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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59条记录   A small molecule regulates hairpin structures in d(CGG) trinucleotide repeats [作者：Hagihara, M; He, HP; Kimura, M; Nakatani, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2000-2003 , 文章类型： Article，,卷期：2012年22-5] Unusual expansion of trinucleotide repeats has been identified as a common mechanism of hereditary neurodegenerative diseases. Although the actual mechanism of repeat expansion remains uncertain, trinucleotide repeat ins... Depigmenting activity of new kojic acid derivative obtained as a side product in the synthesis of cinnamate of kojic acid [作者：Cho, JC; Rho, HS; Baek, HS; Ahn, SM; Woo, BY; Hong, YD; Cheon, JW; Heo, JM; Shin, SS; Park, YH; Suh, KD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2004-2007 , 文章类型： Article，,卷期：2012年22-5] We synthesized cinnamate derivatives of kojic acid for use as depigmenting agents by various esterification methods. The cinnamate of 5-position of kojic acid (6) was obtained by EDC coupling, DCC coupling, acid chloride... Design, synthesis, single-crystal and preliminary antitumor activity of novel arenesulfonylimidazolidin-2-ones [作者：Abdel-Aziz, AAM; El-Azab, AS; El-Subbagh, HI; Al-Obaid, AM; Alanazi, AM; Al-Omar, MA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2008-2014 , 文章类型： Article，,卷期：2012年22-5] Novel series of 1-(arenesulfonyl)imidazolidin-2-one (3a-i) and 1,3-bis(arenesulfonyl)imidazolidin-2-one (5a-i) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from nine dif... Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors [作者：Cuny, GD; Ulyanova, NP; Patnaik, D; Liu, JF; Lin, XJ; Auerbach, K; Ray, SS; Xian, J; Glicksman, MA; Stein, RL; Higgins, JMG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2015-2019 , 文章类型： Article，,卷期：2012年22-5] Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis that has emerged as a possible cancer therapeutic target. High throughput screening of approximately 140,000 compounds identified the... Hit to lead SAR study on benzoxazole derivatives for an NPY Y5 antagonist [作者：Omori, N; Kouyama, N; Yukimasa, A; Watanabe, K; Yokota, Y; Tanioka, H; Nambu, H; Yukioka, H; Sato, N; Tanaka, Y; Sekiguchi, K; Okuno, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2020-2023 , 文章类型： Article，,卷期：2012年22-5] We report a hit to lead study on a novel benzoxazole NPY Y5 antagonist. Starting from HTS hit 1, structure-activity relationships were developed. Compound 12 showed reduction of food intake and a tendency to suppress bod... Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor-beta type I receptor kinase [作者：Amada, H; Sekiguchi, Y; Ono, N; Matsunaga, Y; Koami, T; Asanuma, H; Shiozawa, F; Endo, M; Ikeda, A; Aoki, M; Fujimoto, N; Wada, R; Sato, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2024-2029 , 文章类型： Article，,卷期：2012年22-5] A novel series of 4-thiazolylimidazoles was synthesized as transforming growth factor-beta (TGF-beta) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for ... The anomeric mixture of some O-galactolipid derivatives is more toxic against cancer cells than either anomer alone [作者：Song, SX; Wu, ML; He, XP; Zhou, YB; Sheng, L; Li, J; Chen, GR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2030-2032 , 文章类型： Article，,卷期：2012年22-5] The anomeric mixture of a series of O-galactolipid derivatives is revealed to be more toxic against several cancer cell lines than their either single component with the pure alpha- or beta-configuration. This interestin... The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: Hit-to-lead identification and SAR [作者：Bregman, H; Nguyen, HN; Feric, E; Ligutti, J; Liu, D; McDermott, JS; Wilenkin, B; Zou, AR; Huang, LY; Li, XW; McDonough, SI; DiMauro, EF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2033-2042 , 文章类型： Article，,卷期：2012年22-5] Herein the discovery of a novel class of aminoheterocyclic Na(v)1.7 antagonists is reported. Hit compound 1 was potent but suffered from poor pharmacokinetics and