- 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...
- 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.
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