Evaluation of Synthetic 2,4-Disubstituted-benzo[g]quinoxaline Derivatives as Potential Anticancer Agents

Abstract

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.

Design, Synthesis and Cytotoxic Activity Evaluation of Newly Synthesized Amides-Based TMP Moiety as Potential Anticancer Agents over HepG2 Cells

“…Inspired by the above mentioned aspects and in continue efforts to discover new anticancer agents with better apoptotic properties [28,29], the present study concerned with the design and synthesis of novel series of amide-based compounds in the hopes of obtaining novel dual HDAC and tubulin inhibitors with promising anticancer potency. All the prepared amide compounds were screened for cytotoxicity against hepatocellular carcinoma HepG2 and normal liver cell line HL-7702 cell lines utilizing MTT antiproliferative assay.…”

Design, Synthesis, In Vitro Biological Activity Evaluation and Stabilized Nanostructured Lipid Carrier Formulation of Newly Synthesized Schiff Bases-Based TMP Moieties

“…On the basis of the aforementioned structural analysis, as well as in keeping with our general enthusiasm for the design and development of novel anticancer agents, [29][30][31][32], as potential anticancer medicines, the current work focused on the design and synthesis of novel Schiff bases-based TMP moieties. The basic structural skeleton of the lead compound is formed from two TMP rings connected through amideacrylic acid hydrazide groups.…”

Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity

“…Prompted by the above-mentioned studies and in our continuous program in the search for new candidates with anticancer agents [29][30][31][32], in this study, we describe the synthesis and biological assessment of a novel class of furan-based derivatives that may have enhanced anticancer activity (Figure 2). The newly synthesized compounds were tested against MCF-7 breast cancer and MCF-10A normal breast cell lines for their antiproliferative properties.…”