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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   Synthesis of a spin-labeled anti-estrogen as a dynamic motion probe for the estrogen receptor ligand binding domain [作者：Hendricks, JA; Gulla, SV; Budil, DE; Hanson, RN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1743-1746 , 文章类型： Article，,卷期：2012年22-4] The preparation and characterization of a novel nitroxide spin probe based on a steroidal anti-estrogen is described. The probe 5 demonstrated very high binding affinity for both the alpha and beta isoforms of the estrog... A benzothiazole alkyne fluorescent sensor for Cu detection in living cell [作者：Qi, JJ; Han, MS; Tung, CH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1747-1749 , 文章类型： Article，,卷期：2012年22-4] A new type of alkyne dye, 6-dimethylaminobenzothiazole alkyne (1), was developed for Cu sensing in biological system. Dye (1) offered excellent selective over a panel of ions, only Cu(I) could change the fluorescence of ... Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile [作者：Semple, G; Lehmann, J; Wong, A; Ren, A; Bruce, M; Shin, YJ; Sage, CR; Morgan, M; Chen, WC; Sebring, K; Chu, ZL; Leonard, JN; Al-Shamma, H; Grottick, AJ; Du, FY; Liang, Y; Demarest, K; Jones, RM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1750-1755 , 文章类型： Article，,卷期：2012年22-4] The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. Compound 16 (APD597, JNJ-38431055) was selected for preclinical development based on a good ba... Novel vitamin D receptor ligands bearing a spherical hydrophobic core structure-Comparison of bicyclic hydrocarbon derivatives with boron cluster derivatives [作者：Wongmayura, A; Fujii, S; Ito, S; Kano, A; Taoda, Y; Kawachi, E; Kagechika, H; Tanatani, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1756-1760 , 文章类型： Article，,卷期：2012年22-4] Vitamin D receptor (VDR) is a nuclear receptor for 1 alpha, 25-dihydroxyvitamin D-3 (1 alpha, 25(OH)(2)D-3), and is an attractive target for multiple clinical applications. We recently developed novel non-secosteroidal V... Screening and characterization of a chemical regulator for plant disease resistance [作者：Seo, EK; Nakamura, H; Mori, M; Asami, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1761-1765 , 文章类型： Article，,卷期：2012年22-4] Plants activate systemic acquired resistance (SAR), a form of long-lasting induced defense, to confer protection against a broad spectrum of pathogens. SAR induction is associated with the salicylic acid (SA)mediated def... Suppression of nitric oxide production on LPS/IFN-gamma-stimulated RAW264.7 macrophages by a novel catechin, pilosanol N, from Agrimonia pilosa Ledeb [作者：Taira, J; Ohmine, W; Ogi, T; Nanbu, H; Ueda, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1766-1769 , 文章类型： Article，,卷期：2012年22-4] A novel catechin, pilosanol N (1), was isolated from Agrimonia pilosa Ledeb and its structure was determined by H-1, C-13 NMR and HRESI-MS analyses. Compound 1 inhibited nitric oxide (NO) production in LPS/IFN-gamma-indu... Synthesis and evaluation of a novel series of indoloisoquinolines as small molecule anti-malarial leads [作者：Horrocks, P; Fallon, S; Denman, L; Devine, O; Duffy, LJ; Harper, A; Meredith, EL; Hasenkamp, S; Sidaway, A; Monnery, D; Phillips, TR; Allin, SM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1770-1773 , 文章类型： Article，,卷期：2012年22-4] A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of smallmolecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct region... Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine [作者：Wu, ZC; Yang, CM; Xiong, YS; Feng, Z; Lombardo, M; Verras, A; Chabin, RM; Xu, SY; Tong, XC; Xie, D; Lassman, ME; Bhatt, UR; Garcia-Calvo, MM; Geissler, W; Shen, Z; Chen, Q; Sinharoy, R; Hale, JJ; Tata, JR; Pinto, S; Shen, DM; Colletti, SL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1774-1778 , 文章类型： Article，,卷期：2012年22-4] Efforts to modify the central proline portion of lead compound 4 lead to the discovery of novel prolylcarboxypeptidase (PrCP) inhibitors. Especially, replacement with alanine afforded compound 19 displaying more potent h... Isoform-selective thiazolo[5,4-b]pyridine S1P(1) agonists possessing acyclic amino carboxylate head-groups [作者：Reed, AB; Lanman, BA; Neira, S; Harrington, PE; Sham, KKC; Frohn, M; Pickrell, AJ; Tasker, AS; Gore, A; Fiorino, M; Itano, A; McElvain, M; Middleton, S; Morrison, H; Xu, H; Xu, Y; Wong, M; Cee, VJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1779-1783 , 文章类型： Article，,卷期：2012年22-4] Replacement of the azetidine carboxylate of an S1P(1) agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P(3)-sparing S1P(1) agonist, ( )-2-amino -4-(3-flu... Hybrid liposomes inhibit growth and invasion of human osteosarcoma cells leading to apoptosis [作者：Kitajima, H; Komizu, Y; Ueoka, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1784-1787 , 文章类型： Article，,卷期：2012年22-4] Marked inhibitory effects of hybrid liposomes (HL-n; n = 21, 23, 25) composed of 90 mol % L-alpha-dimyristoylphosphatidylcholine (DMPC) and 10 mol % polyoxyethylene(n) dodecyl ethers on the growth of two human osteosarco... Discovery of CS-2100, a potent, orally active and S1P(3)-sparing S1P(1) agonist [作者：Nakamura, T; Asano, M; Sekiguchi, Y; Mizuno, Y; Tamaki, K; Kimura, T; Nara, F; Kawase, Y; Shimozato, T; Doi, H; Kagari, T; Tomisato, W; Inoue, R; Nagasaki, M; Yuita, H; Oguchi-Oshima, K; Kaneko, R; Watanabe, N; Abe, Y; Nishi, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1788-1792 , 文章类型： Article，,卷期：2012年22-4] S1P(3)-sparing S1P(1) agonists have attracted attention as a suppressant of autoimmunity with reduced side effects. Our synthetic efforts and extensive SAR studies led to the discovery of 10b named CS-2100 with the EC50 ... Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy [作者：Demizu, Y; Okuhira, K; Motoi, H; Ohno, A; Shoda, T; Fukuhara, K; Okuda, H; Naito, M; Kurihara, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1793-1796 , 文章类型： Article，,卷期：2012年22-4] We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquity... 3D-QSAR and 3D-QSSR models of negative allosteric modulators facilitate the design of a novel selective antagonist of human alpha 4 beta 2 neuronal nicotinic acetylcholine receptors [作者：Henderson, BJ; Orac, CM; Maciagiewicz, I; Bergmeier, SC; McKay, DB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1797-1813 , 文章类型： Article，,卷期：2012年22-4] Subtype selective molecules for alpha 4 beta 2 neuronal nicotinic acetylcholine receptors (nAChRs) have been sought as novel therapeutics for nicotine cessation. alpha 4 beta 2 nAChRs have been shown to be involved in me... Efficient double-strand scission of plasmid DNA by quaternized-chitosan zinc complex [作者：Zhang, Q; Xiang, Y; Liang, DW; Peng, YG; Guo, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1814-1817 , 文章类型： Article，,卷期：2012年22-4] N-[(2-Hydroxy-3-trimethylammonium) propyl] chitosan chloride (HTACC) was prepared to construct a chitosan-based zinc complex (HTACC-Zn(II)) as a catalyst with good water solubility for rapid DNA cleavage. Results indicat... Stylissamide X, a new proline-rich cyclic octapeptide as an inhibitor of cell migration, from an Indonesian marine sponge of Stylissa sp. [作者：Arai, M; Yamano, Y; Fujita, M; Setiawan, A; Kobayashi, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1818-1821 , 文章类型： Article，,卷期：2012年22-4] A new proline-rich cyclic octapeptide named stylissamide X (1) was isolated from an Indonesian marine sponge of Stylissa sp. as an inhibitor of cell migration from the guidance of wound-healing assay. The chemical struct... Development of small-molecule probes that selectively kill cells induced to express mutant RAS [作者：Weiwer, M; Bittker, JA; Lewis, TA; Shimada, K; Yang, WS; MacPherson, L; Dandapani, S; Palmer, M; Stockwell, BR; Schreiber, SL; Munoz, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1822-1826 , 文章类型： Article，,卷期：2012年22-4] Synthetic lethal screening is a chemical biology approach to identify small molecules that selectively kill oncogene-expressing cell lines with the goal of identifying pathways that provide specific targets against cance...