Bioorganic and Medicinal Chemistry p. 5029 - 5036 (2018)
Update date:2022-08-04
Topics:
Xin, Minhang
Zhang, Liandi
Tu, Chongxing
Tang, Feng
Wen, Jun
A series of novel hedgehog signaling pathway inhibitors have been designed and synthesized based on our previously reported scaffold of 4-(2-pyrimidinylamino)benzamide. The Hh signaling pathway inhibitory activities were evaluated by Gli-luciferase reporter method and most compounds showed more potent inhibitory activities than vismodegib. Three compounds were picked out to evaluated in vivo for their PK properties, and compound 23b bearing a 2-pyridyl A-ring and (morpholin-4-yl)methylene at 3-position of D-ring demonstrated satisfactory PK properties. This study suggested the 4-(2-pyrimidinylamino)benzamides were a series of potent Hh signaling pathway inhibitors, deserving to further structural optimization.
View MoreAnhui Qingyun Pharmaceutical and Chemical Co.,Ltd
Contact:+86-551-63633067
Address:Shuangfeng Road Hefei Anhui
Lonzeal Pharmaceuticals Co., Ltd.
website:http://www.lonzeal.com
Contact:+86-13381011962
Address:RM 801, Yue MOMA, No. 26 Anningzhuang Rd. Haidian District, Beijing, China
Chengdu NoVi Biotechnology Co., Ltd.(expird)
Contact:13551243286/028-81458053
Address:NO.168-1-224 JULONG ROAD WUHOU DISTRICT, CHENGDU CITY,SICHUAN PROVINCE
Shanghai Haoyuan Chemexpress Co., Ltd.
website:https://www.chemexpress.com/
Contact:86-21-58950125
Address:No.3 Building, No.1999, Zhangheng Road, ZhangjiangHighTech Park, Shanghai, P.R.China,201203
Shanghai Yuking Water Soluble Material Tech Co., Ltd
Contact:86-21-68286299
Address:4F, 13B, No. 600, South Xinyuan Road 201306, Shanghai, China
Doi:10.1021/ol900150u
(2009)Doi:10.1007/BF00956351
(1987)Doi:10.1021/es00051a018
(1994)Doi:10.1055/s-0028-1083266
(2009)Doi:10.1039/jr9610000960
(1961)Doi:10.1039/b816434g
(2009)