Bioorganic and Medicinal Chemistry Letters p. 3527 - 3530 (2003)
Update date:2022-08-05
Topics: Synthesis Evaluation Isatins Cruzain Falcipain-2 Rhodesain
Chiyanzu, Idan
Hansell, Elizabeth
Gut, Jiri
Rosenthal, Philip J.
McKerrow, James H.
Chibale, Kelly
While commercial isatins were practically inactive against the target proteases, thiosemicarbazone derivatives were found to be active. The most active compound from the series displayed an inhibitory IC50 value of 1 μM against rhodesain. One thiosemicarbazone was found to be active against all three proteases with inhibitory IC50 values of 10 μM or less. A combination of N-benzylation and appropriate substitution on the aromatic portion of the isatin scaffold was generally found to be beneficial especially against cruzain for ketone inhibitors.
View MoreWeifang Jahwa Chemical Co.,Ltd
Contact:0086-536-8897731,8897730
Address:No.5166 East Dongfeng Street,Weifang,Shandong,China
Taizhou Sunny Chemical Co.,Ltd
Contact:+86-523-86920899 +86-13951172783
Address:No.11 Xingyuang road, Gaoyong Chemical Industry Park, Gaogang Jiangsu China
Henan zhongda Biological Engineering Co., Ltd
Contact:86-28-18109029985
Address:shenzhou road,xuedian industrial estate,zhengzhou city,henan province CHN
ZHEJIANG CHEMICAL INDUSTRY INSTITUTE TECHNOLOGY CO.,LTD(expird)
Contact:86-575-82730298
Address:shangyu
Hangzhou Dingyan Chem Co., Ltd
website:http://www.dingyanchem.com
Contact:86-571-87157530-8008
Address:RM.1118,NO.1 Building, Baiyun Tower,Jianggan Area, Hangzhou city, China,310004
Doi:10.1016/j.bmcl.2011.06.041
(2011)Doi:10.1080/15257779908041581
(1999)Doi:10.1007/BF00553887
(1980)Doi:10.1055/s-2004-822401
(2004)Doi:10.1021/jm00183a018
(1980)Doi:10.1016/S0031-9422(00)83732-2
(1986)