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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149条记录   Effect of a second nitroimidazole redox centre on the accumulation of a hypoxia marker: Synthesis and in vitro evaluation of Tc-99m-labeled bisnitroimidazole propylene amine oxime complexes [作者：Huang, HF; Zhou, H; Li, ZJ; Wang, XY; Chu, TW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：172-177 , 文章类型： Article，,卷期：2012年22-1] Up to now, most of the hypoxia markers contain only one nitroimidazole redox centre, such as Oxo[[3,3,9,9-tetramethyl-1-(2-nitro-1H-imidazol-1-yl)-4,8-diazaundecane-2,10-dione dioximato] (3-)-N, N', N '', N''']technetium... Efficient photodynamic therapy of cancer using chemotherapeutic porphyrin-ruthenium metalla-cubes [作者：Schmitt, F; Barry, NPE; Juillerat-Jeanneret, L; Therrien, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：178-180 , 文章类型： Article，,卷期：2012年22-1] Two cationic octanuclear metalla-cubes [Ru(8)(eta(6)-C(6)H(5)Me)(8)(tpp-H2)(2)(dhbq)(4)](8+) and [Ru(8)(eta(6)-p-iPrC(6)H(4)Me) 8(tpp-H2) 2(dhbq) 4] 8+ were prepared and evaluated as dual photosensitizers and chemotherap... Activation of human RNase L by 2 '- and 5 '-O-methylphosphonate- modified oligoadenylates [作者：Pav, O; Panova, N; Snasel, J; Zbornikova, E; Rosenberg, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：181-185 , 文章类型： Article，,卷期：2012年22-1] To determine the influence of internucleotide linkage and sugar ring conformation, and the role of 5'-terminal phosphate, on the activation of human RNase L, a series of 2'- and 5'-O-methylphosphonate-modified tetramers ... Synthesis and evaluation of 4-alkoxy-[1 '-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4 '-piperidine)] analogues as histamine-3 receptor antagonists [作者：Becknell, NC; Dandu, RR; Lyons, JA; Aimone, LD; Raddatz, R; Hudkins, RL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：186-189 , 文章类型： Article，,卷期：2012年22-1] A novel class of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues were designed and synthesized as H3R antagonists. Structure-activity relationship identified sulfone 27 with excellent H3R ... Novel and selective spiroindoline-based inhibitors of sky kinase [作者：Powell, NA; Kohrt, JT; Filipski, KJ; Kaufman, M; Sheehan, D; Edmunds, JE; Delaney, A; Wang, YL; Bourbonais, F; Lee, DY; Schwende, F; Sun, F; McConnell, P; Catana, C; Chen, HF; Ohren, J; Perrin, LA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：190-193 , 文章类型： Article，,卷期：2012年22-1] We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibi... 4,5-Dihydropyridazin-3-one derivatives as histamine H-3 receptor inverse agonists [作者：Hudkins, RL; Aimone, LD; Dandu, RR; Dunn, D; Gruner, JA; Huang, ZQ; Josef, KA; Lyons, JA; Mathiasen, JR; Tao, M; Zulli, AL; Raddatz, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：194-198 , 文章类型： Article，,卷期：2012年22-1] H3R structure-activity relationships for a new class of 4,5-dihydropyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modification of the 4,5-dihydropyridazinone moiety to block in vivo metabolism identified... Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series [作者：Lachance, N; Guiral, S; Huang, Z; Leclerc, JP; Li, CS; Oballa, RM; Ramtohul, YK; Wang, H; Wu, J; Zhang, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：623-627 , 文章类型： Article，,卷期：2012年22-1] Elevated levels of stearoyl-CoA desaturase (SCD) activity have been implicated in metabolic disorders such as obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemically-... Novel 5-and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P(1) agonists with in vivo lymphocyte-depleting activity [作者：Frohn, M; Cee, VJ; Lanman, BA; Pickrell, AJ; Golden, J; Rivenzon-Segal, D; Middleton, S; Fiorino, M; Xu, H; Schrag, M; Xu, Y; McElvain, M; Muller, K; Siu, J; Burli, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：628-633 , 文章类型： Article，,卷期：2012年22-1] An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5- and 6-substituted