Pegylated triarylmethanes: Synthesis, antimicrobial activity, anti-proliferative behavior and in silico studies

Colorectal anticancer activity of a novel class of triazolic triarylmethane derivatives

“…First, the commercially available bisacodyl 1 was deacetylated via a saponification reaction in aqueous KOH solution (10% EtOH) at room temperature affording the 4,4′-(dihydroxy-diphenyl)-(2-pyridyl) methane 2 in 97% yield without any further purification. 6 Compound 2 was doubly alkylated using an excess of propargyl bromide in the presence of K 2 CO 3 in DMF at 50 °C, 18 leading to the desired compound 3 in 79% yield. In this step, the yield was optimized to up to 99% by replacing DMF with acetone which is less toxic and easier to handle (Scheme 1).…”

“…Due to their particular structures and properties, 1 they have been used as dyes, pH indicators and fluorescent probes and in photodynamic therapy as photosensitisers. 2 TAM are considered privileged structures in medicinal chemistry considering their association with several biological properties such as anticancer, 3,4 antiinflammatory, 5 antibacterial and antifungal, [6][7][8] or even enhancement of oestrogen metabolism. 9 Some TAM are used in therapy, such as the laxative drug bisacodyl (Fig.…”

“…TAM are considered privileged structures in medicinal chemistry considering their association with several biological properties such as anticancer, 3,4 anti-inflammatory, 5 antibacterial and antifungal, 6–8 or even enhancement of oestrogen metabolism. 9 Some TAM are used in therapy, such as the laxative drug bisacodyl (Fig.…”

Discovery of 2-aryl and 2-pyridinylbenzothiazoles endowed with antimicrobial and aryl hydrocarbon receptor agonistic activities

“…Biofilm formation in S. aureus and P. aeruginosa was determined spectrophotometrically by using the crystal violet test in 96-well plates as previously described (Ricco et al, 2020). The tested compounds (1-16) were assayed at their MIC against S. aureus and P. aeruginosa, respectively, to determine the biofilm anti-adhesion activity.…”