Synthesis and Evaluation of Aryloxy-Acetamide Derivatives as CBX2 Inhibitors.

Authors

Yuichiro Kawamoto, Shohei Takase, Ashutosh Kumar, Yuki Maemoto, Kam Y J Zhang, Hisanaka Ito, Akihiro Ito

Published in

Chemical & pharmaceutical bulletin. Volume 74. Issue 10. Pages 779-784.

Abstract

The CBX2 protein plays a key role in the methylation of histone lysine residues related to epigenetic silencing. In contrast to other polycomb paralogs, there are few examples of CBX2 modulators, which prompted us to develop small-molecule CBX2 inhibitors by synthetic evolution based on virtual screening hit scaffolds previously reported by our group. We synthesized a series of aryloxy-acetamide derivatives and evaluated their CBX2 inhibitory activities using the NanoBRET assay and the subsequent NanoBiT assay. Through structural modifications, compound 16 was identified as the best CBX2 inhibitor in this series.

PMID:
42893867
Bibliographic data and abstract were imported from PubMed on 19 Oct 2026.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.