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

被引:165
作者
Yadav, Pinki [1 ]
Lal, Kashmiri [1 ]
Kumar, Ashwani [2 ]
Guru, Santosh Kumar [3 ]
Jaglan, Sundeep [4 ]
Bhushan, Shashi [3 ,5 ]
机构
[1] Guru Jambheshwar Univ Sci Technol, Dept Chem, Hisar 125001, Haryana, India
[2] Guru Jambheshwar Univ Sci Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India
[3] Indian Inst Integrat Med, Canc Pharmacol Div, Jammu 180001, India
[4] Indian Inst Integrat Med, QC QA & CMC Div, Microbiol Lab, Jammu 180001, India
[5] Indian Pharmacopoeia Commiss, MH&FW, Div Phytopharmaceuticals, Ghaziabad, Uttar Pradesh, India
关键词
Chalcone; 1,2,3-triazole; Molecular hybridization; Anticancer activity; Apoptosis; LINKED 1,4-DISUBSTITUTED 1,2,3-BISTRIAZOLES; ONE-POT SYNTHESIS; CLICK CHEMISTRY; ANTIMALARIAL EVALUATION; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; COPPER NANOPARTICLES; CYTOTOXIC EVALUATION; AGENTS; DERIVATIVES;
D O I
10.1016/j.ejmech.2016.11.030
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 (MTF) 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 mu M 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. (C) 2016 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:944 / 953
页数:10
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