- Monoglycerides from the brown alga Sargassum sagamianum: Isolation, synthesis, and biological activity
[作者:Chang, HW; Jang, KH; Lee, D; Kang, HR; Kim, TY; Lee, BH; Choi, BW; Kim, S; Shin, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3589-3592 , 文章类型: Article,,卷期:2008年18-12]
- Polyunsaturated fatty acid-derived monoglycerides were characterized from the marine brown alga Sargassum sagamianum, collected from Jeju Island, Korea. A new compound of this structural class was isolated and determined...
- Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols
[作者:Innocenti, A; Hilvo, M; Scozzafava, A; Parkkila, S; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3593-3596 , 文章类型: Article,,卷期:2008年18-12]
- Inhibition of the newest isoform of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), CA XV, with a series of phenols was investigated. Murine CA XV showed an inhibition pro. le by phenols distinct of those of the c...
- C3-Spacer-containing circular oligonucleotides as inhibitors of human topoisomerase I
[作者:Wang, YF; Ng, MTT; Zhou, TY; Li, XM; Tan, CH; Li, TH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3597-3602 , 文章类型: Article,,卷期:2008年18-12]
- Some dumbbell-shaped circular oligonucleotides containing internal C3-spacers and Topo I-binding sites were designed and synthesized which displayed high inhibitory efficiency on the activity of human Topo I as well as r...
- Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway
[作者:Lohar, MV; Mundada, R; Bhonde, M; Padgaonkar, A; Deore, V; Yewalkar, N; Bhatia, D; Rathos, M; Joshi, K; Vishwakarma, RA; Kumar, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3603-3606 , 文章类型: Article,,卷期:2008年18-12]
- We herein report the design and synthesis of furoquinoline based novel molecules (16-36) and their in vitro multiple targeted inhibitory potency against PI3K/Akt phosphorylation and mTOR using cell based and cell-free ki...
- Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha 7 nicotinic acetylcholine receptor: In vitro and in vivo activity
[作者:Acker, BA; Jacobsen, EJ; Rogers, BN; Wishka, DG; Reitz, SC; Piotrowski, DW; Myers, JK; Wolfe, ML; Groppi, VE; Thornburgh, BA; Tinholt, PM; Walters, RR; Olson, BA; Fitzgerald, L; Staton, BA; Raub, TJ; Krause, M; Li, KS; Hoffmann, WE; Hajos, M; Hurst, RS; Walker, DP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3611-3615 , 文章类型: Article,,卷期:2008年18-12]
- A novel alpha 7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide ( 3a, PHA-709829), has been identified for the potential treatment of cognitive deficits in schizophrenia. The compo...
- Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCVNS5B polymerase
[作者:Ruebsam, F; Webber, SE; Tran, MT; Tran, CV; Murphy, DE; Zhao, JJ; Dragovich, PS; Kim, SH; Li, LS; Zhou, YF; Han, Q; Kissinger, CR; Showalter, RE; Lardy, M; Shah, AM; Tsan, M; Patel, R; LeBrun, LA; Kamran, R; Sergeeva, MV; Bartkowski, DM; Nolan, TG; Norris, DA; Kirkovsky, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3616-3621 , 文章类型: Article,,卷期:2008年18-12]
- Pyrrolo[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Structure-based design led to the discovery of compound 3k, which displayed potent inhibitory activi...
- Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors
[作者:Bingham, AH; Davenport, RJ; Fosbeary, R; Gowers, L; Knight, RL; Lowe, C; Owen, DA; Parry, DM; Pitt, WR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3622-3627 , 文章类型: Article,,卷期:2008年18-12]
- The synthesis and structure-activity relationship of a novel series of aminopyrimidines are exemplified. Results of key compounds from within this series in the E-selectin reporter cell assay are also reported. (C) 2008 ...
- Structure-based optimization of a potent class of arylamide FMS inhibitors
[作者:Meegalla, SK; Wall, MJ; Chen, J; Wilson, KJ; Ballentine, SK; DesJarlais, RL; Schubert, C; Crysler, CS; Chen, Y; Molloy, CJ; Chaikin, MA; Manthey, CL; Player, MR; Tomczuk, BE; Illig, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3632-3637 , 文章类型: Article,,卷期:2008年18-12]
- An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replac...
- Design, synthesis and evaluation of potent thymidylate synthase X inhibitors
[作者:Onen, FE; Boum, Y; Jacquement, C; Spanedda, MV; Jaber, N; Scherman, D; Myllykallio, H; Herscovici, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3628-3631 , 文章类型: Article,,卷期:2008年18-12]
- Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these mo...
- Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment
[作者:Mayer, SC; Banker, AL; Boschelli, F; Di, L; Johnson, M; Kenny, CH; Krishnamurthy, G; Kutterer, K; Moy, F; Petusky, S; Ravi, M; Tkach, D; Tsou, HR; Xu, WX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3641-3645 , 文章类型: Article,,卷期:2008年18-12]
- Insulin-like growth factor receptor (IGF-1R) is a growth factor receptor tyrosine kinase that acts as a critical mediator of cell proliferation and survival. This receptor is over-expressed or activated in tumor cells an...
- Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype
[作者:Myers, MC; Shah, PP; Beavers, MP; Napper, AD; Diamond, SL; Smith, AB; Huryn, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3646-3651 , 文章类型: Article,,卷期:2008年18-12]
- Recently, we identified a thiocarbazate that exhibits potent inhibitory activity against human cathepsin L. Since this structure represents a novel chemotype with potential for activity against the entire cysteine protea...
- Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer
[作者:Li, Y; Zhang, HB; Huang, WL; Li, YM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3652-3655 , 文章类型: Article,,卷期:2008年18-12]
- Exploration for new MDR-modulator utilizing tetrahydroisoquinoline as scaffold disclosed 6,7-dimethoxy1-(3,4-dimethoxy)benzyl-2-(N-n-octyl-N'-cyano)guanyl-1,2,3,4-tetrahydroisoquinoline (7) as a readily accessible medici...
- IRAK-4 inhibitors. Part III: A series of imidazo[1,2-a] pyridines
[作者:Buckley, GM; Fosbeary, R; Fraser, JL; Gowers, L; Higueruelo, AP; James, LA; Jenkins, K; Mack, SR; Morgan, T; Parry, DM; Pitt, WR; Rausch, O; Richard, MD; Sabin, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3656-3660 , 文章类型: Article,,卷期:2008年18-12]
- Following the identification of a potent IRAK inhibitor through routine project cross screening, a novel class of IRAK-4 inhibitor was established. The SAR of imidazo[1,2-a] pyridino-pyridines and benzimidazolo-pyridines...
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