Jul 2026
Design, synthesis and evaluation of benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one derivatives as novel MTA cooperative PRMT5 inhibitors for the treatment of MTAP-deleted cancers.
Compound 9u exhibited significant antiproliferative activity in MTAP-deleted HCT116 cancer cells, with an IC50 value of 13 nM, exhibiting 70-fold selectivity over MTAP wild type HCT116 cells, and 9u displayed robust efficacy across diverse MTAP-deleted cancer cell lines, achieving IC50 values of <1.5-51 nM.
Bing Liu, Shao-Yan Li, Hui Shi et al.
· Bioorganic chemistry (Print) · 0 citations