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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50条记录   Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors [作者：Escribano, A; Mateo, AI; de la Nava, EMM; Mayhugh, DR; Cockerham, SL; Beyer, TP; Schmidt, RJ; Cao, GQ; Zhang, YY; Jones, TM; Borel, AG; Sweetana, SA; Cannady, EA; Mantlo, NB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3671-3675 , 文章类型： Article，,卷期：2012年22-11] This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and fav... Remarkably fast and selective aromatization of Hantzsch esters with MoOCl4 and MoCl5: A chemical model for possible biologically relevant properties of molybdenum-containing enzymes [作者：Litvic, M; Regovic, M; Smic, K; Lovric, M; Filipan-Litvic, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3676-3681 , 文章类型： Article，,卷期：2012年22-11] Mo(VI) and Mo(V) salts both react selectively with Hantzsch esters to produce substitute pyridines in good-to-excellent yield (75-99%). The remarkable reactivity and selectivity of MoOCl4 under reflux of acetonitrile and... Use of libraries to access new chemical space: Applications to CRTH2 [作者：Masood, MA; Gardner, M; Dack, K; Winpenny, D; Lunn, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3682-3687 , 文章类型： Article，,卷期：2012年22-11] The generation of novel CRTH2 ligands in heavily congested chemical space, by de novo design of libraries is disclosed. Novel (1719) compounds across seven libraries were synthesised. More than 100 of these compounds sho... Xanthones from Polygala karensium inhibit neuraminidases from influenza A viruses [作者：Dao, TT; Dang, TT; Nguyen, PH; Kim, E; Thuong, PT; Oh, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3688-3692 , 文章类型： Article，,卷期：2012年22-11] The emergence of the H1N1 swine flu pandemic has the possibility to develop the occurrence of disasteror drug-resistant viruses by additional reassortments in novel influenza A virus. In the course of an anti-influenza s... Design, synthesis and biological evaluation of potent NAD(+)-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: Aminoalkoxypyrimidine carboxamides [作者：Gu, WX; Wang, TS; Maltais, F; Ledford, B; Kennedy, J; Wei, YY; Gross, CH; Parsons, J; Duncan, L; Arends, SJR; Moody, C; Perola, E; Green, J; Charifson, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3693-3698 , 文章类型： Article，,卷期：2012年22-11] A series of 2,6-disubstituted aminoalkoxypyrimidine carboxamides (AAPCs) with potent inhibition of bacterial NAD(+)-dependent DNA ligase was discovered through the use of structure-guided design. Two subsites in the NAD(... Design, synthesis and biological evaluation of potent NAD(+)-dependent DNA ligase inhibitors as potential antibacterial agents. Part II: 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones [作者：Wang, TS; Duncan, L; Gu, WX; O'Dowd, H; Wei, YY; Perola, E; Parsons, J; Gross, CH; Moody, CS; Arends, SJR; Charifson, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3699-3703 , 文章类型： Article，,卷期：2012年22-11] A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD(+)-dependent DNA ligase that possess potency against Gram-positive bacteria. (C) 2012 Elsevier Ltd... A new high-yield synthetic route to PET CB1 radioligands [C-11]OMAR and its analogs [作者：Gao, MZ; Wang, M; Zheng, QH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3704-3709 , 文章类型： Article，,卷期：2012年22-11] OMAR analogs reference standards and their corresponding desmethylated precursors were synthesized from substituted anilines either in 4 and 5 steps with 27-32% and 24-31% yield, or in 3 and 4 steps with 21-30% and 19-28... Vascular barrier protective effects of eckol and its derivatives [作者：Kim, TH; Lee, T; Ku, SK; Bae, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3710-3712 , 文章类型： Article，,卷期：2012年22-11] In this Letter, we first investigated the barrier protective effects of eckol and its derivatives against pro-inflammatory responses in human umbilical vein endothelial cells (HUVECs) and