European Journal of Medicinal Chemistry p. 338 - 352 (2016)
Update date:2022-07-30
Topics:
Kim, Jina
Chin, Jungwook
Im, Chun Young
Yoo, Eun Kyung
Woo, Seoyeon
Hwang, Hee Jong
Cho, Joong-Heui
Seo, Kyung-Ah
Song, Jaeyoung
Hwang, Hayoung
Kim, Kyung-Hee
Kim, Nam Doo
Yoon, Suk Kyoon
Jeon, Jae-Han
Yoon, Seung-Yun
Jeon, Yong Hyun
Choi, Hueng-Sik
Lee, In-Kyu
Kim, Seong Heon
Cho, Sung Jin
Estrogen-related receptor gamma (ERRγ) has recently been recognized as an attractive target for treating inflammation, cancer, and metabolic disorders. Herein, we discovered and demonstrated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chemical entities that could act as highly selective inverse agonists for ERRγ. The results were comparable to those for GSK5182 (4), a leading ERRγ inverse agonist ligand. Briefly, the half-maximal inhibitory concentration (IC50) range of the synthesized compounds for ERRγ was 0.1-10 μM. Impressively, compound 24e exhibited potency comparable to 4 but was more selective for ERRγ over three other subtypes: ERRα, ERRβ, and estrogen receptor α. Furthermore, compound 24e exhibited a superior in vitro ADMET profile compared to the other compounds. Thus, the newly synthesized class of ERRγ inverse agonists could be lead candidates for developing clinical therapies for ERRγ-related disorders.
View MoreShanghai Demand Chemical Co., ltd,China
Contact:86-021-55237578/55239122
Address:Room 3H, No.578, Yingkou Road, Yangpu District, Shanghai, China
Tianjin Jingye Fine Chemicals Co., Ltd.
Contact:+86-15722078107; +86-22-26911407
Address:Bohua Fine Chemicals Base of Petrochemical Industry Park, Nanhuan Road, Dagang District, Tianjin, 300271, P. R. China
Contact:0086-573-82201031
Address:Jiaxing Industrial Park, Daqiao Town, Jiaxing
Shanghai doly chemical Co.,Ltd
Contact:+86-21-34716221
Address:No.328,WuHe Roard,MinHang,ShangHai China
Yangzhou Siyu Chemical Co.,Ltd.
Contact:+86-514-87325867 13358126196
Address:Room 620 Exposition Pavilion,No. 98 Huaihai Road,Guangling District,Yangzhou City, Jiangsu Province
Doi:10.1021/jo00350a038
(1985)Doi:10.1055/s-1984-31073
(1984)Doi:10.1021/jo00219a022
(1985)Doi:10.1021/ja003608g
(2001)Doi:10.1021/jm301782e
(2013)Doi:10.1016/j.tetlet.2013.09.131
(2013)