- A two step synthesis of BzR/GABAergic active flavones via a Wacker-related oxidation
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A general route for the synthesis of biologically important flavones is reported via a two step sequence employing a catalytic Wacker-Cook oxidation4b as the key step.
- Lorenz, Michael,Shahjahan Kabir,Cook, James M.
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experimental part
p. 1095 - 1098
(2010/04/05)
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- Use of nitroflavonoids for the treatment of anxiety
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PCT No. PCT/GB96/02523 Sec. 371 Date Jul. 8, 1998 Sec. 102(e) Date Jul. 8, 1998 PCT Filed Oct. 16, 1996 PCT Pub. No. WO97/14414 PCT Pub. Date Apr. 24, 1997Methods of treating anxiety with flavonoid compounds according to Formula (I) and dimers thereof, co
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- Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor
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A series of halogenated/nitrated flavone compounds were synthesized. Some of the products were found to be potent central benzodiazepine receptor (BDZ-R) ligands. The structure-activity relationships (SAR) analysis of the new synthetic compounds, together with that of others already described, indicates that substitutions at position 6 or 6 and 3' in the flavone nucleus are the only ones that give rise to high affinity BDZ-R ligands.
- Marder, Mariel,Zinczuk, Juan,Colombo, Maria I.,Wasowski, Cristina,Viola, Haydee,Wolfman, Claudia,Medina, Jorge H.,Ruveda, Edmundo A.,Paladini, Alejandro C.
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p. 2003 - 2008
(2007/10/03)
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- Synthesis and Biochemical Evaluation of a Series of Aminoflavones as Potential Inhibitors of Protein-Tyrosine Kinases p56lek, EGFr, and p60v-src
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A series of nitroflavones, 8a-p, and their corresponding aminoflavone hydrochloride salts, 10a-p, was synthesized.The preparation of nitroflavones 8b-i,o,p began with commercially available o-hydroxyacetophenones 2b-f which were converted to o-hydroxynitroacetophenones 3a-h via a variety of nitration methods, followed by condensation with nitrobenzyl chlorides and cyclization under acidic condition.The nitroflavones 8a,j-n were prepared by nitration of the corresponding flavones 7a-e.These new compounds were evaluated for their abilities to inhibit the in vitro protein-tyrosine kinase activities of p56lek, EGFr, and p60v-src, and all of the active compounds were amino-substituted flavones.None of the nitroflavones inhibited the enzymes.The most active substance in this series against p56lek was compound 10j, which had an IC50 of 18 μM.When tested versus EGFr, compounds 10a,m displayed IC50's of 8.7 and 7.8 μM, respectively.Against p60v-src, 10a,m showed IC50 values of 28.8 and 38.4 μM, respectively.
- Cushman, Mark,Zhu, Helen,Geahlen, Robert L.,Kraker, Alan J.
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p. 3353 - 3362
(2007/10/02)
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