- 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...
- 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...
- 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...
|