Synthesis of extended conjugated indolyl chalcones as potent anti-breast cancer, anti-inflammatory and antioxidant agents

Bhale, Pravin S.; Chavan, Hemant V.; Dongare, Sakharam B.; Shringare, Sadanand N.; Mule, Yoginath B.; Nagane, Samadhan S.; Bandgar, B. P.

doi:10.1016/j.bmcl.2017.02.052

Cited by 71 publications

(39 citation statements)

References 42 publications

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“…To the best of our knowledge, antioxidant activity for other nutraceuticals studied in the present investigation has not been yet reported. This prompted us to investigate antioxidant activity of 1–6 NPs and corresponding bulk compounds using in vitro 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging assays . The antioxidant activities are expressed in terms of percentage inhibition as compared to standard ascorbic acid.…”

Section: Resultsmentioning

confidence: 99%

Anticancer, Antioxidant and Antiangiogenic Activities of Nanoparticles of Bioactive Dietary Nutraceuticals

et al. 2019

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Many nutraceuticals are highly potent, nontoxic, bioactive agents present in dietary vegetables, fruits and spices. They exhibit immune‐modulatory, antioxidant and anticancer activity. The major disadvantage of nutraceuticals is their low aqueous solubility and hence poor bioavailability hindering their therapeutic applications. In the present work, we herein report preparation of nanoparticles of bioactive nutraceuticals such as curcumin (1), quercetin (2), anthraquinone (3), xanthone (4), flavone (5) and vanillin (6) with a view to improve their aqueous‐phase solubility and evaluate their anticancer, antiangiogenic and antioxidant activities. The nanoparticles were prepared by controlled flow rate reprecipitation technique and characterized by spectral and microscopic techniques. Most of the nanoparticles displayed higher in‐vitro anticancer, antioxidant and in‐ovo antiangiogenic activities as compared to the corresponding bulk compounds. The biological activities of nutraceuticals are marked increased by particle size reduction to the nanoscale.

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Section: Resultsmentioning

confidence: 99%

Anticancer, Antioxidant and Antiangiogenic Activities of Nanoparticles of Bioactive Dietary Nutraceuticals

et al. 2019

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“…27 The amide-iminol tautomerism in compound 5e helps to promote extensive delocalization of the single electron, resulting in greater stability of the DPPH-generated radical. 28 The enhanced stability caused by the electronenriched extended conjugation of the radical generated in the structure of 5e is likely the cause of its antioxidant activity. and 81.5 ± 0.11% inhibition) ( Figure 8).…”

Section: Dpph Radical Scavenging Assaymentioning

confidence: 99%

Synthesis of E -stilbene azomethines as potent antimicrobial and antioxidant agents

Iqbal¹,

Khan²,

Shahzad³

et al. 2018

Turk J Chem

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A series of new extensively conjugated E-stilbene azomethines (5a-5h) were synthesized and screened for their antioxidant and antimicrobial activity. The compounds were tested against bacterial (Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, and Bacillus subtilis) and fungal strains (Aspergillus niger, A. flavus, and Trichoderma harzianum) using the agar well diffusion method. Among the tested compounds, N '-(4-nitrobenzylidene)-2-((E)-styryl)benzohydrazide (5g) was found to possess potent antimicrobial activity higher than some drugs with significant activity reported in the literature, e.g., cefradine and terbinafine hydrochloride. Additionally, compounds 5a-5h were also evaluated for antioxidant potential using DPPH free radical scavenging and ferric thiocyanate (FTC) assays. Among these, N '-(4-hydroxybenzylidene)-2-((E)-styryl)benzohydrazide (5e) exhibited significant antioxidant potential by both assays. Compound 5e demonstrated higher DPPH free radical scavenging activity (IC 50 = 22 ± 0.19 µ g/mL) than the standard, butylated hydroxytoluene (BHT; IC 50 = 28 ± 0.10 µ g/mL). A similar trend was observed for compound 5e in FTC assay, which exhibited 86 ± 0.19% inhibition, whereas the BHT control showed 81 ± 0.21% inhibition of linoleic acid peroxidase. The structure elucidation of the synthesized compounds was carried out by UV-Vis, FT-IR, 1 H NMR, 13 C NMR, and elemental analysis and mass spectrometry. These results suggest possible use of these compounds for the rational design of new antimicrobial and antioxidant agents.

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“…As important natural products, flavonoids, and isoflavones exist in edible plants . Chalcone belongs to the core skeleton unit of isoflavones and flavonoids, having a broad‐spectrum of biological activities such as anti‐inflammatory, antibacterial, antiproliferative, insecticidal, antioxidant, antiviral, antifungal, and anticancer . Chu et al reported a series of chalcone derivatives with cationic antimicrobial peptides, and showed that the resistant bacteria MRSA, KPC, and NDM have good bactericidal activities .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antibacterial activity of chalcone derivatives containing thioether triazole

Chen

et al. 2020

Journal of Heterocyclic Chem

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The infection of Xanthomonas oryzae pv. Oryzae (Xoo), Ralstonia solanacearum (Rs), and Xanthomonas axonopodis pv. Citri (Xac) has become a major problem in agricultural production. In this study, a series of novel chalcone derivatives containing thioether triazoles were designed and synthesized. The structures of the novel compounds were systematically characterized via 1H‐NMR, 13C‐NMR, and HRMS. Moreover, the antibacterial activity results showed that E10, E11, E15, and E16 have adequate antibacterial activities against Xoo, Rs, and Xac. Among the different compounds, E15 exhibited remarkable inhibitory effect against Xac with an EC50 of 9.1 μg.mL‐1, which was better than that of commercial agent bismerthiazol (54.9 μg.mL‐1). In addition, the possible antibacterial mechanism of the target compound E15 against Xac was studied via scanning electron microscopy (SEM).

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Synthesis of extended conjugated indolyl chalcones as potent anti-breast cancer, anti-inflammatory and antioxidant agents

Cited by 71 publications

References 42 publications

Anticancer, Antioxidant and Antiangiogenic Activities of Nanoparticles of Bioactive Dietary Nutraceuticals

Anticancer, Antioxidant and Antiangiogenic Activities of Nanoparticles of Bioactive Dietary Nutraceuticals

Synthesis of E -stilbene azomethines as potent antimicrobial and antioxidant agents

Synthesis and antibacterial activity of chalcone derivatives containing thioether triazole

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