Bcl-2/MDM2 dual inhibitors based on universal pyramid-like α-helical mimetics
Z Wang, T Song, Y Feng, Z Guo, Y Fan…
Index: Zhang, Zhichao; Li, Xiangqian; Song, Ting; Zhao, Yan; Feng, Yingang Journal of Medicinal Chemistry, 2012 , vol. 55, # 23 p. 10735 - 10741
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Abstract
No α-helical mimetic that exhibits Bcl-2/MDM2 dual inhibition has been rationally designed due to the different helicities of the α-helixes at their binding interfaces. Herein, we extracted a one-turn α-helix-mimicking ortho-triarene unit from o-phenylene foldamers. Linking benzamide substrates with a rotatable C–N bond, we constructed a novel semirigid pyramid- like scaffold that could support its two-turn α-helix mimicry without aromatic stacking ...
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