- Design, Synthesis, and Biological Evaluation of Quercetagetin Analogues as JNK1 Inhibitors
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The recent discovery of c-Jun NH2-terminal kinase JNK1 suppression by natural quercetagetin (1) is a promising lead for the development of novel anticancer agents. Using both X-ray structure and docking analyses we predicted that 5′-hydroxy- (2
- Hierold, Judith,Baek, Sohee,Rieger, Rene,Lim, Tae-Gyu,Zakpur, Saman,Arciniega, Marcelino,Lee, Ki Won,Huber, Robert,Tietze, Lutz F.
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supporting information
p. 16887 - 16894
(2015/11/16)
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- Synthesis of two unnatural oxygenated aaptaminoids
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Two unprecedented oxygenated aaptaminoids have been synthesized starting from cheap and easily available 2,3-dihydroxybenzoic acid with the satisfactory overall yields of 31% and 34%. The key step of the procedure is the divergent thermic 5-exodig vs base
- Abbiati, Giorgio,Doda, Arjana,Dell'Acqua, Monica,Pirovano, Valentina,Facoetti, Diego,Rizzato, Silvia,Rossi, Elisabetta
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p. 10461 - 10467
(2013/01/15)
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- Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson's agents
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A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives was prepared and their evaluation for anti-Parkinson's activity was measured in vivo using albino rats. The result of the biological activity studies indicated that some of the
- Tiwari, Shashi B.,Kohli
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p. 386 - 398
(2008/12/22)
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- In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D2-like dopamine receptors
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Benzamide derivatives as radiotracers have played an important role in diagnosing malfunction in dopaminergic neurotransmission. A variety of halogenated and two unsubstituted benzamide derivatives were synthesised and their in vitro affinities to dopaminergic, serotonergic and adrenergic receptors and their lipophilicities were determined. As references IBZM (3), raclopride (4) and FLB457 (5) were tested as well. The two iodinated compounds NAE (27) and NADE (28) displayed Ki values of 0.68 and 14 nM for the D2 receptor. The well-established radiotracers FP (1) and DMFP (2) showed affinities in the same range as did the brominated compounds NABrE (29) and NABrDE (30). The log D7.4 values of 2.91 for NAE (27) and of 2.81 for NADE (28) are in the range of those found for IBZM (3), FP (1) and DMFP (2). These facts allow to expect good properties for the two iodinated compounds NAE (27) and NADE (28) regarding in vivo imaging with SPECT.
- Stark, Daniela,Piel, Markus,Huebner, Harald,Gmeiner, Peter,Gruender, Gerhard,Roesch, Frank
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p. 6819 - 6829
(2008/03/27)
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- Synthesis of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole analogues and their binding affinities for dopamine D2 and D3 receptors
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A series of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole derivatives was prepared and their affinity for dopamine D2 and D3 receptors was measured using in vitro binding assays. Several oxadiazole analogues were also prepared and tested for their affinity for dopamine D2 and D3 receptors. The results of receptor binding studies indicated that the incorporation of an imidazole moiety between the phenyl ring and the basic nitrogen did not significantly increase the selectivity for dopamine D3 receptors, whereas the incorporation of an oxadiazole at the same region resulted in a total loss of affinity for both dopamine receptor subtype binding sites. The most selective compound in this series is 2-(5-bromo-2,3-dimethoxyphenyl)-4-(6,7-dimethoxy-1,2,3, 4-tetrahydroisoquinolinomethyl)imidazole (5i), which has a D3 receptor affinity of 21 nM and a 7-fold selectivity for D3 versus D2 receptors. The binding affinity for σ1 and σ2 receptors was also measured, and the results showed that several analogues were selective σ1 receptor ligands.
- Huang, Yunsheng,Luedtke, Robert R.,Freeman, Rebekah A.,Wu, Li,Mach, Robert H.
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p. 3113 - 3122
(2007/10/03)
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- Improved specific radioactivity of the PET radioligand [11C]FLB 457 by use of the GE Medical Systems PETtrace MeI MicroLab
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[11C]FLB 457 is a high affinity dopamine D2 receptor radioligand that is used for visualisation and quantitation of extrastriatal dopamine D2 receptors with positron emission tomography (PET). In this study, we report a co
- Sandell, Johan,Langer, Oliver,Larsen, Peter,Dolle, Frederic,Vaufrey, Francoise,Demphel, Stephane,Crouzel, Christian,Halldin, Christer
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p. 331 - 338
(2007/10/03)
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- Structure-activity relationship studies of N-(9-benzyl)-9- azabicyclo[3.3.1]nonan-3-β-yl benzamide analogues for dopamine D2 and D3 receptors
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A series of benzamide derivatives were prepared in order to determine the nature of the substituent effects in the benzamide aromatic ring on the affinity to dopamine D2 and D3 receptors. Both quantitative structure- activity relatio
- Mach, Robert H.,Hammond, Philip S.,Huang, Yunsheng,Yang, Biao,Xu, Yueping,Cheney, Jason T.,Freeman, Rebekah,Luedtke, Robert R.
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p. 355 - 373
(2007/10/03)
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- Facile preparation of (S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2,3-dimethoxy-5- (tributyltin)benzamide from isoremoxipiride: The precursor of [125I]- and [123I]epidepride
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[125I]Epidepride, (S)-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo-2,3- dimethoxybenzamide ([125I]NCQ 219), is a new, extremely potent radioligand, useful in the study of the distribution of the dopamine D-2 recepto
- De Paulis,Smith
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p. 1091 - 1095
(2007/10/02)
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- SYNTHESIS OF 5-HALOGEN-SUBSTITUTED 2,3-DIHYDROXYPHENYLACETIC ACIDS, THEIR ESTERS, AND 2,3-DIMETHOXYPHENYLACETOHYDROXAMIC ACIDS
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Many-stage general methods were developed for the synthesis of 5-bromo- or 5-chloro-substituted 2,3-dimethoxyphenylacetic acids from o-vanilin.Methods were also developed for their conversion into the corresponding hydroxamic acids, 2,3-dihydroxyphenylace
- Daukshas, V. K.,Martinkus, R. S.,Kuleshyus, V. A.,Shtel'bene, V. P.
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p. 458 - 463
(2007/10/02)
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