Synthesis, Cytotoxic Evaluation, and Molecular Docking Studies of N-(7- hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide/benzamide Analogues

Ahsan, Mohamed Jawed; Kumawat, Rupesh Kumar; Jadav, Surender Singh; Geesi, Mohammed H.; Bakht, Md. Afroz; Hassan, Mohd. Zaheen; Al-Tamimi, Abdulmalik Bin Saleh; Riadi, Yassine; Salahuddin,; Hussain, Afzal; Ganta, Narayana Murthy; Khalilullah, Habibullah

doi:10.2174/1570180815666180501160047

Cited by 4 publications

(2 citation statements)

References 15 publications

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“…GI 50 is the concentration that causes 50% inhibition of cell growth. 51 Ribeiro et al 47 used magnetoliposome for co-delivery of PTX and gemcitabine. They evaluated the cytotoxicity effects of the resulting formulation against human breast cancer MGSO-3 cells.…”

Section: Discussionmentioning

confidence: 99%

In vitro Assessment of Magnetic Liposomal Paclitaxel Nanoparticles as a Potential Carrier for the Treatment of Ovarian Cancer

et al. 2020

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Purpose: This study aimed to evaluate the role of magnetic liposome nanoparticles (ML NPs) as a carrier for paclitaxel (PTX) for the treatment of ovarian cancer in vitro . Methods: Magnetic NPs (MNPs) were synthesized by chemical co-precipitation method. The resulting NPs were characterized in terms of size, size distribution, zeta potential, drug encapsulation efficiency (EE), drug release pattern, and cytotoxicity effects. Results: The size and zeta potential of PTX-PEG-L and PTX-PEG-ML NPs were determined to be 296, 198 nm; -20, and -19 mV, respectively. Also, their drug encapsulation efficiencies were determined to be 97% and 96%, respectively. It was found that PTX-PEG-ML NPs, compared to PTX-PEG-L NPs, caused a reduction (11%) in the rate of drug release. The cytotoxicity of the drug-loaded NPs was assessed using 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay against human ovarian epithelial cancer (A2780CP) cells, and the results demonstrated that PTX-PEG-ML NPs caused higher cytotoxicity (by 14%) compared to PTX-PEG-L NPs (IC 50 : 1.88 ± 0.09 and 2.142 ± 0.1 µM, respectively). Conclusion: Overall, the results of this study suggest that PTX-PEG-ML NPs could be considered as a therapeutic candidate for the treatment of ovarian cancer.

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Section: Discussionmentioning

confidence: 99%

In vitro Assessment of Magnetic Liposomal Paclitaxel Nanoparticles as a Potential Carrier for the Treatment of Ovarian Cancer

et al. 2020

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“…In light of the aforementioned data, we report herein the synthesis of novel hybrid molecules that covalently connect 4-methyl-(1H)-quinolin-2-one and benzimidazole via a triazole ring. Although much work has been done to assess the biological potency of 4-methyl substituted 2-quinolone [32][33][34], its 6-halogeneted derivatives are still insufficiently studied. Hence, we elected to use 6bromo/fluoro-4-methyl-(1H)-quinolin-2-one as a starting point for producing new potential antibiotics.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, structural characterization and antibacterial activity evaluation of novel quinolone-1,2,3-triazole-benzimidazole hybrids

Gadali¹,

Rafya²,

Mansouri

et al. 2023

Journal of Molecular Structure

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Synthesis and Biological Evaluations of N-(4-Substituted Phenyl)-7-Hydroxy-4-Methyl-2-Oxoquinoline-1(2H)-Carbothioamides

Ali

Salahuddin³

et al. 2021

Polycyclic Aromatic Compounds

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The chemicals were purchased from CDH, Merck and Spectrochem (India). The melting point was recorded through open capillary method and was uncorrected. The progress or reaction was monitored by thin layer chromatography (TLC Silica gel 60 F254) and benzene/methanol (8:2) was used as eluent. The spots were visualized under iodine vapors or UV light. IR spectra were recorded on a Bruker Alpha II FT-IR spectrometer, while the nuclear magnetic resonance spectra were recorded on a Bruker AvIII HD-300 ( 1 H NMR at 300 MHz and 13 C NMR at 75 MHz) in DMSO-d6. The mass spectra were recorded on a Waters ACQUITY® TQD LCMS using ESI. General method for the synthesis of N-(4-substituted phenyl)-7-hydroxy-4-methyl-2oxoquinoline-1(2H)-carbothioamides (5a-g)An equimolar amount of 7-hydroxy-4-methyl coumarin (3) (1mmol; 176 mg) and substituted phenyl thiourea (4a-g) (1 mmol) was fused together at 200 ºC on oil bath for 1 h. The reaction mixture was then cooled and 5 mL ethanol was added followed by addition of 5 mL water. The separated solid was collected by vacuum filtration, washed with water, dried and re-crystallizes from acetic acid. N-(4-Chlorophenyl)-7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-carbothioamide (5a) IR 3406

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Synthesis, Cytotoxic Evaluation, and Molecular Docking Studies of N-(7- hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide/benzamide Analogues

Cited by 4 publications

References 15 publications

In vitro Assessment of Magnetic Liposomal Paclitaxel Nanoparticles as a Potential Carrier for the Treatment of Ovarian Cancer

In vitro Assessment of Magnetic Liposomal Paclitaxel Nanoparticles as a Potential Carrier for the Treatment of Ovarian Cancer

Synthesis, structural characterization and antibacterial activity evaluation of novel quinolone-1,2,3-triazole-benzimidazole hybrids

Synthesis and Biological Evaluations of N-(4-Substituted Phenyl)-7-Hydroxy-4-Methyl-2-Oxoquinoline-1(2H)-Carbothioamides

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