Synthesis and In Vitro Anticancer Activities of New 1,4‐Disubstituted‐1,2,3‐triazoles Derivatives through Click Approach

• Published in: ChemistrySelect (Weinheim) 2021-06, Vol.6 (21), p.5173-5179
• Main Authors: Nipate, Amol S., Jadhav, Chetan K., Chate, Asha V., Deshmukh, Tejshri R., Sarkate, Aniket P., Gill, Charansingh. H.
• Format: Article
• Language: English
• Subjects: 1,2,3-Triazole; Acetovanillone; Anticancer Activity; Click Chemistry; Phenyl azide
• ISSN: 2365-6549; 2365-6549
• DOI: 10.1002/slct.202101035

The synthesis of a new series 1‐(3‐methoxy‐4‐((1‐phenyl‐1H‐1,2,3‐triazole‐4‐yl)methoxy) phenyl)ethanone via click chemistry approach utilizing azide‐alkyne cycloaddition reactions is reported in this study. The structures of all newly synthesized compounds were analyzed by IR, NMR, and Mass spectral techniques. All the newly synthesized compounds were subjected to cytotoxicity assay against a panel of three human cancer cell lines (HepG2, A549, and MCF‐7) using 3‐(4,5‐dimethylthiazole‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT), to check in vitro anticancer activity. Compound 5 b was found to be the most potent anticancer agents with IC50 value 3.42 μM, 1.26 μM, and 5.96 μM against HepG2, A549, and MCF‐7 respectively. Among the tested compounds, 5 a and 5 q have shown notable anticancer activity as compared to the reference drug, Adriamycin The synthesis of a new series 1‐(3‐methoxy‐4‐((1‐phenyl‐1H‐1,2,3‐triazole‐4‐yl)methoxy) phenyl)ethanone via click chemistry approach utilizing azide‐alkyne cycloaddition reactions is reported in this study.