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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71条记录   A new approach to the synthesis of polyunsaturated deuterated isoprostanes: Total synthesis of d(4)-5-epi-8,12-iso-iPF(3 alpha)-VI and d(4)-8,12-iso-iPF(3 alpha)-VI [作者：Chang, CT; Patel, P; Gore, V; Song, WL; Lawson, JA; Powell, WS; FitzGerald, GA; Rokach, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6755-6758 , 文章类型： Article，,卷期：2009年19-23] The total and stereospecific synthesis of d(4)-5-epi-8,12-iso-iPF(3 alpha)-VI 55 and d(4)-8,12-iso-iPF(3 alpha)-VI 64, EPA-derived all-syn-isoprostanes (iPs), has been accomplished. Because of issues related to volatilit... Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis [作者：Duc, MH; Tran, MN; Nguyen, TD; Do, TH; Kim, YH; Luong, HV; Ahn, JS; Bae, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6759-6761 , 文章类型： Article，,卷期：2009年19-23] Bioassay-guided fractionation of the chloroform-soluble fraction of Morus bombycis, using an in vitro PTP1B inhibitory assay led to the identification of three 2-arylbenzofurans, albafuran A (1), mulberrofuran W (2) and ... New classes of potent and bioavailable human renin inhibitors [作者：Remen, L; Bezencon, O; Richard-Bildstein, S; Prade, DBL; Corminboeuf, O; Boss, C; Grisostomi, C; Sifferlen, T; Strickner, P; Hess, P; Delahaye, S; Treiber, A; Weller, T; Binkert, C; Steiner, B; Fischli, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6762-6765 , 文章类型： Article，,卷期：2009年19-23] New classes of de novo designed renin inhibitors are reported. Some of these compounds display excellent in vitro and in vivo activities toward human renin in a TGR model. The synthesis of these new types of mono- and bi... Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors [作者：Cho, HJ; Jung, MJ; Kwon, Y; Na, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6766-6769 , 文章类型： Article，,卷期：2009年19-23] A total of seven new oxyranylmethyloxy or thiiranylmethyloxy group substituted 5-azaxanthones and -acridones analogues were synthesized and tested for their biological activities for cancer cell lines and topoisomerases.... Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening [作者：Mok, NY; Chadwick, J; Kellett, KAB; Hooper, NM; Johnson, AP; Fishwick, CWG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6770-6774 , 文章类型： Article，,卷期：2009年19-23] A novel series of isatin-based inhibitors of beta-secretase (BACE-1) have been identified using a virtual high-throughput screening approach. Structure-activity relationship studies revealed structural features important... Preliminary SAR analysis of novel antiproliferative N-6,5 '-bis-ureidoadenosine derivatives [作者：Peterson, MA; Oliveira, M; Christiansen, MA; Cutler, CE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6775-6779 , 文章类型： Article，,卷期：2009年19-23] A preliminary library of novel N-6,5'-bis-ureidoadenosine analogs and related derivatives was prepared and tested for activity against the NCI 60 panel of human cancers. A 2'-O-TBS group was found to be necessary, but no... 5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase [作者：Tarver, JE; Jessop, TC; Carlsen, M; Augeri, DJ; Fu, QH; Healy, JP; Heim-Riether, A; Xu, A; Taylor, JA; Shen, M; Keyes, PE; Kimball, SD; Yu, XC; Miranda, M; Liu, QY; Swaffield, JC; Nouraldeen, A; Wilson, AGE; Finch, R; Jhaver, K; Foushee, AMD; Anderson, S; Oravecz, T; Carson, KG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6780-6783 , 文章类型： Article，,卷期：2009年19-23] A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular pot... Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS [作者：Zhou, Y; Rodriguez, AL; Williams, R; Weaver, CD; Conn, PJ; Lindsley, CW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6502-6506 , 文章类型： Article，,卷期：2009年19-23] This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional... Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors [作者：Jessop, TC; Tarver, JE; Carlsen, M; Xu, A; Healy, JP; Heim-Riether, A; Fu, QH; Taylor, JA; Augeri, DJ; Shen, M; Stouch, TR; Swanson, RV; Tari, LW; Hunter, M; Hoffman, I; Keyes, PE; Yu, XC; Miranda, M; Liu, QY; Swaffield, JC; Kimball, SD; Nouraldeen, A; Wilson, AGE; Foushee, AMD; Jhaver, K; Finch, R; Anderson, S; Oravecz, T; Carson, KG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6784-6787 , 文章类型： Article，,卷期：2009年19-23] A series of deoxycytidine kinase inhibitors was simultaneously optimized for potency and PK properties. A co-crystal structure then allowed merging this series with a high throughput screening hit to afford a highly pote... 2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors [作者：Cole, AG; Bohnstedt, AC; Paradkar, V; Kingsbury, C; Quintero, JG; Park, H; Lu, YC; You, M; Neagu, I; Diller, DJ; Letourneau, JJ; Shao, YF; James, RA; Riviello, CM; Ho, KK; Lin, TH; Wang, BJ; Appell, KC; Sills, M; Quadros, E; Kimble, EF; Ohlmeyer, MHJ; Webb, ML,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6788-6792 , 文章类型： Article，,卷期：2009年19-23] A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the p... Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors [作者：Vincent, F; Nguyen, MT; Emerling, DE; Kelly, MG; Duncton, MAJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6793-6796 , 文章类型： Article，,卷期：2009年19-23] The screening of known medicinal agents against new biological targets has been shown to be a valuable approach for revealing new pharmacology of marketed compounds. Recently, carbamate, urea and ketone inhibitors of fat... Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists [作者：Hategan, G; Polozov, AM; Zeller, W; Cao, H; Mishra, RK; Kiselyov, AS; Ramirez, J; Halldorsdottir, G; Andresson, P; Gurney, ME; Singh, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6797-6800 , 文章类型： Article，,卷期：2009年19-23] We have developed a pharmacophore model for the EP3 receptor antagonists based on its endogenous ligand PGE(2). This ligand-based design yielded a series of novel peri-substituted [4.3.0] bicyclic aromatics featuring 1-a... Discovery and optimization of antibacterial AccC inhibitors [作者：Cheng, CC; Shipps, GW; Yang, ZW; Sun, BY; Kawahata, N; Soucy, KA; Soriano, A; Orth, P; Xiao, L; Mann, P; Black, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6507-6514 , 文章类型： Article，,卷期：2009年19-23] The biotin carboxylase (AccC) is part of the multi-component bacterial acetyl coenzyme-A carboxylase (ACCase) and is essential for pathogen survival. We describe herein the affinity optimization of an initial hit to give... Four new cytotoxic oligosaccharidic derivatives of 12-oleanene from Lysimachia heterogenea Klatt [作者：Huang, XA; Liang, YJ; Cai, XL; Feng, XQ; Zhang, CH; Fu, LW; Deng, WD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6515-6518 , 文章类型： Article，,卷期：2009年19-23] Cytotoxicity-guided phytochemical analysis on the extract of Lysimachia heterogenea Klatt led to the isolation of 3 beta,16 beta-12-oleanene-3,16,23,28-tetrol (1) and its four new oligosaccharidic derivatives heterogenos... Non-hinge-bindingpyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors [作者：Berger, DM; Torres, N; Dutia, M; Powell, D; Ciszewski, G; Gopalsamy, A; Levin, JI; Kim, KH; Xu, WX; Wilhelm, J; Hu, YB; Collins, K; Feldberg, L; Kim, S; Frommer, E; Wojciechowicz, D; Mallon, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6519-6523 , 文章类型： Article，,卷期：2009年19-23] As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies reveale... Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors [作者：Ioannidis, S; Lamb, ML; Davies, AM; Almeida, L; Su, M; Bebernitz, G; Ye, MW; Bell, K; Alimzhanov, M; Zinda, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6524-6528 , 文章类型： Article，,卷期：2009年19-23] The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead...