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

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

  • Eur J Med Chem. 2017 Jan 27:126:944-953. doi: 10.1016/j.ejmech.2016.11.030.
Pinki Yadav 1,  Kashmiri Lal 2,  Ashwani Kumar 3,  Santosh Kumar Guru 4,  Sundeep Jaglan 5,  Shashi Bhushan 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
  • 2 Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India. Electronic address: klal_iitd@yahoo.com.
  • 3 Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
  • 4 Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
  • 5 Microbiology Lab., QC, QA & CMC Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
  • 6 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: sbhusan@iiim.ac.in.
PMID: 28011424 DOI: 10.1016/j.ejmech.2016.11.030
Abstract

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.

Keywords

1,2,3-triazole; Anticancer activity; Apoptosis; Chalcone; Molecular hybridization.

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