Showing 1-13 of 13 results for "128724"
K Takagaki et al.
Journal of biochemical and biophysical methods, 19(2-3), 207-214 (1989-08-01)
The present paper describes a fluorometric assay for galactosaminoglycan-degrading endo-beta-xylosidase, utilizing glycosaminoglycan chains bearing a 4-methylumbelliferyl group at the reducing terminus as a substrate. This fluorogenic substrate is synthesized by human skin fibroblasts cultured in the presence of a fluorogenic...
Juri M Timonen et al.
European journal of medicinal chemistry, 46(9), 3845-3850 (2011-06-18)
A number of 7-hydroxycoumarins have been synthesised by Pechmann cyclisation using differently substituted resorcinols employing perchloric acid as the condensing agent. All the compounds have been characterised by analytical and spectroscopic methods. The anti-inflammatory properties were tested with LPS-induced inflammation...
Lourdes Santana et al.
Journal of medicinal chemistry, 51(21), 6740-6751 (2008-10-07)
The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, we prepared and assayed 33 coumarin derivatives...
Laura Piccagli et al.
Bioorganic & medicinal chemistry, 18(23), 8341-8349 (2010-10-29)
In the present study, a structured-based virtual screening (VS) of differently substituted furocoumarins and analogues has been carried out against nuclear factor kappa B (NF-κB), with the objective of selecting molecules able to inhibit the binding of this transcription factor...
Atsushi Kato et al.
Bioorganic & medicinal chemistry letters, 20(19), 5630-5633 (2010-09-02)
We report the structure-activity relationship of a series of coumarins as aldose reductase 2 (ALR2) inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens. We evaluated their ALR2 selectivity profile against sorbitol dehydrogenase and aldehyde...
Joanna Trykowska Konc et al.
European journal of medicinal chemistry, 46(6), 2252-2263 (2011-03-29)
A series of novel O-aminoalkyl substituted 7-hydroxycoumarins were synthesized and evaluated for antibacterial and anticancer toxicity. Two different synthetic procedures, conventional and microwave assisted were used, and the structures of the compounds were confirmed by IR, 1H, 13C NMR and...
Koichiro Harada et al.
Bioorganic & medicinal chemistry letters, 20(1), 272-275 (2009-12-04)
The synthesis and SAR studies of 3- and 4-substituted 7-hydroxycoumarins as novel 17beta-HSD3 inhibitors are discussed. The most potent compounds from this series exhibited low nanomolar inhibitory activity with acceptable selectivity versus other 17beta-HSD isoenzymes and nuclear receptors.
Maria E Riveiro et al.
Bioorganic & medicinal chemistry, 16(5), 2665-2675 (2007-12-07)
In the present study, we sought to establish the effect of diverse structural-related hydroxycoumarins on the proliferation, cytotoxicity, and induction of apoptosis in promonocytic leukemic cells (U-937). The dihydroxylated coumarins, 7,8-dihydroxy-coumarin and esculetin, induced DNA fragmentation as well as characteristic...
Gavin J Williams et al.
Nature chemical biology, 3(10), 657-662 (2007-09-11)
Natural products, many of which are decorated with essential sugar residues, continue to serve as a key platform for drug development. Adding or changing sugars attached to such natural products can improve the parent compound's pharmacological properties, specificity at multiple...
Adriana Chilin et al.
Journal of medicinal chemistry, 51(4), 752-759 (2008-02-07)
Casein kinase 2 (CK2) is an ubiquitous, essential, and highly pleiotropic protein kinase whose abnormally high constitutive activity is suspected to underlie its pathogenic potential in neoplasia and other diseases. Recently, using different virtual screening approaches, we have identified several...
Sergio A Rodríguez et al.
Bioorganic & medicinal chemistry, 19(21), 6233-6238 (2011-10-04)
The antioxidant activity of 4-hydroxycoumarin synthetic derivatives and 4-methylumbelliferone were determined taking 4-hydroxycoumarin as the reference compound. Six 3-aryl-4-hydroxycoumarin derivatives were synthesized from 4-hydroxycoumarin as precursor in order to evaluate changes in their antioxidant properties due to C3-aryl substituent nature....
Nadia Touisni et al.
Journal of medicinal chemistry, 54(24), 8271-8277 (2011-11-15)
A series of 7-substituted coumarins incorporating various glycosyl moieties were synthesized and investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC These coumarins were very weak or ineffective as inhibitors of the housekeeping, off target isoforms...
Yuan Shi et al.
Bioorganic & medicinal chemistry letters, 21(3), 956-960 (2011-01-11)
A series of new coumarin-based 1,2,4-triazole derivatives were designed, synthesized and evaluated for their antimicrobial activities in vitro against four Gram-positive bacteria (Staphylococcus aureus, MRSA, Bacillus subtilis and Micrococcus luteus), four Gram-negative bacteria (Escherichia coli, Proteus vulgaris, Salmonella typhi and...

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