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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84条记录   Discovery of novel osthole derivatives as potential anti-breast cancer treatment [作者：You, LS; An, R; Wang, XH; Li, YM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7426-7428 , 文章类型： Article，,卷期：2010年20-24] Osthole, an ingredient of Traditional Chinese Medicine (TCM) from natural product Cnidium monnieri (L.) Cusson, was used as a lead compound for structural modification. A series of osthole derivatives bearing aryl substi... Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK [作者：Tanis, SP; Plewe, MB; Johnson, TW; Butler, SL; Dalvie, D; DeLisle, D; Dress, KR; Hu, QY; Huang, BW; Kuehler, JE; Kuki, A; Liu, W; Peng, QH; Smith, GL; Solowiej, J; Tran, KT; Wang, H; Yang, AL; Yin, CF; Yu, XM; Zhang, JH; Zhu, HC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7429-7434 , 文章类型： Article，,卷期：2010年20-24] HIV-1 integrase is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the discovery... 28-Nor-oleanane-type triterpene saponins from Camellia japonica and their inhibitory activity on LPS-induced NO production in macrophage RAW264.7 cells [作者：Thao, NTP; Hung, TM; Cuong, TD; Kim, JC; Kim, EH; Jin, SE; Na, M; Lee, YM; Kim, YH; Choi, JS; Min, BS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7435-7439 , 文章类型： Article，,卷期：2010年20-24] Four new 28-nor-oleanane-type triterpene oligoglycosides, camellenodiol 3-O-beta-D-galactopyranosyl (1 -> 2)[beta-D-xylopyranosyl(1 -> 2)-beta-D-galactopyranosyl(1 -> 3)]-beta-D-glucuronopyranoside (2), camellenodiol 3-O... Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: Discovery of MK-5286 [作者：Li, LH; Berthelette, C; Chateauneuf, A; Ouellet, M; Sturino, CF; Wang, ZY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7440-7443 , 文章类型： Article，,卷期：2010年20-24] The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1S)-1-hydroxy-1-(trifluoromethyl) propyl]-1H-1,2,3-triazol-1-yl} me... Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore [作者：Li, LH; Beaulieu, C; Carriere, MC; Denis, D; Greig, G; Guay, D; O'Neill, G; Zamboni, R; Wang, ZY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7462-7465 , 文章类型： Article，,卷期：2010年20-24] We discovered that the introduction of a methyl group to the benzylic position of the N-benzyl group in lead compound 1a has a dramatic effect on improving the binding selectivity of this ligand for the prostanoid recept... Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease [作者：Beaulieu, C; Isabel, E; Fortier, A; Masse, F; Mellon, C; Methot, N; Ndao, M; Nicoll-Griffith, D; Lee, D; Park, H; Black, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7444-7449 , 文章类型： Article，,卷期：2010年20-24] Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino nitrile warhead in P1 exhibit low nanomolar in vitro potency again... 3-O-Phosphate ester conjugates of 17-beta-O-{1-[2-carboxy-(2-hydroxy-4-methoxy-3-carboxamido)anilido]ethyl}1,3,5(10)-estratriene as novel bone-targeting agents [作者：Nasim, S; Vartak, AP; Pierce, WM; Taylor, KG; Smith, N; Crooks, PA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7450-7453 , 文章类型： Article，,卷期：2010年20-24] A series of 3-O-phosphorylated analogs (4-10) of a novel bone-targeting estradiol analog (3) were synthesized after a thorough study of the reaction of 3 with a selection of phosphoryl chlorides under a variety of reacti... Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3 [作者：Malerich, JP; Lam, JS; Hart, B; Fine, RM; Klebansky, B; Tanga, MJ; D'Andrea, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7454-7457 , 文章类型： Article，,卷期：2010年20-24] Tyrosine kinase 2 (TYK2) is required for signaling of interleukin-23 (IL-23), which plays a key role in rheumatoid arthritis. Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibito... The discovery of new spirocyclic muscarinic M-3 antagonists [作者：Stocks, MJ; Alcaraz, L; Bailey, A; Bowers, K; Donald, D; Edwards, H; Hunt, F; Kindon, N; Pairaudeau, G; Theaker, J; Warner, DJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7458-7461 , 文章类型： Article，,卷期：2010年20-24] The optimisation of a new series of high potency muscarinic M3 antagonists, derived from high throughput screening library hit is described. (C) 2010 Elsevier Ltd. All rights reserved. Design of a novel class of biphenyl CETP inhibitors [作者：Lu, ZJ; Napolitano, JB; Theberge, A; Ali, A; Hammond, ML; Tan, E; Tong, XC; Xu, SYS; Latham, MJ; Peterson, LB; Anderson, MS; Eveland, SS; Guo, Q; Hyland, SA; Milot, DP; Chen, Y; Sparrow, CP; Wright, SD; Sinclair, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7469-7472 , 文章类型： Article，,卷期：2010年20-24] A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model.... Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2 [作者：Xue, CB; Wang, AL; Meloni, D; Zhang, K; Kong, L; Feng, H; Glenn, J; Huang, TS; Zhang, YX; Cao, GF; Anand, R; Zheng, CS; Xia, M; Han, Q; Robinson, DJ; Storace, L; Shao, LX; Li, M; Brodmerkel, CM; Covington, M; Scherle, P; Diamond, S; Yeleswaram, S; Vaddi, K; Newton, R; Hollis, G; Friedman, S; Metcalf, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7473-7478 , 文章类型： Article，,卷期：2010年20-24] Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mC... AdoHcy hydrolase of Trichomonas vaginalis: Studies of the effects of 5 '-modified adenosine analogues and related 6-N-cyclopropyl derivatives [作者：Dornbush, PJ; Vazquez-Anaya, G; Shokar, A; Benson, S; Rapp, M; Wnuk, SF; Wrischnik, LA; Land, KM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7466-7468 , 文章类型： Article，,卷期：2010年20-24] Trypanosoma brucei and Trichomonas vaginalis are both parasitic protozoans that are known to share many similar biochemical pathways. Aristeromycin, as well as 5 '-iodovinyl and 5 '-oxime analogues of adenosine, are pote... Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain [作者：Tyagarajan, S; Chakravarty, PK; Zhou, BS; Taylor, B; Eid, R; Fisher, MH; Parsons, WH; Wyvratt, MJ; Lyons, KA; Klatt, T; Li, XH; Kumar, S; Williams, B; Felix, J; Priest, BT; Brochu, RM; Warren, V; Smith, M; Garcia, M; Kaczorowski, GJ; Martin, WJ; Abbadie, C; McGowan, E; Jochnowitz, N; Weber, A; Duffy, JL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7479-7482 , 文章类型： Article，,卷期：2010年20-24] A series of novel biphenyl pyrazole dicarboxamides were identified as potential sodium channel blockers for treatment of neuropathic pain. Compound 20 had outstanding efficacy in the Chung rat spinal nerve ligation (SNL)... Design and synthesis of cyclic sulfonamides and sulfamates as new calcium sensing receptor agonists [作者：Kiefer, L; Gorojankina, T; Dauban, P; Faure, H; Ruat, M; Dodd, RH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7483-7487 , 文章类型： Article，,卷期：2010年20-24] The design, synthesis and calcimimetic properties of various cyclic sulfonamides and sulfamates are described. The latter were prepared from the corresponding o-alkenylarenesulfonamides via copper-or rhodium-catalyzed in... Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease [作者：Li, XF; Zhang, YK; Liu, Y; Zhang, SM; Ding, CZ; Zhou, YS; Plattner, JJ; Baker, SJ; Liu, LA; Bu, W; Kazmierski, WM; Wright, LL; Smith, GK; Jarvest, RL; Duan, MS; Ji, JJ; Cooper, JP; Tallant, MD; Crosby, RM; Creech, K; Ni, ZJ; Zou, WX; Wright, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7493-7497 , 文章类型： Article，,卷期：2010年20-24] HCV NS3/4A serine protease is essential for the replication of the HCV virus and has been a clinically validated target. A series of HCV NS3/4A protease inhibitors containing a novel acylsulfamoyl benzoxaborole moiety at... Development of a sphingosine kinase 1 specific small-molecule inhibitor [作者：Hengst, JA; Wang, XJ; Sk, UH; Sharma, AK; Amin, S; Yun, JK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7498-7502 , 文章类型： Article，,卷期：2010年20-24] The sphingolipid metabolic pathway represents a potential source of new therapeutic targets for numerous hyperproliferative/inflammatory diseases. Targets such as the sphingosine kinases (SphKs) have been extensively stu...