in mice. Data showed that eckol ... BC-spiro-estradiols. Synthesis and estrogen receptor binding affinity of four new estradiol isomers [作者：Asim, M; Klonowska, D; Choueiri, C; Korobkov, I; Carlson, KE; Katzenellenbogen, JA; Durst, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3713-3717 , 文章类型： Article，,卷期：2012年22-11] The synthesis of four new isomers of estradiol in which the ring A to ring C planes are perpendicular to each other as a result of a spiro BC ring junction is described. Heterocyclic analogs and carbocyclic homologs of t... Design, synthesis, and evaluation of a novel class of 2,3-disubstituted-tetrahydro-beta-carboline derivatives [作者：Zeng, L; Zhang, JW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3718-3722 , 文章类型： Article，,卷期：2012年22-11] Several novel tetrahydro-beta-carboline derivatives with amino acid residues at the 2-position and a glucosamine group at the 3-position of the tetrahydro-beta-carboline nucleus were synthesized from a readily available ... Fluorometric detection of adenine in target DNA by exciplex formation with fluorescent 8-arylethynylated deoxyguanosine [作者：Saito, Y; Kugenuma, K; Tanaka, M; Suzuki, A; Saito, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3723-3726 , 文章类型： Article，,卷期：2012年22-11] We demonstrated an intriguing method to discriminate adenine by incident appearance of an intense new emission via exciplex formation in hybridization of target DNA with newly designed fluorescent 8-arylethynylated deoxy... Discovery of XL413, a potent and selective CDC7 inhibitor [作者：Koltun, ES; Tsuhako, AL; Brown, DS; Aay, N; Arcalas, A; Chan, V; Du, HW; Engst, S; Ferguson, K; Franzini, M; Galan, A; Holst, CR; Huang, P; Kane, B; Kim, MH; Li, J; Markby, D; Mohan, M; Noson, K; Plonowski, A; Richards, SJ; Robertson, S; Shaw, K; Stott, G; Stout, TJ; Young, J; Yu, PW; Zaharia, CA; Zhang, WT; Zhou, PW; Nuss, JM; Xu, W; Kearney, PC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3727-3731 , 文章类型： Article，,卷期：2012年22-11] CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resultin... The design, synthesis, and biological evaluation of PIM kinase inhibitors [作者：Tsuhako, AL; Brown, DS; Koltun, ES; Aay, N; Arcalas, A; Chan, V; Du, HW; Engst, S; Franzini, M; Galan, A; Huang, P; Johnston, S; Kane, B; Kim, MH; Laird, AD; Lin, R; Mock, L; Ngan, I; Pack, M; Stott, G; Stout, TJ; Yu, PW; Zaharia, C; Zhang, WT; Zhou, PW; Nuss, JM; Kearney, PC; Xu, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3732-3738 , 文章类型： Article，,卷期：2012年22-11] A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were poten... Synthesis and SAR of tetrahydroisoquinolines as Rev-erb alpha agonists [作者：Noel, R; Song, XY; Shin, Y; Banerjee, S; Kojetin, D; Lin, L; Ruiz, CH; Cameron, MD; Burris, TP; Kamenecka, TM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3739-3742 , 文章类型： Article，,卷期：2012年22-11] The design and synthesis of a novel series of Rev-erb alpha agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erb alpha ago... Exploring the molecular mechanism of karrikins and strigolactones [作者：Scaffidi, A; Waters, MT; Bond, CS; Dixon, KW; Smith, SM; Ghisalberti, EL; Flematti, GR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3743-3746 , 文章类型： Article，,卷期：2012年22-11] Karrikins and strigolactones are novel plant growth regulators that contain similar molecular features, but very little is known about how they elicit responses in plants. A tentative molecular mechanism has previously b... Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase [作者：Liu, YY; Lim, BH; Jiang, WW; Flentge, CA; Hutchinson, DK; Madigan, DL; Randolph, JT; Wagner, R; Maring, CJ; Kati, WM; Molla, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3747-3750 , 文章类型： Article，,卷期：2012年22-11] Aryl dihydrouracil derivatives were identified from high throughput screening as potent inhibitors of HCV NS5B polymerase. The aryl dihydrouracil derivatives were shown to be non-competitive with respect to template RNA ...