Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 52287-51-1, is researched, SMILESS is BrC1=CC=C2OCCOC2=C1, Molecular C8H7BrO2Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach, Author is Xu, Mengyang; Zhao, Chao; Zhu, Biying; Wang, Liangyue; Zhou, Huihao; Yan, Daoguang; Gu, Qiong; Xu, Jun, the main research direction is nasopharyngeal carcinoma Hsp90 inhibitor fragments chemotypes click chem.Quality Control of 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine.
Hsp90 is a new promising target for cancer treatment. Many inhibitors have been discovered as therapeutic agents, and some have passed Phase I and II. However, no one is approved by FDA yet. Novel and druggable Hsp90 inhibitors are still demanding. Here, we report a new way to discover high potent Hsp90 inhibitors as antinasopharyngeal carcinoma agents through assembling fragments. With chemotyping anal., we extract seven chemotypes from 3482 known Hsp90 inhibitors, screen 500 fragments that are compatible with the chemotypes, and confirm 15 anti-Hsp90 fragments. Click chem. is employed to construct 172 mols. and synthesize 21 compounds among them. The best inhibitor 3d was further optimized and resulted in more potent 4f(I) (IC50 = 0.16μM). In vitro and in vivo experiments confirmed that 4f is a promising agent against nasopharyngeal carcinoma. This study may provide a strategy in discovering new ligands against targets without well-understood structures.
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Reference:
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