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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49条记录   Synthesis and in vitro antitumor activity of asperphenamate derivatives as autophagy inducer [作者：Yuan, L; Li, YC; Zou, CY; Wang, C; Gao, J; Miao, CX; Ma, EL; Sun, TM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2216-2220 , 文章类型： Article，,卷期：2012年22-6] In an effort to improve the aqueous solubility and the antitumor activity of natural product asperphenamate, we have designed and synthesized three series of asperphenamate derivatives, including series I (simplifying mo... Anti-inflammatory and anti-arthritic effects of new synthetic 3-(4-hydroxyphenyl)-4-(4-thiomethoxyphenyl)-1H-pyrrole-2,5-dione [作者：Shin, JS; Noh, YS; Yoo, MS; Lee, JY; Cho, YW; Lee, KT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2221-2225 , 文章类型： Article，,卷期：2012年22-6] We previously reported that 3-(4-hydroxyphenyl)-4-(4-thiomethoxyphenyl)-1H-pyrrole-2,5-dione (1, HMP) has a strong inhibitory effect on prostaglandin E-2 (PGE(2)) production. In this study, the anti-inflammatory and anti... Synthesis and biological evaluation of 21-arylidenepregnenolone derivatives as neuroprotective agents [作者：Jiang, CS; Guo, XJ; Gong, JX; Zhu, TT; Zhang, HY; Guo, YW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2226-2229 , 文章类型： Article，,卷期：2012年22-6] A series of 21-arylidenepregnenolone derivatives and their corresponding epoxides were synthesized. The neuroprotective effects of these steroidal compounds against amyloid-beta(5-35)(A beta(25-35))- and hydrogen peroxid... Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors [作者：Lin, H; Erhard, K; Hardwicke, MA; Luengo, JI; Mack, JF; McSurdy-Freed, J; Plant, R; Raha, K; Rominger, CM; Sanchez, RM; Schaber, MD; Schulz, MJ; Spengler, MD; Tedesco, R; Xie, R; Zeng, JJ; Rivero, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2230-2234 , 文章类型： Article，,卷期：2012年22-6] A series of PI3K-beta selective inhibitors, imidazo[1,2-a]-pyrimidin-5(1H)-ones, has been rationally designed based on the docking model of the more potent R enantiomer of TGX-221, identified by a chiral separation, in a... Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors [作者：Al-Hourani, BJ; Sharma, SK; Suresh, M; Wuest, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2235-2238 , 文章类型： Article，,卷期：2012年22-6] A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (C... Synthesis and cytotoxicity of diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group [作者：Xing, YJ; Lou, LG; Chen, XZ; Ye, QS; Xu, YP; Xie, CY; Jiang, J; Liu, WP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2239-2241 , 文章类型： Article，,卷期：2012年22-6] Six diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group were synthesized and characterized by elemental analysis, FAB-MS, FT-IR, H-1 and C-13 NMR along with a single crystal X-ray di... Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain [作者：Jiao, GS; Kim, S; Moayeri, M; Crown, D; Thai, A; Cregar-Hernandez, L; McKasson, L; Sankaran, B; Lehrer, A; Wong, T; Johns, L; Margosiak, SA; Leppla, SH; Johnson, AT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2242-2246 , 文章类型： Article，,卷期：2012年22-6] Four core structures capable of providing sub-nanomolar inhibitors of anthrax lethal factor (LF) were evaluated by comparing the potential for toxicity, physicochemical properties, in vitro ADME profiles, and relative ef... Ketoolivosyl-tetracenomycin C: A new ketosugar bearing tetracenomycin reveals new insight into the substrate flexibility of glycosyltransferase ElmGT [作者：Nybo, SE; Shabaan, KA; Kharel, MK; Sutardjo, H; Salas, JA; Mendez, C; Rohr, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2247-2250 , 文章类型： Article，,卷期：2012年22-6] A new tetracenomycin analog, 8-demethyl-8-(4'-keto)-alpha-L-olivosyl-tetracenomycin C, was generated through combinatorial biosynthesis. Streptomyces lividans TK 24 (cos16F4) was used as a host for expression of a 'sugar... One pot synthesis and