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Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles.
Yadav, Pinki; Lal, Kashmiri; Kumar, Ashwani; Guru, Santosh Kumar; Jaglan, Sundeep; Bhushan, Shashi.
Afiliación
  • Yadav P; Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
  • Lal K; Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India. Electronic address: klal_iitd@yahoo.com.
  • Kumar A; Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
  • Guru SK; Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
  • Jaglan S; Microbiology Lab., QC, QA & CMC Division, Indian Institute of Integrative Medicine, Jammu, 180001, India.
  • Bhushan S; 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.
Eur J Med Chem ; 126: 944-953, 2017 Jan 27.
Article en En | MEDLINE | ID: mdl-28011424
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Triazoles / Diseño de Fármacos / Chalcona / Antineoplásicos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2017 Tipo del documento: Article País de afiliación: India

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Triazoles / Diseño de Fármacos / Chalcona / Antineoplásicos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2017 Tipo del documento: Article País de afiliación: India
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