25284-11-1Relevant articles and documents
Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition
Yeon Kim, Bo,Hee Yoon, Ji,Kim, Myeongbin,Nyoung Kim, Jae,Park, Hwangseo,Eon Ryu, Seong,Lee, Sangku
supporting information, p. 1746 - 1748 (2019/05/21)
Structure based virtual screening attempts to discover DUSP1 inhibitors have yielded a scaffold featuring benzoxazole and acylthiourea pharmacophore. A series of its analogues were synthesized to explore structure activity relationship (SAR) of DUSP1 inhi
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: A novel class of small molecule heparanase inhibitors
Courtney, Stephen M.,Hay, Philip A.,Buck, Richard T.,Colville, Claire S.,Porter, David W.,Scopes, David I. C.,Pollard, Faye C.,Page, Martin J.,Bennett, James M.,Hircock, Margaret L.,McKenzie, Edward A.,Stubberfield, Colin R.,Turner, Paul R.
, p. 3269 - 3273 (2007/10/03)
A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids are described as inhibitors of the endo-β-glucuronidase heparanase. Several of the compounds, for example, 2-[4-propylamino-5-[5-(4-chloro)phenyl-benzoxazol-2- yl]phenyl]-2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid (9c), display potent heparanase inhibitory activity (IC50 200-500nM) and have high selectivity (>100-fold) over human β-glucuronidase. They also show anti-angiogenic effects. Such compounds should serve as useful biological tools and may provide a basis for the design of novel therapeutic agents.
