Evaluation of Synthetic 2,4-Disubstituted-benzo[g]quinoxaline Derivatives as Potential Anticancer Agents.
Islam ZakiSara A Abu El-AtaEman FayadOla A Abu AliAli Hussein Abu AlmaatyAhmed S SaadPublished in: Pharmaceuticals (Basel, Switzerland) (2021)
A new series of 2,4-disubstituted benzo[g]quinoxaline molecules have been synthesized, using naphthalene-2,3-diamine and 1,4-dibromonaphthalene-2,3-diamine as the key starting materials. The structures of the new compounds were confirmed by spectral data along with elemental microanalyses. The cytotoxic activity of all synthesized benzo[g]quinoxaline derivatives was assessed in vitro against the breast MCF-7 cancer cell line. The tested molecules revealed good cytotoxicity toward the breast MCF-7 cancer cell line, especially compound 3. The results of topoisomerase IIβ inhibition assay revealed that compound 3 exhibits potent inhibitory activity in submicromolar concentration. Additionally, compound 3 was found to cause pre-G1 apoptosis, and slightly increase the cell population at G1 and S phases of the cell cycle profile in MCF-7 cells. Finally, compound 3 induces apoptosis via Bax activation and downregulation of Bcl2, as revealed by ELISA assay.
Keyphrases
- cell cycle
- breast cancer cells
- papillary thyroid
- single cell
- induced apoptosis
- cell cycle arrest
- cell proliferation
- endoplasmic reticulum stress
- squamous cell
- high throughput
- cell death
- lymph node metastasis
- squamous cell carcinoma
- cell therapy
- optical coherence tomography
- high resolution
- magnetic resonance imaging
- computed tomography
- machine learning
- bone marrow
- mesenchymal stem cells
- deep learning
- human health
- oxide nanoparticles