European Journal of Medicinal Chemistry p. 289 - 296 (2014)
Update date:2022-08-03
Topics:
Shi, Da-Hua
Huang, Wei
Li, Chao
Liu, Yu-Wei
Wang, Shi-Fan
A series of aloe-emodin derivatives were synthesized and evaluated as xanthine oxidase inhibitors. Among them, four aloe-emodin derivatives showed significant inhibitory activities against xanthine oxidase. The compound 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carbaldehyde (A1) possessed the best xanthine oxidase inhibitory activity with IC50 of 2.79 μM. Lineweaver-Burk plot analysis revealed that A1 acted as a mixed-type inhibitor for xanthine oxidase. The docking study revealed that the molecule A1 had strong interactions with the active site of xanthine oxidase and this result was in agreement with kinetic study. Consequently, compound A1 is a new-type candidate for further development for the treatment of gout.
View MoreTianjin Te-An Chemtech Co., Ltd.(expird)
Contact:+86-22-65378638
Address:A5-8, No.80 Haiyun Street, TEDA
Shanghai Potomer International Trade CO., LTD
Contact:+86-21-61397128
Address:Room 304,No.505 ,Caoyang Road.Shanghai,China
Hangzhou Share Chemical Co., Ltd(expird)
Contact:+86-57187093700
Address:Hang Xing Road
website:http://www.orchid-chem.com
Contact:+86-571-85395792
Address:607, North Zhongshan Road, Hangzhou 310000 China
website:http://www.np-chem.com
Contact:0086-25-52346877
Address:199, Jian Ye Road, Nanjing, China
Doi:10.1021/ja312346s
(2013)Doi:10.1016/j.tetlet.2013.01.108
(2013)Doi:10.1021/acs.joc.5b00706
(2015)Doi:10.1021/ol400252p
(2013)Doi:10.3987/COM-12-12592
(2013)Doi:10.1016/j.tetlet.2011.04.014
(2011)