Design and Synthesis of Novel 5-(4-chlorophenyl)furan Derivatives with Inhibitory Activity on Tubulin Polymerization

Moussa, Shaimaa A.; Osman, Essam Eldin A.; Eid, Nahed M.; Abou‐Seri, Sahar M.; Moghazy, Samir M. El

doi:10.4155/fmc-2018-0036

Cited by 3 publications

(2 citation statements)

References 24 publications

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“…rotator at 4 °C for 30 min, and were added to each well for 2 h at 37 °C. The plates were then read on a scintillation counter (Topcount Microplate Reader, Packard Instruments, Winooski, VT, USA) [ 48 , 49 ].…”

Section: Methodsmentioning

confidence: 99%

“…Premix tubulin-biotine-streptavidin scintillation proximity assay beads (180 mL; 4.4 mg streptavidin yttrium silicate beads (Amersham Bioscience, London, UK) are mixed into 15 mL buffer and incubated on a slow 10 r.p.m. rotator at 4 • C for 30 min, and were added to each well for 2 h at 37 • C. The plates were then read on a scintillation counter (Topcount Microplate Reader, Packard Instruments, Winooski, VT, USA) [48,49].…”

Section: Colchicine Site Competitive Binding Assaymentioning

confidence: 99%

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Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

et al. 2020

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A novel series of quinoline derivatives of combretastatin A-4 incorporating rigid hydrazone and a cyclic oxadiazole linkers were synthesized and have demonstrated potent tubulin polymerization inhibitory properties. Many of these novel derivatives have shown significant antiproliferative activities in the submicromolar range. The most potent compound, 19h, demonstrated superior IC50 values ranging from 0.02 to 0.04 µM against four cancer cell lines while maintaining low cytotoxicity in MCF-10A non-cancer cells, thereby suggesting 19h’s selectivity towards proliferating cancer cells. In addition to tubulin polymerization inhibition, 19h caused cell cycle arrest in MCF-7 cells at the G2/M phase and induced apoptosis. Collectively, these findings indicate that 19h holds potential for further investigation as a potent chemotherapeutic agent targeting tubulin.

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Section: Methodsmentioning

confidence: 99%

Section: Colchicine Site Competitive Binding Assaymentioning

confidence: 99%

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

et al. 2020

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Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study

Mustafa

Anwar

Elgamal

et al. 2019

European Journal of Medicinal Chemistry

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Cytotoxicity, in silico predictions and molecular studies for androstane heterocycle compounds revealed potential antitumor agent against lung cancer cells

Tantawy

Shaheen

Kattan

et al. 2020

Journal of Biomolecular Structure and Dynamics

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Full methodologies for MTT assay, Tubulin assay, flow cytometry, DNA fragmentation, RT-PCR genes expression analysis, and docking results for other compounds are supported as supplementary 1. Cell cultures and MTT assay A549, MCF-7 and GMSC cell lines were provided from the American Type Culture Collection (ATCC, USA) via VACERA Co. (Egypt). Cells were maintained and propagated in proper complete RPMI-1640/DMEM media l-Glutamine (Lonza Verviers SPRL, Belgium, cat#12-604F) which supplemented with 10% fetal bovine serum (FBS) (Seralab, UK, cat# EU-000-H), and 1% antibiotic (Antibiotic antimycotic, Biowest, cat# L0010). The cells were reared in humidified incubator with 5% CO2 at 37 °C, sub-cultured using 0.25% (w/v) trypsin/EDTA, and then counted using trypan blue staining and investigated under inverted microscope according to the standard tissue culture technique.The cytotoxic effects of the tested heterocyclic steroids on A549, MCF-7 and GMSC cell lines were evaluated by the cell viability colorimetric assay using MTT (3-[4,5methylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) dye. 5-FU is a standard reference drug was used as a positive control. Briefly, cell line (1×10 4 cells/well) were seeded in a 96-well plate in triplicate and were allowed to adhere for 24 h. Compounds were dissolved in 500 µl Dimethyl sulfoxide (DMSO) to have stock solution of 100 mM, then various concentrations of the tested derivatives or 5-FU were prepared by diluting in complete medium to have four final concentration of 1, 10, 100, and 1000 µM. Worth noting, the final concentration of DMSO in the culture medium didn't exceed 0.2% (v/v). Treated and non-treated cells were allowed to grow for 48 h. 10 μl of MTT (5 mg/ml in PBS w/o Ca, Mg, Lonza Verviers SPRL Belgium, cat#17-516F) was added in each well four hours before completion of incubation. After the incubation with MTT, color was developed by adding 100 μl of DMSO to each well and measured at 490 nm using Bio-Tek microplate reader. The experiment was conducted six times. Data were calculated as percent of cell viability by the following formula: % cell viability= (Mean absorbance in test wells / Mean absorbance in control wells) ×100, then IC50 was calculated using the Origin software.

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Design and Synthesis of Novel 5-(4-chlorophenyl)furan Derivatives with Inhibitory Activity on Tubulin Polymerization

Abstract: Compounds 7c and 11a may be considered as promising CBSI based on their excellent activity and favorable drug likeness profile.

Cited by 3 publications

References 24 publications

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study

Cytotoxicity, in silico predictions and molecular studies for androstane heterocycle compounds revealed potential antitumor agent against lung cancer cells

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