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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149条记录   Conformationally restricted analog and biotin-labeled probe based on beauveriolide III [作者：Doi, T; Muraoka, T; Ohshiro, T; Matsuda, D; Yoshida, M; Takahashi, T; Omura, S; Tomoda, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：696-699 , 文章类型： Article，,卷期：2012年22-1] A conformationally restricted oxazoline analog 7 was designed on the basis of a SAR study of beauveriolide III (2) and its analogs reported previously. Conformational analysis by molecular mechanics calculation suggested... 4 '-Bromo-5,6,7-trimethoxyflavone represses lipopolysaccharide-induced iNOS and COX-2 expressions by suppressing the NF-kappa B signaling pathway in RAW 264.7 macrophages [作者：Kim, DH; Yun, CH; Kim, MH; Kumar, CN; Yun, BH; Shin, JS; An, HJ; Lee, YH; Yun, YD; Rim, HK; Yoo, MS; Lee, KT; Lee, YS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：700-705 , 文章类型： Article，,卷期：2012年22-1] The regulations of the NO and PGE(2) productions are research topics of interest in the field of anti-inflammatory drug development. In the present study, 5,6,7-trimethoxy- and 5,6,7-trihydroxyflavones 3a-3g were synthes... Inhibitory constituents of Nardostachys chinensis on nitric oxide production in RAW 264.7 macrophages [作者：Hwang, JS; Lee, SA; Hong, SS; Han, XH; Lee, C; Lee, D; Lee, CK; Hong, JT; Kim, Y; Lee, MK; Hwang, BY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：706-708 , 文章类型： Article，,卷期：2012年22-1] The activity-guided fractionation of the MeOH extract of the rhizomes and roots of Nardostachys chinensis led to the isolation of two new sesquiterpenoids, narchinol B (8) and narchinol C (9), along with 10 known compoun... Synthesis and activity of folate conjugated didemnin B for potential treatment of inflammatory diseases [作者：Henne, WA; Kularatne, SA; Ayala-Lopez, W; Doorneweerd, DD; Stinnette, TW; Lu, YJ; Low, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：709-712 , 文章类型： Article，,卷期：2012年22-1] A folate receptor targeted didemnin B conjugate was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. Cell cytotoxicity and TNF-alpha inhibition in RAW264.7 macr... Hydroxycoumarins as selective MAO-B inhibitors [作者：Serra, S; Ferino, G; Matos, MJ; Vazquez-Rodriguez, S; Delogu, G; Vina, D; Cadoni, E; Santana, L; Uriarte, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：258-261 , 文章类型： Article，,卷期：2012年22-1] A series of 3-aryl-4-hydroxycoumarin derivatives was synthesized with the aim to find out the structural features for the MAO inhibitory activity and selectivity. Methoxy and/or chloro substituents were introduced in the... Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases [作者：Ple, PA; Jung, F; Ashton, S; Hennequin, L; Laine, R; Morgentin, R; Pasquet, G; Taylor, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：262-266 , 文章类型： Article，,卷期：2012年22-1] A new series of Quinazoline Ether Inhibitor which potently inhibits VEGFR-2 and PDGFR tyrosine kinases is described here. In vitro, pharmacokinetics and in vivo evaluations led to the selection of AZD2932. (C) 2011 Elsev... 5-and 6-Membered (thio)lactones are prodrug type carbonic anhydrase inhibitors [作者：Carta, F; Maresca, A; Scozzafava, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：267-270 , 文章类型： Article，,卷期：2012年22-1] The inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1) with (thio) coumarins has been recently reported (Maresca et al., J. Am. Chem. Soc. 2009, 131, 3057). Here we demonstrate that a series of gamma- and ... Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2 [作者：De Savi, C; Morley, AD; Nash, I; Karoutchi, G; Page, K; Ting, A; Gerhardt, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：271-277 , 文章类型： Article，,卷期：2012年22-1] Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has de... Design, synthesis and in vitro evaluation of novel bivalent S-adenosylmethionine analogues [作者：Joce, C; White, R; Stockley, PG; Warriner, S; Turnbull, WB; Nelson, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：278-284 , 文章类型： Article，,卷期：2012年22-1] In optimal cases, bivalent ligands can bind with exceptionally high affinity to their protein targets. However, designing optimised linkers, that orient the two binding groups perfectly, is challenging, and yet crucial i... Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E-2 synthase-1 inhibitors [作者：Shiro, T; Takahashi, H; Kakiguchi, K; Inoue, Y; Masuda, K; Nagata, H; Tobe, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：285-288 , 文章类型： Article，,卷期：2012年22-1] The imidazoquinoline derivative 1 was found as a novel mPGES-1 inhibitor. Optimization of 1 led to the identification of the 2-chlorophenyl group at the C(2)-position and the quinolone structure at the C(4)-position. Com... II. Novel HCV NS5B polymerase inhibitors: Discovery of indole C2 acyl sulfonamides [作者：Anilkumar, GN; Selyutin, O; Rosenblum, SB; Zeng, QB; Jiang, YH; Chan, TY; Pu, HY; Wang, L; Bennett, F; Chen, KX; Lesburg, CA; Duca, J; Gavalas, S; Huang, YH; Pinto, P; Sannigrahi, M; Velazquez, F; Venkatraman, S; Vibulbhan, B; Agrawal, S; Ferrari, E; Jiang, CK; Huang, HC; Shih, NY; Njoroge, FG; Kozlowski, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：713-717 , 文章类型： Article，,卷期：2012年22-1] Development of SAR at the C2 position of indole lead 1, a palm site inhibitor of HCV NS5B polymerase (NS5B IC(50) = 0.053 mu M, replicon EC(50) = 4.8 mu M), is described. Initial screening identified an acyl sulfonamide ... Discovery of a novel class of aldol-derived 1,2,3-triazoles: Potent and selective inhibitors of human cytochrome P450 19A1 (aromatase) [作者：McNulty, J; Nair, JJ; Vurgun, N; DiFrancesco, BR; Brown, CE; Tsoi, B; Crankshaw, DJ; Holloway, AC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：718-722 , 文章类型： Article，,卷期：2012年22-1] The discovery of a novel five-component 1,2,3-triazole-containing pharmacophore that exhibits potent and selective inhibition of aromatase (CYP 450 19A1) is described. All compounds are derived from an initial aldol reac... Lead diversification. Application to existing drug molecules: Mifepristone 1 and antalarmin 8 [作者：Masood, MA; Farrant, E; Morao, I; Bazin, M; Perez, M; Bunnage, ME; Fancy, SA; Peakman, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：723-728 , 文章类型： Article，,卷期：2012年22-1] A series of C-H functionalisation plate-based chemical screens and other C-H activation protocols were developed for the chemical diversification of drug molecules. In this Letter, metalloporphyrin and other catalytic ox... A small molecule inhibitor of p53-inducible protein phosphatase PPM1D [作者：Yagi, H; Chuman, Y; Kozakai, Y; Imagawa, T; Takahashi, Y; Yoshimura, F; Tanino, K; Sakaguchi, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：729-732 , 文章类型： Article，,卷期：2012年22-1] PPM1D is a p53-inducible Ser/Thr protein phosphatase. PPM1D gene amplification and overexpression have been reported in a variety of human tumors, including breast cancer and neuroblastoma. Because the phosphatase activi... Indole RSK inhibitors. Part 1: Discovery and initial SAR [作者：Boyer, SJ; Burke, J; Guo, X; Kirrane, TM; Snow, RJ; Zhang, YL; Sarko, C; Soleymanzadeh, L; Swinamer, A; Westbrook, J; DiCapua, F; Padyana, A; Cogan, D; Gao, A; Xiong, ZM; Madwed, JB; Kashem, M; Kugler, S; O'Neill, MM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：733-737 , 文章类型： Article，,卷期：2012年22-1] A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were identified through high throughput screening. An RSK crystal... Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity [作者：Kirrane, TM; Boyer, SJ; Burke, J; Guo, X; Snow, RJ; Soleymanzadeh, L; Swinamer, A; Zhang, YL; Madwed, JB; Kashem, M; Kugler, S; O'Neill, MM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：738-742 , 文章类型： Article，,卷期：2012年22-1] A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1 H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This...