selectivity. The compact structure of 1 offered a modular... The use of small molecule probes to study spatially separated stimulus-induced signaling pathways [作者：Kravchenko, VV; Gloeckner, C; Stowe, GN; Kang, YJ; Tobias, PS; Mathison, JC; Ulevitch, RJ; Kaufmann, GF; Janda, KD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2043-2045 , 文章类型： Article，,卷期：2012年22-5] Simultaneous activation of signaling pathways requires dynamic assembly of higher-order protein complexes at the cytoplasmic domains of membrane-associated receptors in a stimulus-specific manner. Here, using the paradig... Discovery of a new class of ghrelin receptor antagonists [作者：Mihalic, JT; Kim, YJ; Lizarzaburu, M; Chen, XQ; Deignan, J; Wanska, M; Yu, M; Fu, JS; Chen, X; Zhang, A; Connors, R; Liang, LM; Lindstrom, M; Ma, J; Tang, L; Dai, K; Li, LP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2046-2051 , 文章类型： Article，,卷期：2012年22-5] A series of benzodiazepine antagonists of the human ghrelin receptor GHSR1a were synthesized and their antagonism and metabolic stability were evaluated. The potency of these analogs was determined using a functional aeq... Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists [作者：Chakka, N; Bregman, H; Du, BF; Nguyen, HN; Buchanan, JL; Feric, E; Ligutti, J; Liu, D; McDermott, JS; Zou, AR; McDonough, SI; DiMauro, EF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2052-2062 , 文章类型： Article，,卷期：2012年22-5] Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of... Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKK epsilon kinases [作者：Wang, T; Block, MA; Cowen, S; Davies, AM; Devereaux, E; Gingipalli, L; Johannes, J; Larsen, NA; Su, QB; Tucker, JA; Whitston, D; Wu, JQ; Zhang, HJ; Zinda, M; Chuaqui, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2063-2069 , 文章类型： Article，,卷期：2012年22-5] The design, synthesis and biological evaluation of a series of azabenzimidazole derivatives as TBK1/IKK epsilon kinase inhibitors are described. Starting from a lead compound 1a, iterative design and SAR exploitation of ... Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo [3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1 [作者：Le Brazidec, JY; Pasis, A; Tam, B; Boykin, C; Black, C; Wang, DP; Claassen, G; Chong, JH; Chao, JH; Fan, JH; Nguyen, K; Silvian, L; Ling, LN; Zhang, L; Choi, M; Teng, M; Pathan, N; Zhao, S; Li, T; Taveras, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2070-2074 , 文章类型： Article，,卷期：2012年22-5] Since the early 2000s, the Aurora kinases have become major targets of oncology drug discovery particularly Aurora-A and Aurora-B kinases (AKA/AKB) for which the selective inhibition in cells lead to different phenotypes... Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H-3 antagonists [作者：Shao, N; Aslanian, R; West, RE; Williams, SM; Wu, RL; Hwa, J; Sondey, C; Lachowicz, J; Palani, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2075-2078 , 文章类型： Article，,卷期：2012年22-5] The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H-3 antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core... Cytotoxic terpenoids from Juglans sinensis leaves and twigs [作者：Yang, H; Cho, HJ; Sim, SH; Chung, YK; Kim, DD; Sung, SH; Kim, J; Kim, YC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2079-2083 , 文章类型： Article，,卷期：2012年22-5] Bioassay-guided fractionation of an 80% MeOH extract of Juglan sinensis leaves and twigs has resulted in the isolation of three new triterpenes (1-3) and two new sesquiterpenes (4-5) along with two known sesquiterpenes (... Identification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis [作者：Jung, SK; Ko, Y; Yu, KR; Kim, JH; Lee, JY; Chae, CH; Ji, S; Kim, CH; Lee, HK; Choi, EB; Kim, BY; Erikson, RL; Chung, SJ; Kim, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2084-2088 , 文章类型： Article，,卷期：2012年22-5] The serine phosphatase SerB653 plays a crucial role in the infection of Porphyromonas gingivalis, which contributes to the pathogenesis of periodontitis, an inflammatory disease of teeth-supporting tissues. Because funct...