Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6

Quinoxaline, its derivatives and applications: A State of the Art review

“…4-Alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines were also synthesized and anti-inflammatory activity was tested as inhibitors of the pro-inflammatory cytokines TNF-a and IL-6 [53]. Results revealed efficiency in both cytokines was demonstrated.…”

Present status of quinoxaline motifs: Excellent pathfinders in therapeutic medicine

“…The Schiff bases of quinoxaline bearing 2-furyl 131 and 4-chlorophenyl side chain 132 have shown significant protection against the edema formation at 65.9% inhibition [39]. Guirado and coworkers assayed a series of triazolo [4,3-a]quinoxalines to test their inhibitory efficiency on the pro-inflammatory cytokines TNF-α and IL-6 [133] and they came up with the findings that 133 (IC 50 = 9.1 µM) was the best inhibitor against TNF-α while 134 [IC 50 = 10.0 µM] emerged as the best inhibitor of IL-6 [133]. Anti-inflammatory activities of sulfonamido-quinoxaline 135 [134], alkylated derivative 136 [135] and hydrazone 137 [136] have also been reported to be highly promising for further investigations.…”

Synthesis and Evaluation of New Quinoxaline Derivatives of Dehydroabietic Acid as Potential Antitumor Agents

“…The presence of lone-electron pairs on heteroatoms benefits the formation of hydrogen bonding with water, which increases the solubility, and likely improves the binding of the molecule to its potential targets [ 18 ]. Quinoxalines have shown a variety of biological activities, including antibacterial, antiviral, herbicidal, anti-inflammatory and antitumor activities [ 19 , 20 , 21 , 22 , 23 ], which indicates that they are an important class of N -containing heterocycles in organic synthesis and drug discovery [ 24 ]. Some drug candidates bearing quinoxaline core structures are currently under clinical trials for anticancer therapeutic purposes [ 25 ].…”