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

Amol S. Nipate, Chetan K. Jadhav, Asha V. Chate, Tejshri R. Deshmukh, Aniket P. Sarkate, Charansingh H. Gill

2021ChemistrySelect29 citationsDOI

Abstract

Abstract 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 IC 50 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

Topics & Concepts

Click chemistryChemistryCycloadditionIn vitroCombinatorial chemistryCytotoxicityBromideTriazoleStereochemistryMTT assayProton NMR1,2,3-TriazoleAzideOrganic chemistryBiochemistryCatalysisClick Chemistry and ApplicationsSynthesis and Characterization of Heterocyclic CompoundsSynthesis and biological activity