| Literature DB >> 25743216 |
Yakaiah Chinthala1, Sneha Thakur1, Shalini Tirunagari1, Srinivas Chinde2, Anand Kumar Domatti3, Niranjana Kumar Arigari1, Srinivas K V N S1, Sarfaraz Alam4, Kotesh Kumar Jonnala5, Feroz Khan4, Ashok Tiwari3, Paramjit Grover2.
Abstract
A series of novel chalcone-triazole derivatives were synthesized and screened for in vitro anticancer activity on the human cancer cell lines IMR32 (neuroblastoma), HepG2 (hepatoma) and MCF-7 (breast adenocarcinoma), DU-145 (prostate carcinoma), and A549 (lung adenocarcinoma). Among the tested compounds, 4r showed the most promising anticancer activity in all the cell lines whereas, compounds 4c (IC50 65.86 μM), 4e (IC50 66.28 μM), 4o (IC50 35.81 μM), 4q (IC50 50.82 μM) and 4s (IC50 48.63 μM) showed better activity than the standard doxorubicin (IC50 69.33 μM) in A549 cell line alone. Rat intestinal α-glucosidase inhibitory activity of the synthesized derivatives showed 4m (IC50 67.77 μM), 4p (IC50 74.94 in μM) and 4s (IC50 102.10 μM) as most active compared to others. The in silico docking of synthesized derivatives 4a-4t with DNA topoisomerase IIα revealed the LibDock score in the range of 71.2623-118.29 whereas, compounds 4h, 4m, 4p and 4s with docking target α-glucosidase were in the range of 100.372-107.784.Entities:
Keywords: 1,2,3-Triazoles; Anticancer activity; Chromanochalcones; Molecular docking; α-Glucosidase inhibition
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Year: 2015 PMID： 25743216 DOI： 10.1016/j.ejmech.2015.02.027
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514