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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53条记录   Parallel RNA-strand recognition by 2 '-amino-beta-L-LNA [作者：Kumar, TS; Ostergaard, ME; Sharma, PK; Nielsen, P; Wengel, J; Hrdlicka, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2396-2399 , 文章类型： Article，,卷期：2009年19-9] A short synthetic route to the first beta-L-ribo configured locked nucleic acid (LNA), that is, 2'-amino-beta-L-LNA thymine phosphoramidite 6, has been developed from bicyclic nucleoside 1. Incorporation of 2'-amino-beta... Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists [作者：Humphries, PS; Benbow, JW; Bonin, PD; Boyer, D; Doran, SD; Frisbie, RK; Piotrowski, DW; Balan, G; Bechle, BM; Conn, EL; Dirico, KJ; Oliver, RM; Soeller, WC; Southers, JA; Yang, XJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2400-2403 , 文章类型： Article，,卷期：2009年19-9] The development of a series of novel 1,2,3,4-tetrahydroisoquinolin-1-ones as antagonists of G protein-coupled receptor 40 (GPR40) is described. The synthesis, in vitro inhibitory values for GPR40, in vitro microsomal cle... Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta [作者：Sarachine, MJ; Janjic, JM; Wipf, P; Day, BW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2404-2408 , 文章类型： Article，,卷期：2009年19-9] The C-cyclopropylalkylamide scaffold was previously identified as a new structural framework for antiestrogens. A second generation library provided three compounds that bind estrogen receptor ( ER) a. Further screening ... Synthesis and SAR of tolylamine 5-HT6 antagonists [作者：Singer, JM; Wilson, MW; Johnson, PD; Graham, SR; Cooke, LW; Roof, RL; Boxer, PA; Gold, LH; Meltzer, LT; Janssen, A; Roush, N; Campbell, JE; Su, TZ; Hurst, SI; Stoner, CL; Schwarz, JB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2409-2412 , 文章类型： Article，,卷期：2009年19-9] The synthesis and SAR of tolylamines with 5-HT6 receptor antagonist activity is presented. The amine, core aromatic, peripheral aromatic, and ether linker moieties of HTS hit 1 were modulated and the effect on potency at... 1-Sulfonylindazoles as potent and selective 5-HT6 ligands [作者：Liu, KG; Lo, JR; Comery, TA; Zhang, GM; Zhang, JY; Kowal, DM; Smith, DL; Di, L; Kerns, EH; Schechter, LE; Robichaud, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2413-2415 , 文章类型： Article，,卷期：2009年19-9] As part of our continuing efforts to identify therapeutics for CNS diseases, such as schizophrenia and Alzheimer's disease (AD), we have been focused on the 5-HT6 receptor in an attempt to identify ligands as a potential... Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction [作者：Watanabe, A; Fujii, H; Nakajima, M; Hasebe, K; Mochizuki, H; Nagase, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2416-2419 , 文章类型： Article，,卷期：2009年19-9] An attempt to prepare a trimer having the 1,3,5-trioxazatriquinane skeleton led to discovery of a novel rearrangement reaction that afforded a compound with an oxabicyclo[3.2.1]octane skeleton whose reaction mechanism wa... Synthesis of potent antitumor and antiviral benzofuran derivatives [作者：Galal, SA; El-All, ASA; Abdallah, MM; El-Diwani, HI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2420-2428 , 文章类型： Article，,卷期：2009年19-9] A new series of potent antitumor and antiviral benzofuran derivatives was synthesized by the reaction of the furochromone-6-carboxaldehydes 1 and 2 with different heterocyclic amines to yield the benzofuran-5-carbonyl de... Induction of apoptosis promoted by Bang52; a small molecule that downregulates Bcl-x(L) [作者：Rossi, M; Bang, JK; Mazur, S; Iera, JA; Phillips, DC; Zambetti, GP; Appella, DH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2429-2434 , 文章类型： Article，,卷期：2009年19-9] Cancer cells evade death by over-producing specific proteins that inhibit apoptosis. One such group of proteins is the Bcl-2 family, of which Bcl-x(L) is an important member. This protein binds and inhibits BAK, another ... Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P-2 pyridine scaffold [作者：Hamada, Y; Ohta, H; Miyamoto, N; Sarma, D; Hamada, T; Nakanishi, T; Yamasaki, M; Yamani, A; Ishiura, S; Kiso, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2435-2439 , 文章类型： Article，,卷期：2009年19-9] Recently, we reported potent substrate-based pentapeptidic BACE1 inhibitors possessing a hydroxymethylcarbonyl isostere as a substrate transition-state mimic. Because these inhibitors contained some natural amino acids, ... Carbonic anhydrase activators: Activation of human isozymes I, II and IX with phenylsulfonylhydrazido L-histidine derivatives [作者：Abdo, MR; Vullo, D; Saada, MC; Montero, JL; Scozzafava, A; Winum, JY; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2331-2443 , 文章类型： Article，,卷期：2009年19-9] Activation of the human carbonic anhydrase (CA, EC 4.2.1.1) isozymes I, II (cytosolic) and IX (transmembrane, tumor-associated isoform) with a series of arylsulfonylhydrazido-L-histidines incorporating 4-substituted-phen... Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors [作者：Lee, SH; Van, HTM; Yang, SH; Lee, KT; Kwon, Y; Cho, WJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2444-2447 , 文章类型： Article，,卷期：2009年19-9] Benz[b]oxepines 4a-g and 12-oxobenzo[c]phenanthridines 5a-d were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular radical cyclization reaction. Radical cyclization of O-vinyl... Synthesis and protonation behavior of a water-soluble N-fused porphyrin: Conjugation with an oligoarginine by click chemistry [作者：Ikawa, Y; Harada, H; Toganoh, M; Furuta, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2448-2452 , 文章类型： Article，,卷期：2009年19-9] A water-soluble derivative of N-fused porphyrin (NFP) possessing a nona-arginine (R9) peptide tail was synthesized for the first time by a Cu(I)-catalyzed azide-alkyne 'click' reaction. In aqueous solution, at pH 8, the ... Interactions of curcumin with the PfATP6 model and the implications for its antimalarial mechanism [作者：Ji, HF; Shen, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2453-2455 , 文章类型： Article，,卷期：2009年19-9] Despite curcumin has been proved to possess antimalarial effects, the underlying mechanism remains to be elucidated. In this letter, the active site binding modes of curcumin in PfATP6, an important antimalarial target, ... Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform [作者：Rano, TA; Sieber-McMaster, E; Pelton, PD; Yang, M; Demarest, KT; Kuo, GH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2456-2460 , 文章类型： Article，,卷期：2009年19-9] Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein ( CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovas... Synthesis and PKC theta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles [作者：Dushin, RG; Nittoli, T; Ingalls, C; Boschelli, DH; Cole, DC; Wissner, A; Lee, J; Yang, X; Morgan, P; Brennan, A; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2461-2463 , 文章类型： Article，,卷期：2009年19-9] A series of 4-indolylamino-5-phenyl-3-pyridinecarbonitrile inhibitors of PKC theta were synthesized as potential anti-inflammatory agents. The effects of specific substitution on the 5-phenyl moiety and variations of the... 3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors [作者：Vu, AT; Cohn, ST; Terefenko, EA; Moore, WJ; Zhang, P; Mahaney, PE; Trybulski, EJ; Goljer, I; Dooley, R; Bray, JA; Johnston, GH; Leiter, J; Deecher, DC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2464-2467 , 文章类型： Article，,卷期：2009年19-9] A series of 3-(arylamino)-3-phenylpropan-2-olamines was prepared and screened for their ability to inhibit monoamine reuptake. A number of analogues displayed significant dual norepinephrine and serotonin reuptake inhibi...