Article
Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription.
Journal of medicinal chemistry - 12 Oct 2017
Liu Gang, Huang Wenjing, Wang Juan, Liu Xiaohua, Yang Jun, Zhang Yu, Geng Yong, Tan Wenfu, Zhang Ao
Abstract excerpt
A systemic medicinal chemistry campaign was conducted based on a literature hit compound 5 bearing the 4,5-dihydro-2H-benzo[b][1,5]oxazocin-6(3H)-one core through cyclization of two side substituents of the bicyclic skeleton combined with N-atom walking or ring walking and the central ring expansion or extraction approaches, leading to several series of structurally unique tricyclic compounds. Among these,...
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