Evaluation of Synthetic 2,4-Disubstituted-benzo[<i>g</i>]quinoxaline Derivatives as Potential Anticancer Agents
A new series of 2,4-disubstituted benzo[<i>g</i>]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 micro...
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| Main Authors: | , , , , , |
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| Format: | Book |
| Published: |
MDPI AG,
2021-08-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | A new series of 2,4-disubstituted benzo[<i>g</i>]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[<i>g</i>]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 <b>3</b>. The results of topoisomerase IIβ inhibition assay revealed that compound <b>3</b> exhibits potent inhibitory activity in submicromolar concentration. Additionally, compound <b>3</b> 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 <b>3</b> induces apoptosis via Bax activation and downregulation of Bcl2, as revealed by ELISA assay. |
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| Item Description: | 10.3390/ph14090853 1424-8247 |