- Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells
[作者:Nakao, Y; Narazaki, G; Hoshino, T; Maeda, S; Yoshida, M; Maejima, H; Yamashita, JK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2982-2984 , 文章类型: Article,,卷期:2008年18-9]
- Evaluation of antiangiogenic activity of marine sponge derived azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells was carried out. Azumamide E (5) strongly inhibited i...
- Molecular features crucial to the activity of pyrimidine benzamide-based thrombopoietin receptor agonists
[作者:Reiter, LA; Jones, CS; Brissette, WH; McCurdy, SP; Abramov, YA; Bordner, J; DiCapua, FM; Munchhof, MJ; Rescek, DM; Samardjiev, IJ; Withka, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3000-3006 , 文章类型: Article,,卷期:2008年18-9]
- The identification of small molecule modulators of biological processes mediated via protein-protein interactions has generally proved to be a challenging endeavor. In the case of the thrombopoietin receptor (TPOr), howe...
- Reactive derivatives for affinity labeling in the ifenprodil site of NMDA receptors
[作者:Alarcon, K; Martz, A; Mony, L; Neyton, J; Paoletti, P; Goeldner, M; Foucaud, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2765-2770 , 文章类型: Article,,卷期:2008年18-9]
- To prepare thiol-reactive ifenprodil derivatives designed as potential probes for cysteine-substituted NR2B containing NMDA receptors, electrophilic centers were introduced in different areas of the ifenprodil structure....
- In silico multi-filter screening approaches for developing novel beta-secretase inhibitors
[作者:Fujimoto, T; Matsushita, Y; Gouda, H; Yamaotsu, N; Hirono, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2771-2775 , 文章类型: Article,,卷期:2008年18-9]
- A large database of chemical structures was screened for potential inhibitors of beta-secretase was carried out using in silico multi-filter techniques. Substructure screening, computer-aided ligand docking, binding free...
- Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines
[作者:Bardelle, C; 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:2776-2780 , 文章类型: Article,,卷期:2008年18-9]
- A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the...
- Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
[作者:Sbardella, G; Castellano, S; Vicidomini, C; Rotili, D; Nebbioso, A; Miceli, M; Altucci, L; Mai, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2788-2792 , 文章类型: Article,,卷期:2008年18-9]
- Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of ...
- Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases
[作者:Claridge, S; Raeppel, F; Granger, MC; Bernstein, N; Saavedra, O; Zhan, L; Llewellyn, D; Wahhab, A; Deziel, R; Rahil, J; Beaulieu, N; Nguyen, H; Dupont, I; Barsalou, A; Beaulieu, C; Chute, I; Gravel, S; Robert, MF; Lefebvre, S; Dubay, M; Pascal, R; Gillespie, J; Jin, Z; Wang, J; Besterman, JM; MacLeod, AR; Vaisburg, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2793-2798 , 文章类型: Article,,卷期:2008年18-9]
- A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC50 values in the low nanomolar range in vitro while the lead compound also s...
- Synthesis and cytotoxic activity of new 9-substituted camptothecins
[作者:Dallavalle, S; Rocchetta, DG; Musso, L; Merlini, L; Morini, G; Penco, S; Tinelli, S; Beretta, GL; Zunino, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2781-2787 , 文章类型: Article,,卷期:2008年18-9]
- A series of novel 9-substituted camptothecins derived from 9-formylcamptothecin were synthesized. The aldehyde was obtained from 10-hydroxycamptothecin or, better, by total synthesis. The compounds showed antiproliferati...
- Bis-aryl triazoles as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1
[作者:Aster, SD; Graham, DW; Kharbanda, D; Patel, G; Ponpipom, M; Santorelli, GM; Szymonifka, MJ; Mundt, SS; Shah, K; Springer, MS; Thieringer, R; Hermanowski-Vosatka, A; Wright, SD; Xiao, J; Zokian, H; Balkovec, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2799-2804 , 文章类型: Article,,卷期:2008年18-9]
- 3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. T...
- Development of a fluorescence polarization based assay for histone deacetylase ligand discovery
[作者:Mazitschek, R; Patel, V; Wirth, DF; Clardy, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2809-2812 , 文章类型: Article,,卷期:2008年18-9]
- Histone deacetylases (HDACs) regulate many important physiological processes and the discovery of small molecules that modulate HDAC activity has both academic and clinical relevance. HDAC inhibitors, most notably SAHA, ...
- Design of (N)-methanocarba adenosine 5 '-uronamides as species-independent A(3) receptor-selective agonists
[作者:Melman, A; Gao, ZG; Kumar, D; Wan, TC; Gizewski, E; Auchampach, JA; Jacobson, KA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2813-2819 , 文章类型: Article,,卷期:2008年18-9]
- 2-Chloro-5'-N-methylcarboxamidoadenosine analogues containing the (N)-methanocarba (bicyclo[3.1.0] hexane) ring system as a ribose substitute display increased selectivity as agonists of the human A(3) adenosine receptor...
- New tetrazole-based selective anandamide uptake inhibitors
[作者:Ortar, G; Moriello, AS; Cascio, MG; De Petrocellis, L; Ligresti, A; Morera, E; Nalli, M; Di Marzo, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2820-2824 , 文章类型: Article,,卷期:2008年18-9]
- A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC50 = 2.3-5....
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