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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106条记录   Induction of microtubule-damage, mitotic arrest, Bcl-2 phosphorylation, Bak activation, and mitochondria-dependent caspase cascade is involved in human Jurkat T-cell apoptosis by aruncin B from Aruncus dioicus var. kamtschaticus [作者：Han, CR; Jun, DY; Woo, HJ; Jeong, SY; Woo, MH; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：945-953 , 文章类型： Article，,卷期：2012年22-2] Exposure of human Jurkat T cells to aruncin B, purified from Aruncus dioicus, caused apoptosis along with microtubule damage, G(2)/M-arrest, Bcl-2 phosphorylation, Bak activation, mitochondrial membrane potential (Delta ... Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents [作者：Yang, YH; Wang, ZL; Yang, JZ; Yang, T; Pi, WY; Ang, W; Lin, YN; Liu, YY; Li, ZC; Luo, YF; Wei, YQ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：954-957 , 文章类型： Article，,卷期：2012年22-2] A series of compounds with a diphenyl ether nucleus were synthesized by incorporating various amines into the diphenyl ether scaffold with an amide bond. Their antitubercular activities were evaluated against Mycobacteri... Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent [作者：Huang, H; Lu, WQ; Li, X; Cong, XL; Ma, HM; Liu, XF; Zhang, Y; Che, P; Ma, RQ; Li, HL; Shen, X; Jiang, HL; Huang, J; Zhu, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：958-962 , 文章类型： Article，,卷期：2012年22-2] Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing age... Preparation and characterization of a novel polymorph of indiplon, Form alpha [作者：Xu, LJ; Wang, J; Xiao, BK; Yang, JY; Liu, YR; Huang, RQ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：963-968 , 文章类型： Article，,卷期：2012年22-2] A new polymorph alpha of indiplon was discovered, initially prepared by two methods, and further characterized by various means including single-crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), variabl... Discovery of novel antitubercular 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1, 3,4-oxadiazol-2-yl]methylamino)-1,2-dihydro-3H-pyrazol-3-one analogues [作者：Ahsan, MJ; Samy, JG; Jain, CB; Dutt, KR; Khalilullah, H; Nomani, MS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：969-972 , 文章类型： Article，,卷期：2012年22-2] In search of potential therapeutics for tuberculosis, we describe herewith the synthesis, characterization and antimycobacterial activity of 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1,2-d... Antioxidative oligostilbenes from Caragana sinica [作者：Jin, Q; Han, XH; Hong, SS; Lee, C; Choe, S; Lee, D; Kim, Y; Hong, JT; Lee, MK; Hwang, BY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：973-976 , 文章类型： Article，,卷期：2012年22-2] Two new oligostilbenes, caragasinins A (5) and B (10), and eight known compounds, kobophenol A (1), (+)-alpha-viniferin (2), (+)-ampelopsin F (3), pallidol (4), (+)-isoampelopsin F (6), miyabenol C (7), carasinaurone (8)... Synthesis and evaluation of 17 alpha-E-20-(heteroaryl)norpregn-1,3,5(10),20 tetraene-3,17 beta-diols [17 alpha-(heteroaryl)vinyl estradiols] as ligands for the estrogen receptor-alpha ligand binding domain (ER alpha-LBD) [作者：Olmsted, SL; Tongcharoensirikul, P; McCaskill, E; Gandiaga, K; Labaree, D; Hochberg, RB; Hanson, RN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：977-979 , 文章类型： Article，,卷期：2012年22-2] A series of 17 alpha-(heteroaryl)vinyi estradiols was prepared to evaluate the influence of heteroatom on the affinity and efficacy of estrogenic ligands for the estrogen receptor-alpha ligand binding domain (ER alpha-LB... Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series [作者：Lachance, N; Gareau, Y; Guiral, S; Huang, Z; Isabel, E; Leclerc, JP; Leger, S; Martins, E; Nadeau, C; Oballa, RM; Ouellet, SG; Powell, DA; Ramtohul, YK; Tranmer, GK; Trinh, T; Wang, H; Zhang, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：980-984 , 文章类型： Article，,卷期：2012年22-2] Inhibition of stearoyl-CoA desaturase (SCD) activity represents a potential novel mechanism for the treatment of metabolic disorders including obesity and type II diabetes. To circumvent skin and eye adverse events obser... Cellular uptake of highly-functionalized ruthenium(II) tris-bipyridine protein-surface mimetics [作者：Turrell, SJ; Filby, MH; Whitehouse, A; Wilson, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：985-988 , 文章类型： Article，,卷期：2012年22-2] This manuscript describes cell-uptake studies with HEK 293T cells on a series of ruthenium complexes shown previously to act as receptors for protein surface recognition and was motivated by a desire to establish if thes... Capture hydrolysis signals in the microsomal stability assay: Molecular mechanisms of the alkyl ester drug and prodrug metabolism [作者：Sun, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：989-995 , 文章类型： Article，,卷期：2012年22-2] The hydrolysis of carboxylic acid esters is often catalyzed by carboxylesterases in human liver microsomes, which is also a common 'noise' in the microsomal stability assay, a widely used screening protocol in drug disco... 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists [作者：Orain, D; Ofner, S; Koller, M; Carcache, DA; Froestl, W; Allgeier, H; Rasetti, V; Nozulak, J; Mattes, H; Soldermann, N; Floersheim, P; Desrayaud, S; Kallen, J; Lingenhoehl, K; Urwyler, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：996-999 , 文章类型： Article，,卷期：2012年22-2] A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified wit... In vitro and in silico studies of polycondensed diazine systems as anti-parasitic agents [作者：Almerico, AM; Tutone, M; Guarcello, A; Lauria, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1000-1004 , 文章类型： Article，,卷期：2012年22-2] Parasitic diseases caused by protozoarian agents are still relevant today more than ever. Recently, we synthesized several polycondensed diazine derivatives by means 1,3-dipolar cycloaddition reactions. A broad selection... 6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3 beta: Discovery of nitrile derivatives with picomolar potency [作者：Li, B; Cociorva, OM; Nomanbhoy, T; Li, Q; Nakamura, K; Nomura, M; Okada, K; Yumoto, K; Liyanage, M; Zhang, MC; Aban, A; Szardenings, AK; Kozarich, JW; Kohno, Y; Shreder, KR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1005-1008 , 文章类型： Article，,卷期：2012年22-2] We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3 beta inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant a... Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors [作者：Poulsen, A; Williams, M; Nagaraj, HM; William, AD; Wang, HS; Soh, CK; Xiong, ZC; Dymock, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1009-1013 , 文章类型： Article，,卷期：2012年22-2] A virtual screen of our in-house database using various fingerprint techniques returned several triazine hits which were found to be mTOR inhibitors with a slight selectivity over PI3K alpha. Using structure-guided lead ... The discovery of potent antagonists of NPBWR1 (GPR7) [作者：Romero, FA; Hastings, NB; Moningka, R; Guo, ZQ; Wang, M; Di Salvo, J; Lei, Y; Trusca, D; Deng, QL; Tong, V; Terebetski, JL; Ball, RG; Ujjainwalla, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1014-1018 , 文章类型： Article，,卷期：2012年22-2] The synthesis and evaluation of small molecule antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)... The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia [作者：Ho, GD; Yang, SW; Smotryski, J; Bercovici, A; Nechuta, T; Smith, EM; McElroy, W; Tan, Z; Tulshian, D; McKittrick, B; Greenlee, WJ; Hruza, A; Xiao, L; Rindgen, D; Mullins, D; Guzzi, M; Zhang, XP; Bleickardt, C; Hodgson, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1019-1022 , 文章类型： Article，,卷期：2012年22-2] High-throughput screening identified a series of pyrazoloquinolines as PDE10A inhibitors. The SAR development led to the discovery of compound 27 as a potent, selective, and orally active PDE10A inhibitor. Compound 27 in...