2009
DOI: 10.1055/s-0029-1234266
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The characterization, total synthesis and antiprotozoal activities of novel bichalcones from Rhus pyroides

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Cited by 6 publications
(9 citation statements)
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“…This plant is also known to be the sources of several O-linked and C-C coupled bichalcones ( Figure 2 ) and biflavonoids, some of which have been obtained by total synthesis [ 48 , 49 , 50 , 51 , 52 ]. The bichalcones and their analogues are known to possess cytotoxic [ 47 ], antiprotozoal [ 48 , 49 ] and carbonic anhydrase inhibitory [ 50 ] activities. Meanwhile, biflavones from this plant, e.g., agathisflavone and amentoflavone have shown an affinity for the GABA A /benzodiazepine receptor [ 51 ].…”
Section: Discussionmentioning
confidence: 99%
“…This plant is also known to be the sources of several O-linked and C-C coupled bichalcones ( Figure 2 ) and biflavonoids, some of which have been obtained by total synthesis [ 48 , 49 , 50 , 51 , 52 ]. The bichalcones and their analogues are known to possess cytotoxic [ 47 ], antiprotozoal [ 48 , 49 ] and carbonic anhydrase inhibitory [ 50 ] activities. Meanwhile, biflavones from this plant, e.g., agathisflavone and amentoflavone have shown an affinity for the GABA A /benzodiazepine receptor [ 51 ].…”
Section: Discussionmentioning
confidence: 99%
“…4) and biflavonoids, some of which have been obtained by total synthesis [48][49][50][51][52]. The rhuschalcones and their analogues are known to possess cytotoxic [47], antiprotozoal [48,49] and carbonic anhydrase inhibitory [50] activities.…”
Section: Discussionmentioning
confidence: 99%
“…Molecular docking studies onto available sirt1 and sirt2 crystal structures resulted in two sirt1 and sirt2 inhibitors with moderate inhibitory effect. Although the rhuschalcones 8 and 9 have been known to possess other biological activities [47][48][49][50][51][52], it is yet unclear if their cytotoxicities are related to their abilities to inhibit sirtuins. However, natural product libraries like the p-ANAPL and the newly developed NANPDB [70] libraries could be good sources to search for novel modulators of sirtuins with novel scaffolds.…”
Section: Discussionmentioning
confidence: 99%
“…These compounds were shown to be active in the in vitro assay, with the best activity against sirt1 being an IC50 value of 40.8 µM for the rhuschalcone I analogue. Although several known O-linked and C-C coupled bichalcones, and biflavonoids from this plant were not tested in the assays, [122][123][124][125] research of novel more potent and selective bichalcones as sirtuin inhibitors lies in the fact that their total synthesis has been described [122][123][124][125]. It must, however, be mentioned that this class of compounds has shown diverse biological activities, e.g.…”
Section: Bichalcones From the African Medicinal Plant Rhuspyroidesmentioning
confidence: 99%
“…It must, however, be mentioned that this class of compounds has shown diverse biological activities, e.g. cytotoxic, antiprotozoal [122][123], carbonic anhydrase inhibitory activities [124], as well as an affinity for the GABAA/benzodiazepine receptor [125].…”
Section: Bichalcones From the African Medicinal Plant Rhuspyroidesmentioning
confidence: 99%