazo[1,2-a]pyridine AZD-0865 2 have proven efficacious at low oral doses in acid related gastric disorders. Herein we describe some of the broader SAR in this class of molecule... The regulation of inflammatory cytokine secretion in macrophage cell line by the chemical constituents of Rhus sylvestris [作者：Ding, Y; Nguyen, HT; Kim, SI; Kim, HW; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3607-3610 , 文章类型： Article，,卷期：2009年19-13] In our preliminary screening study on the anti-inflammatory activity, eight triterpenes, one sterol, and one chalcone were isolated from the CH2Cl2-soluble extract of the stems and leaves of Rhus sylvestris Siebold and Z... Regioselective synthesis and biological evaluation of bis(indolyl)methane derivatized 1,4-disubstituted 1,2,3-bistriazoles as anti-infective agents [作者：Damodiran, M; Muralidharan, D; Perumal, PT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3611-3614 , 文章类型： Article，,卷期：2009年19-13] The regioselective synthesis of 1,4-disubstituted 1,2,3-bistriazoles from a variety of N-propargyl bis(indolyl)methanes with sodium azide using CuI as the catalyst in polyethyleneglycol-400 is reported. This process is o... Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors [作者：Rajamaki, S; Innitzer, A; Falciani, C; Tintori, C; Christ, F; Witvrouw, M; Debyser, Z; Massa, S; Botta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3615-3618 , 文章类型： Article，,卷期：2009年19-13] A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the ... Selection of a DNA aptamer that binds 8-OHdG using GMP-agarose [作者：Miyachi, Y; Shimizu, N; Ogino, C; Fukuda, H; Kondo, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3619-3622 , 文章类型： Article，,卷期：2009年19-13] DNA aptamers, which bind specific molecule, such as 8-OHdG, with high affinity were investigated using an in vitro selection strategy called systematic evolution of ligands by exponential enrichment (SELEX). However, 8-O... Optimization of 5-phenyl-3-pyridinecarbonitriles as PKC theta inhibitors [作者：Boschelli, DH; Wang, D; Prashad, AS; Subrath, J; Wu, B; Niu, C; Lee, J; Yang, XK; Brennan, A; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3623-3626 , 文章类型： Article，,卷期：2009年19-13] The key intermediate, 4-chloro-5-iodo-3-pyridinecarbonitrile, allowed for ready optimization of the PKC theta inhibitory activity of a series of 3-pyridinecarbonitriles. Analog 13b with a 4-methylindol-5-ylamino group at... Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists [作者：Kobayashi, K; Uchiyama, M; Ito, H; Takahashi, H; Yoshizumi, T; Sakoh, H; Nagatomi, Y; Asai, M; Miyazoe, H; Tsujita, T; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Ohta, H; Okamoto, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3627-3631 , 文章类型： Article，,卷期：2009年19-13] The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identi... Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors [作者：Im, I; Lee, ES; Choi, SJ; Lee, JY; Kim, YC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3632-3636 , 文章类型： Article，,卷期：2009年19-13] Human rhinovirus 3C protease (HRV 3C(pro)) is known to be a promising target for development of therapeutic agents against the common cold because of the importance of the protease in viral replication as well as its exp... Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors [作者：Hendricks, RT; Fell, JB; Blake, JF; Fischer, JP; Robinson, JE; Spencer, SR; Stengel, PJ; Bernacki, AL; Leveque, VJP; Le Pogam, S; Rajyaguru, S; Najera, I; Josey, JA; Harris, JR; Swallow, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3637-3641 , 文章类型： Article，,卷期：2009年19-13] The importance of internal hydrogen bonding in a series of benzothiadiazine and 1,4-benzothiazine NS5b inhibitors has been explored. Computational analysis has been used to compare the protonated vs. anionic forms of eac... Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones [作者：de Vicente, J; Hendricks, RT; Smith, DB; Fell, JB; Fischer, J; Spencer, SR; Stengel, PJ; Mohr, P; Robinson, JE; Blake, JF; Hilgenkamp, RK; Yee, C; Adjabeng, G; Elworthy, TR; Tracy, J; Chin, E; Li, J; Wang, B; Bamberg, JT; Stephenson, R; Oshiro, C; Harris, SF; Ghate, M; Leveque, V; Najera, I; Le Pogam, S; Rajyaguru, S; Ao-Ieong, G; Alexandrova, L; Larrabee, S; Brandl, M; Briggs, A; Sukhtankar, S; Farrell, R; Xu, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3642-3646 , 文章类型： Article，,卷期：2009年19-13] A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with thi... Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208 [作者：Dolle, RE; Michaut, M; Martinez-Teipel, B; Seida, PR; Ajello, CW; Muller, AL; DeHaven, RN; Carroll, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3647-3650 , 文章类型： Article，,卷期：2009年19-13] Cyclic tetrapeptide c[Phe-pro-Phe-trp] 2, a diastereomer of CJ-15,208 ( 1), was identified as a potent dual kappa/mu opioid receptor antagonist devoid of delta opioid receptor affinity against cloned human receptors: K-i... Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases [作者：Riester, D; Hildmann, C; Haus, P; Galetovic, A; Schober, A; Schwienhorst, A; Meyer-Almes, FJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3651-3656 , 文章类型： Article，,卷期：2009年19-13] Histone deacetylases reside among the most important and novel target classes in oncology. Selective lead structures are intensively developed to improve efficacy and reduce adverse effects. The common assays used so far...