Citation: . Study of the synthesis, antiviral bioactivity and interaction mechanisms of novel chalcone derivatives that contain the 1, 1-dichloropropene moiety[J]. Chinese Chemical Letters, ;2017, 28(7): 1566-1570. doi: 10.1016/j.cclet.2017.03.013
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A series of novel chalcone derivatives that contain the 1, 1-dichloropropene moiety was designed and synthesized. Bioactivity assays showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus (TMV) at 500 μg/mL. Among the target compounds, compound 7h showed the highest in vivo inactivation activity against TMV with the EC50 and EC90 value of 45.6 and 327.5 μg/mL, respectively, which was similar to that of Ningnanmycin (46.9 and 329.4 μg/mL) and superior to that of Ribavirin (145.1 and 793.1 μg/mL). Meanwhile, the microscale thermophoresis and fluorescence spectroscopy experiments showed that the compound 7h had a strong interaction with the tobacco mosaic virus coat protein.
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