Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors

By rational design and modification, compound 9m showed excellent HDACs inhibitory activity, strong anti-proliferative activity against human cancer cell lines including RMPI 8226 and HCT 116. Moreover, compound 9m noticeably up-regulated the level of histone H3 acetylation at the low concentration of 0.3 μM.189