Synthesis of novel 1,2,3-triazole substituted-N-alkyl/aryl nitrone derivatives, their anti-inflammatory and anticancer activity

On the vasoprotective mechanisms underlying novel β-phosphorylated nitrones: Focus on free radical characterization, scavenging and NO-donation in a biological model of oxidative stress

“…Indeed, this chemical property of PBN is increasingly invoked to explain some of its pharmacological actions [16,18]. Among the increasing number of available PBNs designed for a therapeutic purpose, most were elaborated on the basis of cell targeting, bioavailability or increased membrane crossing [13,19,20], and if a few were built around a phenolic-based antioxidant scaffold [21][22][23][24] (Figure 1A), no further structural modification of the non aromatic side of the nitrone function was done to improve the EPR detection of spin adducts. 9 significantly decreased with increasing steric bulk of the substituent.…”

Tandem synthesis of 1-formyl-1,2,3-triazoles

“…Analogs of the 4-formyl-1,2,3-triazole motif have recently been reported to display enzyme inhibitory, 22 anti-cancer 23,24 antileishmanial 25 and anti-tuberculosis activity. 26,27 With the aldehyde group an attractive handle for synthetic diversification, such compounds have also served as synthons for preparing bioimaging, 28 anti-cancer, 23,24 and antituberculosis 26,27 agents.…”

“…26,27 With the aldehyde group an attractive handle for synthetic diversification, such compounds have also served as synthons for preparing bioimaging, 28 anti-cancer, 23,24 and antituberculosis 26,27 agents. Likewise, 4-imino-1,2,3-triazoles formed from amine condensation reactions have been shown to be useful for constructing novel coordination compounds.…”

“…The direct synthesis from propynal has been reported, 32 but is impractical due to this reagent’s low boiling point and lack of commercial availability. A two-step method of CuAAC reaction with propargyl alcohol followed by oxidation of the hydroxymethylated triazole intermediate with reagents such as CrO 3 24 or MnO 2 30 is effective but limited to substituents that can withstand such oxidants, and is environmentally unfriendly. Advances in this approach using organic oxidants 23,33 and polymer-immobilized two-component catalysis 34 methods have recently been reported.…”

Triazole analog 1-(1-benzyl-5-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)-2-(4-bromophenylamino)-1-(4-chlorophenyl)ethanol induces reactive oxygen species and autophagy-dependent apoptosis in both in vitro and in vivo breast cancer models

“…1,2,3-triazole is a well-known pharmacophore with antifungal, anti-viral, anti-inflammatory and anticancer activities (He et al, 2014;Sambasiva Rao et al, 2014;Yu et al, 2014). Previously, we have reported a series of 1,4,5-trisubstituted 1,2,3-triazoles having anti-breast cancer activity (Ajay et al, 2012).…”