Design and application of a rigid quinazolone scaffold based on two-face Bim α-helix mimicking

…, X Liang, X Li, T Song, Q Chen, H Sheng

Index: Zhang, Zhichao; Liang, Xiaomeng; Li, Xiangqian; Song, Ting; Chen, Qingbin; Sheng, Hongkun European Journal of Medicinal Chemistry, 2013 , vol. 69, p. 711 - 718

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Citation Number: 7

Abstract

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 ...