title: Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles.
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 IC50values 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.
authors.affiliation: Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
authors.forename: Pinki
authors.initials: P
authors.lastname: Yadav
authors.affiliation: Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India. Electronic address: klal_iitd@yahoo.com.
authors.forename: Kashmiri
authors.initials: K
authors.lastname: Lal
authors.affiliation: Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
authors.forename: Ashwani
authors.initials: A
authors.lastname: Kumar
authors.affiliation: Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
authors.forename: Santosh Kumar
authors.initials: SK
authors.lastname: Guru
authors.affiliation: Microbiology Lab., QC, QA & CMC Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
authors.forename: Sundeep
authors.initials: S
authors.lastname: Jaglan
authors.affiliation: 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.
authors.forename: Shashi
authors.initials: S
authors.lastname: Bhushan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D055772:Green Chemistry Technology; D006801:Humans; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D014867:Water; D002599:Chalcone
keywords: 1,2,3-triazole; Anticancer activity; Apoptosis; Chalcone; Molecular hybridization