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 MoreSinoway International (Jiangsu) Co., Ltd.
Contact:+86-25-86630167
Address:17 Beijing Road (West), Nanjing, China
Goldwills Pharmaceuticals Co., Ltd.
Contact:0916-2237889 13991621155
Address:North Suburb of Hanzhong city, Shaanxi Province
Shenzhen ZheYi Chemicals Co.,LTD(Shanghai Branch)
Contact:+86-21-54159691
Address:Room1002,Building No.2, Lane 98 Bixiu Road,Minhang District, Shanghai,China 201100
Xiamen Hisunny Chemical Co.,Ltd
website:http://www.hisunnychem.com
Contact:+86-592-3327115
Address:Unit 603,No.879,Xiahe Road,Meixin Building,Xiamen,China
Contact:+86-710-3516804
Address:Number 83,Panggong road,Xiangcheng District,Xiangyang ,Hubei
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)