Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFV600E inhibition

A series of novel BRAFV600E inhibitory agents (Compound 1-16) have been designed and synthesized. Compound 12 indicated fine BRAFV600E inhibitory effect with no obvious activity for BRAFWT. Docking simulation inferred the differences in binding patterns of BRAFV600E and BRAFWT, indicating the future orientations for selectivity.277