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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 …