Synthesis and biological evaluation of novel series of chalcone derivatives as inhibitors of cyclooxygenase and LPS-induced TNF-α with potent antioxidant properties

Bandgar, B. P.; Hote, Baliram S.; Dhole, N.A.; Gacche, Rajesh N.

doi:10.1007/s00044-011-9746-6

Cited by 13 publications

(5 citation statements)

References 30 publications

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“…Especially, 4-methylcoumarin is a popular scaffold for constructing novel antioxidants. 11e13 On the other hand, chalcones also possess various biological properties 14 including antioxidant 15 and anticancer activities, 16 and are usually applied as a basic structure for preparing novel antioxidants. 17 In our previous work, we found that the inhibitory effect of 4-methylcoumarin on the radical-mediated oxidation of DNA can be increased by the moiety of 4,5-dihydropyrazole.…”

Section: Introductionmentioning

confidence: 99%

Coumarin moiety can enhance abilities of chalcones to inhibit DNA oxidation and to scavenge radicals

Liu

2014

Tetrahedron

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Section: Introductionmentioning

confidence: 99%

Coumarin moiety can enhance abilities of chalcones to inhibit DNA oxidation and to scavenge radicals

Liu

2014

Tetrahedron

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“…The B3LYP method was employed with the 6-31G(d) basis set that was used in the PCgamess program, and further single point calculations were done for the obtained optimised geometries [18]. The inhibition of LPS-induced TNP-α production by 15 compounds that were studied was all taken from the reference [19].…”

Section: Methodsmentioning

confidence: 99%

Quantitative Structure-Activity Relationship Studies Of Series Of Chalcones Derivatives as Inhibitors Of Tumor Necrosis Factor-Alpha

Alhassan

Ismae²,

Alshawi³

2020

Al-Qadisiyah Journal of Pure Science

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Quantitative structure-activity relationship (QSAR) teqnique was used to predict the biological activity of a series of chalcones compounds as anti-inflammatory. 26 physicochemical descriptors are tested in QSAR equations configuration to predict biological effectiveness of compounds under study. The values of R2 in Eqs (1–3) ranged from 0.794–0.873, the F values ranged from 14.161–26.206 and the S values ranged from 0.262–0.334. The results demonstrated excellent models based on Eq.3, along with high of R2, F and minimum S by employing three parameters r(C3-C5), (LUMO+1) and (LUMO+2). This signifies that these parameters play a significant role in determining anti-inflammatory characteristics.

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“…Additionally, the authors postulated anti-proliferative and anti-carcinogenic activity. Chalcones (isosalipurposid and its derivatives) and flavanones (naringenin and its glucosides) are known to enhance spasmolytic and anti-inflammatory activity ( Bandgar et al, 2012 ; Letafat et al, 2013 ). For catechin and epicatechin a lot of pharmacological effects like anti-oxidative, anti-carcinogenic, or cardioprotective effects were reported ( Ganeshpurkar and Saluja, 2020 ).…”

Section: Introductionmentioning

confidence: 99%

Chemoprofiling as Breeding Tool for Pharmaceutical Use of Salix

et al. 2021

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Willow bark is traditionally used for pharmaceutical purposes. Evaluation is so far based on the salicylate content, however, health promoting effects of extracts might be attributed to the interaction of those salicylates with other compounds, which support and complement their action. So far, only S. purpurea, S. daphnoides, and S. fragilis are included in pharmaceutical extracts. Crossing with other species could result in a more diverse secondary metabolite profile with higher pharmacological value. With the help of targeted inter- and intraspecific crossing, new chemotypes were generated, whereby nine different Salix genotypes (S. alba, S. daphnoides, S. humboldtiana, S. lasiandra, S. nigra, S. pentandra, S. purpurea, S. x rubens, S. viminalis) were included in the study. Based on substances known for their health promoting potential and characteristic for Salix (selected phenolic compounds including salicylates), a targeted metabolomics analysis and clustering of 92 generated Salix clones was performed revealing four different cluster/chemoprofiles. In more specific, one group is formed by S. daphnoides clones and inter- and intraspecific hybrids, a second group by S. viminalis clones and inter- and intraspecific hybrids, a third group generally formed by S. alba, S. pentandra, S. x rubens, and S. lasiandra clones and hybrids, and a fourth group by S. purpurea clones and inter- and intraspecific hybrids. Clustering on the basis of the selected phenolic compounds can be used for identifying Salix clones with a different compound profile. New combinations of secondary plant metabolites offer the chance to identify Salix crosses with improved effects on human health.

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Synthesis and biological evaluation of novel series of chalcone derivatives as inhibitors of cyclooxygenase and LPS-induced TNF-α with potent antioxidant properties

Cited by 13 publications

References 30 publications

Coumarin moiety can enhance abilities of chalcones to inhibit DNA oxidation and to scavenge radicals

Coumarin moiety can enhance abilities of chalcones to inhibit DNA oxidation and to scavenge radicals

Quantitative Structure-Activity Relationship Studies Of Series Of Chalcones Derivatives as Inhibitors Of Tumor Necrosis Factor-Alpha

Chemoprofiling as Breeding Tool for Pharmaceutical Use of Salix

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