Synthesis of New Quinoxaline Pharmacophores as Antitumor Agents on MCF-7 breast cancer cells | ||||
| Alfarama Journal of Basic & Applied Sciences | ||||
| Volume 5, Issue 3, July 2024, Page 364-380 PDF (1.29 MB) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajbas.2024.256230.1205 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
El-Sherbiny Hamdi El-Sayed1; Ahmed Saad Saad2; Sara Adel Hegazy  3
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| 1Department of Chemistry, Faculty of Science, Port Said University, Port Said, Egypt | ||||
| 2Pharmacology and Toxicology department, Faculty of Pharmacy, Port Said University, Port Said, Egypt | ||||
| 3Chemistry department, Faculty of science, portsaid university | ||||
| Abstract | ||||
| A new first series from 2-substituted quinoxalines (3-6) were synthesized using o-phenylenediamine with aryl bromomethyl ketones as a key starting material. Moreover, a new second series from 2-oxo-1,2,3,4-tetrahydro-benzo [g] quinoxaline (8-10) were obtained from the reaction of naphthalene-2,3-diamine with ethyl chloroacetate. The structures of the two compound types were confirmed by spectral data studies along with elemental microanalysis. The cytotoxic effects of the synthesized compounds were tested using a MTT colorimetric assay in MCF-7 cells. Four of the compounds, given numbers 4, 5, 9 and 10, were found to induce significant levels of cytotoxicity. Compounds number 5 and 9 showed promising assay results and were tested in the non-cancerous cell line MCF-10A and neither of them showed cellular deterioration. Furthermore, compound 9 was reported to suppress tubulin polymerization. These findings were confirmed by the docking study results demonstrating a remarkable binding affinity of compound 9 to tubulin active site. These findings suggestes that compound 9 has a pharmacological potential as an antineoplastic drug in MCF-7 cells. | ||||
| Keywords | ||||
| Microtubules; Quinoxaline; Breast Cancer; Tubulin | ||||
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