S1P(1) agonists. Structural optimization for potency ultimately deli... Protective effect of ginseng sapogenins against 2,2 '-azobis (1-aminopropane) dihydrochloride (AAPH)-induced LLC-PK1 cell damage [作者：Kang, KS; Kim, HY; Yoo, HH; Piao, XL; Ham, J; Yang, HO; Park, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：634-637 , 文章类型： Article，,卷期：2012年22-1] The effect of ginseng sapogenins, aglycone parts of ginsenosides, against oxidative damage by radical generator, 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH), in renal epithelial LLC-PK1 cells was investigated t... Site of action of a pentapeptide agonist at the glucagon-like peptide-1 receptor. Insight into a small molecule agonist-binding pocket [作者：Dong, MQ; Pinon, DI; Miller, LJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：638-641 , 文章类型： Article，,卷期：2012年22-1] The development of small molecule agonists for class B G protein-coupled receptors (GPCRs) has been quite challenging. With proof-of-concept that exenatide, the parenterally administered peptide agonist of the glucagon-l... Facile synthesis of 1,2,3-triazole analogs of SGLT2 inhibitors by 'click chemistry' [作者：Li, LT; Zhou, LF; Li, YJ; Huang, J; Liu, RH; Wang, B; Wang, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：642-644 , 文章类型： Article，,卷期：2012年22-1] Novel analogs of SGLT2 inhibitors containing the 1,2,3-triazole motif were designed and synthesized for urinary glucose excretion evaluation. The C-glucosides with triazole aglycone can be easily constructed by click che... aza-Flavanones as potent cross-species microRNA inhibitors that arrest cell cycle [作者：Chandrasekhar, S; Pushpavalli, SNCVL; Chatla, S; Mukhopadhyay, D; Ganganna, B; Vijeender, K; Srihari, P; Reddy, CR; Ramaiah, MJ; Bhadra, U,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：645-648 , 文章类型： Article，,卷期：2012年22-1] aza-Flavanones have been identified as a new class of selective microRNA inhibitors. These compounds were found to arrest cell cycle via a novel cross species microRNA-dependent regulatory pathway interpreting an unexpec... SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors [作者：Lu, ZJ; Yi-Heng, C; Napolitano, JB; Taylor, G; Ali, A; Hammond, ML; Deng, QL; Tan, E; Tong, XC; Xu, SYS; Latham, MJ; Peterson, LB; Anderson, MS; Eveland, SS; Guo, Q; Hyland, SA; Denise, PM; Chen, Y; Sparrow, CP; Wright, SD; Sinclair, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：199-203 , 文章类型： Article，,卷期：2012年22-1] SAR studies of the substitution effect on the central phenyl ring of the biphenyl scaffold were carried out using anacetrapib (9a) as the benchmark. The results revealed that the new analogs with substitutions to replace... Synthesis of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as platelet aggregation inhibitors [作者：Tian, X; Wang, LY; Xia, SA; Li, ZB; Liu, XH; Yuan, Y; Fang, L; Zuo, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：204-206 , 文章类型： Article，,卷期：2012年22-1] Novel 2H-benzo[b][1,4] oxazin-3(4H)-ones have been synthesized by condensation, reduction, O-alkylation and Smiles rearrangement using 3-bromo-4-hydroxy benzaldehyde, anilines, and chloroacetyl chloride as starting mater... Eudesmane-type sesquiterpene lactones inhibit multiple steps in the NF-kappa B signaling pathway induced by inflammatory cytokines [作者：Tamura, R; Chen, YJ; Shinozaki, M; Arao, K; Wang, LY; Tang, WX; Hirano, S; Ogura, H; Mitsui, T; Taketani, S; Ando, M; Kataoka, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：207-211 , 文章类型： Article，,卷期：2012年22-1] Inflammatory cytokines, such as interleukin-1 alpha (IL-1 alpha) and tumor necrosis factor-a (TNF-alpha), induce the intracellular signaling pathway leading to the activation of nuclear factor kappa B (NF-kappa B). A ser... Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents [作者：Kumar, D; Kumar, NM; Ghosh, S; Shah, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：212-215 , 文章类型： Article，,卷期：2012年22-1] A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 ...