Bioorganic and Medicinal Chemistry (2019)
Update date:2022-07-31
Topics:
Jeong, Jieun
Kim, Kun-Hee
Kim, Dong-Young
Chandrasekaran, Gopalakrishnan
Kim, Minhee
Pagire, Suvarna H.
Dighe, Mahesh
Choi, Eun Young
Bak, Su-Min
Kim, Eun-Young
Shin, Myung-Geun
Choi, Seok-Yong
Ahn, Jin Hee
A new series of 1,3-diketone, heterocyclic and α,β-unsaturated derivatives were synthesized and evaluated for their AhR antagonist activity using zebrafish and mammalian cells. Compounds 1b, 2c, 3b and 5b showed significant AhR antagonist activity in a transgenic zebrafish model. Among them, compound 3b, and 5b were found to have excellent AhR antagonist activity with IC50 of 3.36 nM and 8.3 nM in a luciferase reporter gene assay. In stem cell proliferation assay, compound 5b elicited marked HSC expansion.
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