In silico studies, synthesis and anticancer activity of novel diphenyl ether-based pyridine derivatives

Verma, Ruchi and Bairy, Indira and Tiwari, Mradul and Bhat, Varadaraj G and Shenoy, Gautham G (2019) In silico studies, synthesis and anticancer activity of novel diphenyl ether-based pyridine derivatives. Molecular Diversity, 23. pp. 541-554. ISSN 1381-1991

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Abstract

A series of novel 2-amino-4-(3-hydroxy-4-phenoxyphenyl)-6-(4-substituted phenyl) nicotinonitriles were synthesized and evaluated against HepG2, A-549 and Vero cell lines. Compounds 3b (IC50 16.74±0.45 μM) and 3p (IC50 10.57±0.54 μM) were found to be the most active compounds against A-549 cell line among the evaluated compounds. Further 3b- and 3p- induced apoptosiswas characterized byAO/EB (acridine orange/ethidium bromide) nuclear staining method and also byDNA fragmentation study. A decrease in cell viability and initiation of apoptosis was clearly evident through the morphological changes in the A-549 cells treated with 3b and 3p when stained with this method. Fragmentation of DNA into nucleosomes was observed which further confirmed the cell apoptosis in cells treated with compound 3b. Flow cytometry studies confirmed the cell cycle arrest at G2/M phase in A549 cells treated with compound 3b. Further in silico studies performed supported the in vitro anticancer activity of these compounds as depicted by dock score and binding energy values

Item Type: Article
Uncontrolled Keywords: Triclosan; Diphenyl ether derivatives; Human enoyl-acyl carrier protein reductase (hER)
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Depositing User: KMC Library
Date Deposited: 17 Aug 2019 04:01
Last Modified: 17 Aug 2019 04:01
URI: http://eprints.manipal.edu/id/eprint/154396

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