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

• DOI: 10.1016/j.ejmech.2016.11.030
• Publication Date: 2016-11-14T19:04:37Z
• Authors: Pinki Yadav; Kashmiri Lal; Ashwani Kumar; Santosh Kumar Guru; Sundeep Jaglan; Shashi Bhushan
• Keywords: Membrane Potential, Mitochondrial; Dose-Response Relationship, Drug; Water; Antineoplastic Agents; Apoptosis; Green Chemistry Technology; Chemistry Techniques, Synthetic; Triazoles; 01 natural sciences; 0104 chemical sciences; 3. Good health; G2 Phase Cell Cycle Checkpoints; Structure-Activity Relationship; Chalcone; Cell Line, Tumor; Drug Design; Humans; M Phase Cell Cycle Checkpoints; Drug Screening Assays, Antitumor; Cell Proliferation

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 IC50 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.