Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles.

Eur J Med Chem

Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Jammu, 180001, India; Division of Phyto-pharmaceuticals, Indian Pharmacopoeia Commission, MH&FW, Ghaziabad, UP, India. Electronic address:

Published: January 2017

A series of chalcone linked-1,2,3-triazoles was synthesized via cellulose supported copper nanoparticle catalyzed click reaction in water. The structures of all the compounds were analyzed by IR, NMR and Mass spectral techniques. All the synthesized products were subjected to 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay against a panel of four human cancer cell lines (MCF-7, MIA-Pa-Ca-2, A549, HepG2) to check their anticancer potential. Compound 6h was found to be most active against all the tested cancer cell lines with IC values in the range of 4-11 μM and showed better or comparable activity to the reference drug against all the tested cell lines. Cell cycle analysis revealed that compound 6h induces apoptosis and G2/S arrest in MIA-Pa-Ca-2 cells. Compound 6h triggers mitochondrial potential loss in pancreatic cancer MIA-Pa-Ca-2 cells. Further, Compound 6h also triggers caspase-3 and PARP-1 cleavage, which increases in dose dependent manner.

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http://dx.doi.org/10.1016/j.ejmech.2016.11.030DOI Listing

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