- Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors
[作者:Nilsson, J; Nielsen, EO; Liljefors, T; Nielsen, M; Sterner, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5713-5716 , 文章类型: Article,,卷期:2008年18-21]
- A series of azaflavone derivatives and analogues were prepared and evaluated for their affinity to the benzodiazepine binding site of the GABA(A) receptor, and compared to their flavone counterparts. Three of the compoun...
- Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
[作者:Bardelle, C; Coleman, T; Cross, D; Davenport, S; Kettle, JG; Ko, EJ; Leach, AG; Mortlock, A; Read, J; Roberts, NJ; Robins, P; Williams, EJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5717-5721 , 文章类型: Article,,卷期:2008年18-21]
- Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent...
- Discovery of (naphthalen-4-yl)( phenyl) methanones and N-methyl-N-phenylnaphthalen-1-amines as new apoptosis inducers using a cell- and caspase-based HTS assay
[作者:Jiang, SC; Crogan-Grundy, C; Drewe, J; Tseng, B; Cai, SX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5725-5728 , 文章类型: Article,,卷期:2008年18-21]
- We report the discovery of a series of (naphthalen-4-yl)(phenyl)methanones as potent inducers of apoptosis using our proprietary cell- and caspase-based ASAP HTS assay. Through SAR studies, a group of N-methyl-N-phenylna...
- N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists
[作者:Aissaoui, H; Koberstein, R; Zumbrunn, C; Gatfield, J; Brisbare-Roch, C; Jenck, F; Treiber, A; Boss, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5729-5733 , 文章类型: Article,,卷期:2008年18-21]
- A series of dual OX1R/OX2R orexin antagonists was prepared based on a N-glycine-sulfonamide core. SAR studies of a screening hit led to compounds with low nanomolar affinity for both receptors and good oral bioavailabili...
- Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons
[作者:Zieminska, E; Lazarewicz, JW; Couladouros, EA; Moutsos, VI; Pitsinos, EN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5734-5737 , 文章类型: Article,,卷期:2008年18-21]
- Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic ...
- Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d] pyrimidines
[作者:Hubbard, RD; Dickerson, SH; Emerson, HK; Griffin, RJ; Reno, MJ; Hornberger, KR; Rusnak, DW; Wood, ER; Uehling, DE; Waterson, AG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5738-5740 , 文章类型: Article,,卷期:2008年18-21]
- A novel class of substituted pyrrolidinyl-acetylenic thieno[3,2-d] pyrimidines has been identified that are potent and selective inhibitors of both EGFR/ErbB-2 receptor tyrosine kinases. The inhibitors are found to displ...
- Highly cytotoxic and neurotoxic acetogenins of the Annonaceae: New putative biological targets of squamocin detected by activity-based protein profiling
[作者:Derbre, S; Gil, S; Taverna, M; Boursier, C; Nicolas, V; Demey-Thomas, E; Vinh, J; Susin, SA; Hocquemiller, R; Poupon, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5741-5744 , 文章类型: Article,,卷期:2008年18-21]
- Acetogenins of the Annonaceae are strong inhibitors of mitochondrial complex I but discrepancies in the structure/activity relationships pled the search for other targets within the whole cell proteome. Combining hemisyn...
- New classes of Gram-positive selective antibacterials: Inhibitors of MRSA and surrogates of the causative agents of anthrax and tuberculosis
[作者:Kabir, MS; Engelbrecht, K; Polanowski, R; Krueger, SM; Ignasiak, R; Rott, M; Schwan, WR; Stemper, ME; Reed, KD; Sherman, D; Cook, JM; Monte, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5745-5749 , 文章类型: Article,,卷期:2008年18-21]
- An antimicrobial phenolic stilbene, (E)-3-hydroxy-5-methoxystilbene, 1 was recently isolated from the leaves of Comptonia peregrina (L.) Coulter and shown to possess inhibitory activity against several Gram-positive bact...
- Regioselective nitration of N-alpha,N-1-bis(trifluoroacetyl)-L-tryptophan methyl ester: Efficient synthesis of 2-nitro and 6-nitro-N-trifluoroacetyl-L-tryptophan methyl ester
[作者:Osborne, AS; Som, P; Metcalf, JL; Phillips, RS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5750-5752 , 文章类型: Article,,卷期:2008年18-21]
- Nitration of N-alpha,N-1-bis(trifluoroacetyl)-L-tryptophan methyl ester with HNO3 in acetic anhydride at 0 degrees C provides N-alpha-trifluoroacetyl-2-nitro-L-tryptophan methyl ester in 67% yield, whereas nitration in t...
- Tetrakis-azaaromatic quaternary ammonium salts: Novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release
[作者:Zhang, ZF; Zheng, GR; Pivavarchyk, M; Deaciuc, AG; Dwoskin, LP; Crooks, PA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5753-5757 , 文章类型: Article,,卷期:2008年18-21]
- A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-e...
- Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors
[作者:Stevens, KL; Reno, MJ; Alberti, JB; Price, DJ; Kane-Carson, LS; Knick, VB; Shewchuk, LM; Hassell, AM; Veal, JM; Davis, ST; Griffin, RJ; Peel, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5758-5762 , 文章类型: Article,,卷期:2008年18-21]
- A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modi. cation of the hinge-binding amine or the...
- A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties
[作者:Choong, IC; Serafimova, I; Fan, JF; Stockett, D; Chan, E; Cheeti, S; Lu, YF; Fahr, B; Pham, P; Arkin, MR; Walker, DH; Hoch, U,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5763-5765 , 文章类型: Article,,卷期:2008年18-21]
- The identification of a selective CDK2, 7, 9 inhibitor 4 with improved permeability is described. Compound 4 exhibits comparable CDK selectivity profile to SNS-032, but shows improved permeability and higher bioavailabil...
- Synthesis and biological evaluation of the Zn (II)-IDB complexes appended with oligopolyamide as potent artificial nuclease
[作者:Li, C; Qiao, RZ; Wang, YQ; Zhao, YF; Zeng, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5766-5770 , 文章类型: Article,,卷期:2008年18-21]
- The zinc (II) complexes, which contain oligopolyamide and bis(2-benzimidazolylmethyl) amine (IDB) conjugated by flexible linker, have been successfully synthesized, characterized, and evaluated as DNA cleavage agents. Th...
- Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl
[作者:Janssen, CO; Lim, S; Lo, EP; Wan, KF; Yu, VC; Lee, MA; Ng, SB; Everett, MJ; Buss, AD; Lane, DP; Boyce, RS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5771-5773 , 文章类型: Article,,卷期:2008年18-21]
- The cytotoxic macrolide kendomycin was identified as a ligand of Bcl-xl, an anti-apoptotic member of the Bcl-2 protein family. Hydrolysis-stable and protonable semi-synthetic analogues have been obtained that retain cyto...
- Antioxidant activity of N-carboxymethyl chitosan oligosaccharides
[作者:Sun, T; Yao, Q; Zhou, DX; Mao, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5774-5776 , 文章类型: Article,,卷期:2008年18-21]
- Three N-carboxymethyl chitosan oligosaccharides (N-CMCOSs) with different degrees of substitution (NA: 0.28, NB: 0.41, and NC: 0.54, respectively) were prepared by the control of the amount of glyoxylic acid in the ether...
|