anticancer activity of dimeric phloroglucinols [作者：Chauthe, SK; Bharate, SB; Periyasamy, G; Khanna, A; Bhutani, KK; Mishra, PD; Singh, IP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2251-2256 , 文章类型： Article，,卷期：2012年22-6] A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phlo... Novel oxoisoaporphine-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation [作者：Tang, H; Zhao, HT; Zhong, SM; Wang, ZY; Chen, ZF; Liang, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2257-2261 , 文章类型： Article，,卷期：2012年22-6] A series of novel oxoisoaporphine-based inhibitors (10-aminoalkylamino-1-azabenzanthrone ArNH(CH2)(n)(NRR2)-R-1) of acetylcholinesterase (AChE) has been designed, synthesized, and tested for their ability to inhibit AChE... Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors [作者：Hu, E; Kunz, RK; Rumfelt, S; Chen, N; Burli, R; Li, C; Andrews, KL; Zhang, JD; Chmait, S; Kogan, J; Lindstrom, M; Hitchcock, SA; Treanor, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2262-2265 , 文章类型： Article，,卷期：2012年22-6] We report the discovery of 6,7-dimethoxy-4-(pyridin-3-yl)cinnolines as novel inhibitors of phosphodiesterase 10A (PDE10A). Systematic examination and analyses of structure-activity-relationships resulted in single digit ... Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis [作者：Andrews, MJI; Clase, JA; Bar, G; Tricarico, G; Edwards, PJ; Brys, R; Chambers, M; Schmidt, W; MacLeod, A; Hirst, K; Allen, V; Birault, V; Le, J; Harris, J; Self, A; Nash, K; Dixon, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2266-2270 , 文章类型： Article，,卷期：2012年22-6] MAPKAPK5 has been proposed to play a role in regulation of matrix metalloprotease expression and so to be a potential target for intervention in rheumatoid arthritis. We present here the identification of a series of com... Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity [作者：Hanrahan, P; Bell, J; Bottomley, G; Bradley, S; Clarke, P; Curtis, E; Davis, S; Dawson, G; Horswill, J; Keily, J; Moore, G; Rasamison, C; Bloxham, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2271-2278 , 文章类型： Article，,卷期：2012年22-6] Substituted azaquinazolinones were identified as antagonists of the GHSr-1A receptor for the treatment of type II diabetes and obesity. Optimisation for potency and LogD lead to the identification of orally bioavailable,... Biotransformations of 6 ',7 '-dihydroxybergamottin and 6 ',7 '-epoxybergamottin by the citrus-pathogenic fungi diminish cytochrome P450 3A4 inhibitory activity [作者：Myung, K; Manthey, JA; Narciso, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2279-2282 , 文章类型： Article，,卷期：2012年22-6] Penicillium digitatum, as well as five other citrus pathogenic species, (Penicillium ulaiense Link, Geotrichum citri Link, Botrytis cinerea P. Micheli ex Pers., Lasiodiplodia theobromae (Pat.) Griffon & Maubl., and Phomo... Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors [作者：Bussenius, J; Anand, NK; Blazey, CM; Bowles, OJ; Bannen, LC; Chan, DSM; Chen, BL; Co, EW; Costanzo, S; DeFina, SC; Dubenko, L; Engst, S; Franzini, M; Huang, P; Jammalamadaka, V; Khoury, RG; Kim, MH; Klein, RR; Laird, D; Le, DT; Mac, MB; Matthews, DJ; Markby, D; Miller, N; Nuss, JM; Parks, JJ; Tsang, TH; Tsuhako, AL; Wang, Y; Xu, W; Rice, KD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2283-2286 , 文章类型： Article，,卷期：2012年22-6] The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active in... Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1) [作者：Harikrishnan, LS; Srivastava, N; Kayser, LE; Nirschl, DS; Kumaragurubaran, K; Roy, A; Gupta, A; Karmakar, S; Karatt, T; Mathur, A; Burford, NT; Chen, J; Kong, Y; Cvijic, M; Cooper, CB; Poss, MA; Trainor, GL; Wong, TW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2287-2290 , 文章类型： Article，,卷期：2012年22-6] Identification, synthesis and structure-activity relationship of small-molecule VIPR1 antagonists encompassing two chemical series are described. (C) 2012 Elsevier Ltd. All rights reserved.