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doi:10.26655/jmchemsci.2022.4.16

Cited by 6 publications

(6 citation statements)

References 49 publications

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“…The synthesised fused coumarin compounds, along with their control substance, were solubilized in DMSO to obtain seven different concentration levels (400.00, 200.00, 100.00, 50.00, 25.00, 12.50, and 6.25 µg/ml). Then, they were tested against six tumorigenic cell lines: KYSE-30, SK-OV-3, SKG, AMN3, HeLa, and MCF-7 [31,32]. The tested tumorous cell lines were used to obtain 10,000 cells per well by dividing them into a 96well plate, and each well was treated independently with varying doses of the synthesised fused coumarin compounds after 24 hours.…”

Section: In-vitro Biological Potentials Apoptotic-inducing Activitymentioning

confidence: 99%

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2022

J. Med. Chem. Sci.

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This work involves the synthesis of eight novel fused coumarin compounds, which were confirmed by various spectrophotometers and then, assessed for their apoptotic-inducing and free radical-quenching activities. The pharmacokinetic parameters were evaluated in silico using pre-ADMET, a free online program. The apoptotic-inducing activity was tested against six tumorigenic cell lines. Also, their safety against normal cells was examined. The free radical-quenching activity was assessed by checking these compounds' ability to eliminate DDPT and hydroxyl moieties. Pharmacokinetic investigations showed that the synthesized fused coumarin compounds have excellent penetration across the GIT mucosa and most of them have poor penetration across the blood-brain barrier. These findings suggest good oral bioavailability along with low neurological toxicity profiles. The evaluation of the apoptotic-inducing activity revealed that all of the compounds have weaker activity as compared to the reference. Among these compounds, SA4 was the most potent one. Nevertheless, all of these new compounds had an excellent safety profile against normal cells. On the other hand, the assessment of the free radical-quenching activity of these synthesized compounds also indicated that all of them were less active than the reference. In this field, SA0 was the strongest free radical-quenching compound. From these realizations, along with the apparent safety and good pharmacokinetic characteristics in accordance with the in silico study, compounds SA4 and SA0 are considered the most promising agents. The authors hope that these new fused coumarin compounds can be utilized in the coming years for the production of new powerful drugs with apoptoticinducing and free radical-quenching potentials which can help in the battle against many diseases.

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Section: In-vitro Biological Potentials Apoptotic-inducing Activitymentioning

confidence: 99%

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2022

J. Med. Chem. Sci.

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“…As the reaction was finished, H2O (50 mL) was added to the mixture, and the organic layer was separated, dehydrated, and vaporized. The SY congener was acquired [29,30] by the recrystallization of a mixture of propanone and CH2Cl2 (1:2). SY2:…”

Section: Synthetic Technique Of Sy2-sy7 Congenersmentioning

confidence: 99%

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2022

J. Med. Chem. Sci.

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“…However, its most important usage is to synthesize different products in the pharmaceutical industry [7]. Coumarins, from natural and/or synthetic sources have different biomedical potentials, such as anti-diabetic [8,9], anti-viral [10,11], anti-tubercular [12], anti-fungal [13][14][15], anti-coagulant [16,17], anti-cancer [18][19][20][21][22], anti-bacterial [23][24][25][26][27], and antioxidant [28][29][30][31] properties. Moreover, these molecules have many appealing characteristics, such as low toxicity, high bioavailability, simple planar structure, and low molecular weight, which confirm that they could play a significant role in drug development and research [32][33][34].…”

Section: Introductionmentioning

confidence: 99%

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2022

J. Med. Chem. Sci.

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In recent times, many researchers in pharmaceutical chemistry have been preoccupied with the quest for new potent anti-infective agents to combat antimicrobial resistance. A novel series of naphthalene-based derivatives were synthesized as part of these studies. Different spectral techniques, such as UV-Vis, FTIR, 13C-NMR, and 1H-NMR were used to affirm the synthesized compounds' chemical structures, while an ADME study was conducted to investigate their pharmacokinetics and drug-like properties. The potential of the synthesized naphthalene-based derivatives as anti-infective candidates versus pathogenic microbes was evaluated using a broth microdilution assay. These microbes involved six aerobic gram-negative bacteria, four anaerobic bacteria, and two fungi. In addition, their safety was assessed versus normal bacterial flora. From the obtained results, the authors reported the following principal outcomes: Compound SF5 revealed a significant aerobic gram-negative bactericidal impact while indicating high safety versus the non-pathological bacterial strain. Most of the synthesized naphthalene-based derivatives demonstrated outstanding potential as fungicidal candidates, but compound SF1 was the most potent one. According to ADME analysis, almost all of the synthesized derivatives have good theoretical pharmacokinetics and drug-likeness characteristics making them suitable as oral-derived agents.

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Cited by 6 publications

References 49 publications

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