259101-08-1

Upstream product

• 259100-47-5 2-amino-5-(benzylsulfanyl)[1,3]thiazolo[4,5-d]pyrimidin-7-ol 
• 259103-40-7 {[4-amino-2-(benzylsulfanyl)-6-hydroxypyrimidin-5-yl]sulfanyl}formonitrile 
• 37660-23-4 4-amino-2-(benzylthio)-6-hydroxypyrimidine 
• 259103-38-3 7-chloro-5-[(phenylmethyl)thio]thiazolo[4,5-d]pyrimidin-2-amine 
• 141-43-5 ethanolamine 

Relevant academic research and scientific papers

PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells

Targeting p21-activated kinase 4 (PAK4) is a potential therapeutic strategy against human colorectal cancer (CRC). In this study, we synthesized a series of novel thiazolo[4,5-d]pyrimidine derivatives (PB-1–12) and identified PB-10 (PAK4 IC50 = 15.12 μM) as a potential and potent PAK4 inhibitor. Our results showed that PB-10 significantly suppressed the proliferation and colony formation of human CRC cells. PB-10 also arrested HCT-116 CRC cells at sub G0/G1 phase while promoting the expression of proapoptotic proteins. In addition, PB-10 inhibited migration, invasion, and adhesion as well as the PAK4 downstream signaling pathway in HCT-116 cells. Molecular docking analysis showed possible binding modes between PB-10 and PAK4. Our study provides a novel compound that may block the PAK4 signaling in CRC cells.

NOVEL THIAZOLOPYRIMIDINE COMPOUNDS

The invention provides certain thiazolopyrimidine compounds, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.