Ontology highlight
ABSTRACT:
SUBMITTER: Farooqi AS
PROVIDER: S-EPMC6901289 | biostudies-literature | 2019 Apr
REPOSITORIES: biostudies-literature
Farooqi Ali Sohail AS Hong Jun Young JY Cao Ji J Lu Xuan X Price Ian Robert IR Zhao Qingjie Q Kosciuk Tatsiana T Yang Min M Bai Jessica Jingyi JJ Lin Hening H
Journal of medicinal chemistry 20190415 8
Sirtuin 2 (SIRT2) is a protein lysine deacylase that has been indicated as a therapeutic target for cancer. To further establish the role of SIRT2 in cancers, it is necessary to develop selective and potent inhibitors. Here, we report the facile synthesis of novel lysine-derived thioureas as mechanism-based SIRT2 inhibitors with anticancer activity. Compounds AF8, AF10, and AF12 selectively inhibited SIRT2 with IC<sub>50</sub> values of 0.06, 0.15, and 0.08 μM, respectively. Compounds AF8 and AF ...[more]