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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56条记录   Discovery of a new class of glucosylceramide synthase inhibitors [作者：Koltun, E; Richards, S; Chan, V; Nachtigall, J; Du, HW; Noson, K; Galan, A; Aay, N; Hanel, A; Harrison, A; Zhang, J; Won, KA; Tam, D; Qian, F; Wang, T; Finn, P; Ogilvie, K; Rosen, J; Mohan, R; Larson, C; Lamb, P; Nuss, J; Kearney, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6773-6777 , 文章类型： Article，,卷期：2011年21-22] A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained ... Acid mediated formation of an N-acyliminium ion from tubulysins: A new methodology for the synthesis of natural tubulysins and their analogs [作者：Vlahov, IR; Wang, Y; Vetzel, M; Hahn, S; Kleindl, PJ; Reddy, JA; Leamon, CP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6778-6781 , 文章类型： Article，,卷期：2011年21-22] Tubuylsins are extremely potent cytotoxic agents which inhibit tubulin polymerization and lead to cell cycle arrest and apoptosis. Tubulysins have been isolated from fermentation mixtures and have been chemically synthes... The design, synthesis and biological evaluation of novel URB602 analogues as potential monoacylglycerol lipase inhibitors [作者：Szabo, M; Agostino, M; Malone, DT; Yuriev, E; Capuano, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6782-6787 , 文章类型： Article，,卷期：2011年21-22] We have synthesised an extensive series of URB602 analogues as inhibitors of monoacylglycerol lipase (MAGL), which is the major enzyme responsible for metabolising the endocannabinoid 2-arachidonylglycerol. The recently ... Synthesis of purine modified 2 '-C-methyl nucleosides as potential anti-HCV agents [作者：Zhang, HW; Zhou, LH; Coats, SJ; McBrayer, TR; Tharnish, PM; Bondada, L; Detorio, M; Amichai, SA; Johns, MD; Whitaker, T; Schinazi, RF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6788-6792 , 文章类型： Article，,卷期：2011年21-22] Based on the anti-hepatitis C activity of 2'-C-methyl-adenosine and 2'-C-methyl-guanosine, a series of new modified purine 2'-C-methyl nucleosides was prepared as potential anti-hepatitis C virus agents. Herein, we repor... Synthesis and in vivo evaluation of [(18)F]N-(2-benzofuranylmethyl)-N '-[4-(2-fluoroethoxy)benzyl]piperazine, a novel sigma(1) receptor PET imaging agent [作者：Moussa, IA; Banister, SD; Giboureau, N; Meikle, SR; Kassiou, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6820-6823 , 文章类型： Article，,卷期：2011年21-22] N-(2-Benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine (6, sigma(1) K(i) = 2.6 nM) was radiolabeled with fluorine-18 to provide a potential sigma(1) receptor radioligand for use in positron emission tomography ... Structural requirement of phenylthiourea analogs for their inhibitory activity of melanogenesis and tyrosinase [作者：Thanigaimalai, P; Lee, KC; Sharma, VK; Joo, C; Cho, WJ; Roh, E; Kim, Y; Jung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6824-6828 , 文章类型： Article，,卷期：2011年21-22] Effect of a series of 1-phenylthioureas 1a-k and 1,3-disubstituted thioureas 2a-k were evaluated against melanin formation in melanoma B16 cell line and mushroom tyrosinase. Inhibitory activity of tyrosinase of 1-phenylt... Structure-activity relationship study of arylsulfonylimidazolidinones as anticancer agents [作者：Sharma, VK; Lee, KC; Venkateswararao, E; Joo, C; Kim, MS; Sharma, N; Jung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6829-6832 , 文章类型： Article，,卷期：2011年21-22] In an effort to find novel N-arylsulfonylimidazolidinones as highly potent anticancer agent, the structure-activity relationship of ethyl 2-methyl-4-(2-oxo-4-phenylimidazolidin-1-ylsulfonyl)phenylcarbamate was explored t... Fatty acids as natural specific inhibitors of the proto-oncogenic protein Shp2 [作者：Liu, DP; Kong, GP; Chen, QC; Wang, GH; Li, J; Xu, Y; Lin, T; Tian, YP; Zhang, XK; Yao, XS; Feng, GS; Lu, ZX; Chen, HF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6833-6837 , 文章类型： Article，,卷期：2011年21-22] Src homology-2 domain-containing protein tyrosine phosphatase (Shp2), a novel proto-oncogenic protein, is an important target in cancer therapy research. Approximately 2000 plant extracts were screened to find its natura... Investigating the role of the hydroxyl groups of substrate erythrose 4-phosphate in the reaction catalysed by the first enzyme of the shikimate pathway [作者：Tran, D; Pietersma, AL; Schofield, LR; Rost, M; Jameson, GB; Parker, EJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6838-6841 , 文章类型： Article，,卷期：2011年21-22] 3-Deoxy-D-arabino-heptulosonate 7-phosphate (DAH7P) synthase catalyses the first step of the shikimate pathway, which is responsible for the biosynthesis of aromatic amino acids in microorganisms and plants. This enzyme ... Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores [作者：Betageri, R; Gilmore, T; Kuzmich, D; Kirrane, TM; Bentzien, J; Wiedenmayer, D; Bekkali, Y; Regan, J; Berry, A; Latli, B; Kukulka, AJ; Fadra, TN; Nelson, RM; Goldrick, S; Zuvela-Jelaska, L; Souza, D; Pelletier, J; Dinallo, R; Panzenbeck, M; Torcellini, C; Lee, H; Pack, E; Harcken, C; Nabozny, G; Thomson, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6842-6851 , 文章类型： Article，,卷期：2011年21-22] We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. ... Discovery of highly potent small molecule Hepatitis C Virus entry inhibitors [作者：Mittapalli, GK; Jackson, A; Zhao, F; Lee, H; Chow, S; McKelvy, J; Wong-Staal, F; Macdonald, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6852-6855 , 文章类型： Article，,卷期：2011年21-22] Novel, highly potent small molecule HCV entry inhibitors are reported. The SAR exploration of a hit molecule identified from screening of a compound library led to the identification of highly potent compounds with IC(50... Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies [作者：Yang, YF; Miller, KJ; Zhu, YH; Hong, Y; Tian, Y; Murugesan, N; Gu, ZX; O'Tanyi, E; Keim, WJ; Rohrbach, KW; Johnghar, S; Behnia, K; Pelleymounter, MA; Carlson, KE; Ewing, WR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6856-6860 , 文章类型： Article，,卷期：2011年21-22] Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans.... Identification of 4-quinolone derivatives as inhibitors of reactive oxygen species production from human umbilical vein endothelial cells [作者：Onda, K; Narazaki, F; Ishibashi, N; Nakanishi, K; Sawada, Y; Imamura, K; Momose, K; Furukawa, S; Shimada, Y; Moriguchi, H; Yuda, M; Kayakiri, H; Ohta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6861-6866 , 文章类型： Article，,卷期：2011年21-22] Oxidative stress is widely recognized as being associated with a number of disorders, including metabolic dysfunction and atherosclerosis. A series of substituted 4-quinolone derivatives were prepared and evaluated as in... Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: The 14-3-3 sigma case [作者：Corradi, V; Mancini, M; Santucci, MA; Carlomagno, T; Sanfelice, D; Mori, M; Vignaroli, G; Falchi, F; Manetti, F; Radi, M; Botta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6867-6871 , 文章类型： Article，,卷期：2011年21-22] Targeting the binding site of 14-3-3 proteins lets the release of partner proteins involved in cell cycle progression, apoptosis, cytoskeletal rearrangement and transcriptional regulation and may therefore be regarded as... A fluorescent probe for GM1 gangliosidosis related beta-galactosidase: N-(Dansylamino) hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-D-galactitol [作者：Frohlich, RFG; Fantur, K; Furneaux, RH; Paschke, E; Stutz, AE; Wicki, J; Withers, SG; Wrodnigg, TM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6872-6875 , 文章类型： Article，,卷期：2011年21-22] N-(Dansylamino)hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-D-galactitol, a strong competitive inhibitor of beta-galactosidase, enhances residual beta-galactosidase activities in fibroblasts and serves as lead en route... AHL-dependent quorum sensing inhibition: Synthesis and biological evaluation of alpha-(N-alkyl-carboxamide)-gamma-butyrolactones and alpha-(N-alkyl-sulfonamide)-gamma-butyrolactones [作者：Boukraa, M; Sabbah, M; Soulere, L; El Efrit, ML; Queneau, Y; Doutheau, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6876-6879 , 文章类型： Article，,卷期：2011年21-22] New N-acylhomoserine lactone (AHL) analogues in which the amide function is replaced by a reverse-amide one have been studied as AHL QS modulators. The series of compounds consists of alpha-(N-alkyl-carboxamide)- gamma-b...