Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists

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Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists

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作者：Jina Kim^a ; ¹ ; Jungwook Chin^a ; ¹ ; Chun Young Im^a ; Eun Kyung Yoo^b ; Seoyeon Woo^a ; Hee Jong Hwang^a ; Joong-heui Cho^a ; Kyung-ah Seo^a ; Jaeyoung Song^a ; Hayoung Hwang^a ; Kyung-Hee Kim^a ; Nam Doo Kim^a ; Suk Kyoon Yoon^a ; Jae-Han Jeon^b ; ^c ; Seung-Yun Yoon^d ; Yong Hyun Jeon^d ; Hueng-Sik Choi^e ; In-Kyu Lee^b ; ^c ; Seong Heon Kim^a ; ^{rose1998@boryung.co.kr" class="auth_mail" title="E-mail the corresponding author} ; Sung Jin Cho^a ; ^b ; ^{sjcho@dgmif.re.kr" class="auth_mail" title="E-mail the corresponding author}
关键词：ERRγ inverse agonist ; Nuclear receptor ; ADMET ; GSK5182
刊名：European Journal of Medicinal Chemistry
出版年：2016
出版时间：14 September 2016
年：2016
卷：120
期：Complete
页码：338-352
全文大小：1451 K

文摘

•: Compound 24e represents a new structural class of promising 4-hydroxytamoxifen analogs.
•: Our novel compound exhibited a significantly improved in vitro ADMET profile.
•: 24e is a promising enhancer for restoring NIS protein expression in ATC cells.

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