Abstract Based on our previous discovery of an anthraquinone scaffold mimicking two faces of Bim α-helix, we derived a quinazolone scaffold through structure simplification and optimization. It was inferred that a rigid bicyclic ring was necessary and efficient to maintain the two-faced binding mode. A novel dual inhibitor 6c [6, 7, 8-trihydroxy-3-(2-hydroxy-5- methylbenzyl)-2-phenylquinazolin-4 (3H)-one] was obtained based on this scaffold. 6c ...