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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   Identification of a sub-micromolar, non-peptide inhibitor of beta-secretase with low neural cytotoxicity through in silico screening [作者：Xu, WJ; Chen, G; Zhu, WL; Zuo, ZL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5763-5766 , 文章类型： Article，,卷期：2010年20-19] Nowadays identification of novel non-peptide beta-secretase (BACE-1, hereinafter) inhibitors with low cytotoxicity and good blood-brain barrier (BBB) property holds common interest of drug discovery for Alzheimer's disea... Cytotoxic cycloartane triterpene and rare isomeric bisclerodane diterpenes from the leaves of Polyalthia longifolia var. pendula [作者：Sashidhara, KV; Singh, SP; Kant, R; Maulik, PR; Sarkar, J; Kanojiya, S; Kumar, KR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5767-5771 , 文章类型： Article，,卷期：2010年20-19] A 24-methylenecycloartane-3 beta, 16 beta, 23 beta-triol, Longitriol (1), rare bisclerodane imides, Longimide A (2) and previously known Longimide B (3) were isolated from ethanolic extract of the leaves of Polyalthia lo... Structure-activity relationships of tulipalines, tuliposides, and related compounds as inhibitors of MurA [作者：Mendgen, T; Scholz, T; Klein, CD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5757-5762 , 文章类型： Article，,卷期：2010年20-19] The enzyme MurA performs an essential step in peptidoglycan biosynthesis and is therefore a target for the discovery of novel antibacterial compounds. We report here the inhibition of MurA by natural products from tulips... Synthesis and cytotoxicity of some biurets against human breast cancer T47D cell line [作者：Fouladdel, S; Khalaj, A; Adibpour, N; Azizi, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5772-5775 , 文章类型： Article，,卷期：2010年20-19] Design, synthesis and cytotoxicity of several known and novel biurets against human breast cancer T47D cell line in comparison to doxorubicin are described. Biurets incorporating 2-methyl quinoline-4-yl and benzo[d]thiaz... Synthesis and biological evaluation of indomethacin analogs possessing a N-difluoromethyl-1,2-dihydropyrid-2-one ring system: A search for novel cyclooxygenase and lipoxygenase inhibitors [作者：Chowdhury, MA; Huang, ZJ; Abdellatif, KRA; Dong, Y; Yu, G; Velazquez, CA; Knaus, EE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5776-5780 , 文章类型： Article，,卷期：2010年20-19] A novel class of indomethacin analogs were synthesized wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety (5-LOX pharmacophore) was attached at its C-4 or C-5 position via either a C=O (14a-b) or CH2 (19a-b) linker... Biochemical and biophysical characterization of unique switch pocket inhibitors of p38 alpha [作者：Swann, SL; Merta, PJ; Kifle, L; Groebe, D; Sarris, K; Hajduk, PJ; Sun, CH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5787-5792 , 文章类型： Article，,卷期：2010年20-19] Herein we describe the identification and characterization of a class of molecules that are believed to extend into a region of p38 known as the 'switch pocket'. Although these molecules lack a canonical hinge binding mo... Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region [作者：Ahn, YM; Clare, M; Ensinger, CL; Hood, MM; Lord, JW; Lu, WP; Miller, DF; Patt, WC; Smith, BD; Vogeti, L; Kaufman, MD; Petillo, PA; Wise, SC; Abendroth, J; Chun, L; Clark, R; Feese, M; Kim, H; Stewart, L; Flynn, DL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5793-5798 , 文章类型： Article，,卷期：2010年20-19] Switch control pocket inhibitors of p38-alpha kinase are described. Durable type II inhibitors were designed which bind to arginines (Arg67 or Arg70) that function as key residues for mediating phospho-threonine 180 depe... Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase [作者：De Schutter, JW; Zaretsky, S; Welbourn, S; Pause, A; Tsantrizos, YS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5781-5786 , 文章类型： Article，,卷期：2010年20-19] A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhi... Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO) [作者：Reynolds, A; Hanani, R; Hibbs, D; Damont, A; Da Pozzo, E; Selleri, S; Dolle, F; Martini, C; Kassiou, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5799-5802 , 文章类型： Article，,卷期：2010年20-19] Herein, we report the synthesis of four new phenyl alkyl ether derivatives (7, 9-11) of the pyrazolo[1,5-a]pyrimidine acetamide class, all of which showed high binding affinity and selectivity for the TSPO and, in the ca... Pyrazolopyridines as potent PDE4B inhibitors: 5-Heterocycle SAR [作者：Mitchell, CJ; Ballantine, SP; Coe, DM; Cook, CM; Delves, CJ; Dowle, MD; Edlin, CD; Hamblin, JN; Holman, S; Johnson, MR; Jones, PS; Keeling, SE; Kranz, M; Lindvall, M; Lucas, FS; Neu, M; Solanke, YE; Somers, DO; Trivedi, NA; Wiseman, JO,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5803-5806 , 文章类型： Article，,卷期：2010年20-19] Following the discovery of 4-(substituted amino)-1-alkyl-pyrazolo[3,4-b]pyridine-5-carboxamides as potent and selective phosphodiesterase 4B inhibitors, [Hamblin, J. N.; Angell, T.; Ballentine, S., et al. Bioorg. Med. Ch... Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors [作者：Watanabe, T; Umezawa, Y; Takahashi, Y; Akamatsu, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5807-5810 , 文章类型： Article，,卷期：2010年20-19] Pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase (OSC) inhibitors 3 and 4 were discovered by conducting a virtual screening, a docking study based on the crystallographic structure of OSC, and biological assay... Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF) [作者：Hare, AA; Leng, L; Gandavadi, S; Du, X; Cournia, Z; Bucala, R; Jorgensen, WL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5811-5814 , 文章类型： Article，,卷期：2010年20-19] The cytokine MIF is involved in inflammation and cell proliferation via pathways initiated by its binding to the transmembrane receptor CD74. MIF also exhibits keto-enol tautomerase activity, believed to be vestigial in ... Reverse-benzamidine antimalarial agents: Design, synthesis, and biological evaluation [作者：Berger, O; Wein, S; Duckert, JF; Maynadier, M; El Fangour, S; Escale, R; Durand, T; Vial, H; Vo-Hoang, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5815-5817 , 文章类型： Article，,卷期：2010年20-19] In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity o... Fluorinated 2 '-hydroxychalcones as garcinol analogs with enhanced antioxidant and anticancer activities [作者：Padhye, S; Ahmad, A; Oswal, N; Dandawate, P; Rub, RA; Deshpande, J; Swamy, KV; Sarkar, FH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5818-5821 , 文章类型： Article，,卷期：2010年20-19] Chalcones are involved in the synthesis of flavonoids and are themselves known to exhibit multiple pharmacological properties. However, compared to other structurally similar phytochemicals like garcinol and curcumin, th... Identification of a new biaryl scaffold generating potent renin inhibitors [作者：Lacombe, P; Aspiotis, R; Bayly, C; Chen, A; Dube, D; Fortin, R; Gallant, M; Juteau, H; Liu, S; Mckay, D; Roy, P; Wu, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5822-5826 , 文章类型： Article，,卷期：2010年20-19] The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple,... Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases [作者：Valente, S; Bana, E; Viry, E; Bagrel, D; Kirsch, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5827-5830 , 文章类型： Article，,卷期：2010年20-19] The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpre...